Zeitschriftenartikel: „Cucurbitacin D“

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Ku, Jin Mo, Se Hyang Hong, Hyo In Kim, Ye Seul Lim, Sol Ji Lee, Mia Kim, Hye Sook Seo, Yong Cheol Shin und Seong-Gyu Ko. „Cucurbitacin D exhibits its anti-cancer effect in human breast cancer cells by inhibiting Stat3 and Akt signaling“. European Journal of Inflammation 16 (01.01.2018): 1721727X1775180. http://dx.doi.org/10.1177/1721727x17751809.

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Cucurbitacins are triterpenoids commonly found in Cucurbitaceae and Cruciferae and have long been used in traditional medicine. Cucurbitacins demonstrate anti-inflammatory and anti-cancer activities. We investigated whether cucurbitacin D affects viability in breast cancer cells and its mechanism of action. An MTT assay was used to measure the viability of breast cancer cells. Western blot analysis was used to measure the expression of various modulators, such as p-p53, p-Stat3, p-Akt, and p-NF-κB. Doxorubicin and cucurbitacin D affected the viability of MCF7, MDA-MB-231, and SKBR3 cells. Cucurbitacin D and doxorubicin increased p-p53 expression in MCF7, SKBR3, and MDA-MB-231 cells. Cucurbitacin D suppressed p-Akt, p-NF-κB, and p-Stat3 expression in MCF7, MDA-MB-231, and SKBR3 cells. Doxorubicin alone did not decrease p-Akt and p-Stat3 levels. Cucurbitacin D decreased p-NF-κB and p-Stat3 levels. Doxorubicin in combination with cucurbitacin D increased p-p53 levels and suppressed Akt, NF-κB, Stat3, and Bcl-2 expression more than cucurbitacin D alone. Our results clearly demonstrate that cucurbitacin D could be a useful compound for treating human breast cancer.

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Tosun, Emir, und Ahmet Baysar. „Simultaneous isolation and purification of cucurbitacin D and I from Ecballium elaterium (l.) A. Rich fruit juice“. Macedonian Journal of Chemistry and Chemical Engineering 38, Nr. 2 (30.12.2019): 171. http://dx.doi.org/10.20450/mjcce.2019.1648.

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The objective of this study was to develop a rapid, economic, and efficient method for simultaneous selective isolation, separation, and purification of cucurbitacin D and I from Ecballium elaterium (L.) A. Rich fruit juice via reversed-phase flash chromatography combined with HPLC. The chloroform extract of the fruit juice was fractionated with flash chromatography using a chloroform, acetone and methanol solvent combination at a 5 ml/min flow rate. Then, a validated HPLC method was utilized for purification of the two targeted cucurbitacins. Cucurbitacin D and I were collected automatically by the fraction collector. The fractions containing the same compounds were pooled and lyophilized. The purified cucurbitacin D and I compounds were identified by NMR, LC-MS, and UV spectra analysis. The results suggest that the applied procedure is simple, quick, and highly efficient. The HPLC method was found to be linear, accurate, precise and rugged for the quantification of the cucurbitacins studied.

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Abdel Halim, Osama B., El-Sayed M. Marawan, Ali A. El-Gamal und Mona G. Zaghloul. „Socotroside, a New Pentacyclic Cucurbitane Glycoside from Dendrosicyos socotrana“. Zeitschrift für Naturforschung B 63, Nr. 12 (01.12.2008): 1415–20. http://dx.doi.org/10.1515/znb-2008-1212.

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Phytochemical investigation of the ethyl acetate extract of the stem of Dendrosicyos socotrana Balf. f. resulted in the isolation of a new pentacyclic cucurbitane glycoside Socotroside, in addition to the three known cucurbitacins, dihydrocucurbitacin D, dihydrocucurbitacin F and cucurbitacin G. The structures of the isolated compounds were established on the basis of their spectral data. The isolated cucurbitacin aglycones showed marked cytotoxic activity.

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Cai, Yuee, Xiefan Fang, Chengwei He, Peng Li, Fei Xiao, Yitao Wang und Meiwan Chen. „Cucurbitacins: A Systematic Review of the Phytochemistry and Anticancer Activity“. American Journal of Chinese Medicine 43, Nr. 07 (Januar 2015): 1331–50. http://dx.doi.org/10.1142/s0192415x15500755.

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Cucurbitacins are highly oxidized tetracyclic triterpenoids that are widely present in traditional Chinese medicines (Cucurbitaceae family), possess strong anticancer activity, and are divided into 12 classes from A to T with over 200 derivatives. The eight most active cucurbitacin components against cancer are cucurbitacin B, D, E, I, IIa, L glucoside, Q, and R. Their mechanisms of action include antiproliferation, inhibition of migration and invasion, proapoptosis, and cell cycle arrest promotion. Cucurbitacins are also found to be the inhibitors of JAK-STAT3, Wnt, PI3K/Akt, and MAPK signaling pathways, which play important roles in the apoptosis and survival of cancer cells. Recently, new studies have discovered synergistic anticancer effects by using cucurbitacins together with clinically approved chemotherapeutic drugs, such as docetaxel and methotrexate. This paper provides a summary of recent research progress on the anticancer property of cucurbitacins and the various intracellular signaling pathways involved in the regulation of cancer cell proliferation, death, invasion, and migration. Therefore, cucurbitacins are a class of promising anticancer drugs to be used alone or be intergraded in current chemotherapies and radiotherapies to treat many types of cancers.

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Muñoz, Orlando, Carla Delporte, Nadine Backhouse, Silvia Erazo, Rosa Negrete, Sergio Maldonado, José L. López-Pérez und Arturo San Feliciano. „A New Cucurbitacin Glycoside from Kageneckia oblonga (Rosaceae)“. Zeitschrift für Naturforschung C 55, Nr. 3-4 (01.04.2000): 141–45. http://dx.doi.org/10.1515/znc-2000-3-403.

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Abstract A novel cucurbitacin glycoside has been isolated from aerial parts of Kageneckia oblonga R. et P. and shown to be 3β-(β-D-glucosyloxy)-16α,23α-epoxycucurbita-5,24-dien-11-one. The structure was established by usual spectroscopic and two-dimensional (2D ) NMR techniques. This compound has found to be nontoxic when tested in-vivo cell culture assays. In previous investigations we reported 23,24-dihydrocucurbitacin F and prunasine. This was the first report on cucurbitacins from the genus Kageneckia (Rosaceae).

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Mu, Shicheng, Jiao Li, Cui Liu, Yan Zeng, Yan Men, Yi Cai, Ning Chen, Hongwu Ma und Yuanxia Sun. „Effective Glycosylation of Cucurbitacin Mediated by UDP-Glycosyltransferase UGT74AC1 and Molecular Dynamics Exploration of Its Substrate Binding Conformations“. Catalysts 10, Nr. 12 (15.12.2020): 1466. http://dx.doi.org/10.3390/catal10121466.

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Cucurbitacins, a group of diverse tetracyclic triterpenes, display a variety of biological effects. Glycosylation mediated by glycosyltransferases (UGTs) plays a vital role in structural and functional diversity of natural products and influences their biological activities. In this study, GT-SM, a mutant of UGT74AC1 from Siraitia grosvenorii, was chosen as a potential catalyst in glycosylation of cucurbitacins, and its optimal pH, temperature, and divalent metal ions were detected. This enzyme showed high activity (kcat/Km, 120 s−1 µM−1) toward cucurbitacin F 25-O-acetate (CA-F25) and only produced CA-F25 2-O-β-d-glucose which was isolated and confirmed by 1D and 2D nuclear magnetic resonance. A pathway for uridine diphosphate glucose (UDP-Glc) regeneration and cucurbitacin glycoside synthesis was constructed by combing GT-SM and sucrose synthase to cut down the costly UDP-Glc. The molar conversion of CA-F25 was 80.4% in cascade reaction. Molecular docking and dynamics simulations showed that CA-F25 was stabilized by hydrophobic interactions, and the C2-OH of CA-F25 showed more favorable catalytic conformation than that of C3-OH, explaining the high regioselectivity toward the C2-OH rather than the ortho-C3-OH of CA-F25. This work proved the important potential application of UGT74AC1 in cucurbitacins and provided an understanding of glycosylation of cucurbitacins.

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D. Sarker, Satyajit, Pensri Whiting, René Lafont, Jean-Pierre Girault und Laurence Dinan. „Cucurbitacin D from Cercidiphyllum japonicum“. Biochemical Systematics and Ecology 25, Nr. 1 (Januar 1997): 79–80. http://dx.doi.org/10.1016/s0305-1978(96)00093-2.

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Delporte, Carla, Orlando Muñozb, Javier Rojas, Marisa Ferrándiz, Miguel Payá, Silvia Erazo, Rosa Negrete, Sergio Maldonado, Arturo San Feliciano und Nadine Backhouse. „Pharmaco-Toxicological Study of Kageneckia oblonga, Rosaceae“. Zeitschrift für Naturforschung C 57, Nr. 1-2 (01.02.2002): 100–108. http://dx.doi.org/10.1515/znc-2002-1-218.

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The probable antipyretic, antiinflammatory, analgesic and antioxidant properties of Kageneckia oblonga, Rosaceae, were investigated and the major compounds of its active extracts were isolated. The study comprised the acute toxicity of the extracts of global methanol, hexane, dichloromethane and methanol. The cytotoxicity of global methanol extract was studied in three tumoral cell lines. All the extracts exhibited the pharmacological activities under study. Methanol and dichloromethane were the most toxic extracts. From the global methanol extract, isolations were performed of prunasin, 23,24- dihydro-cucurbitacin F, and a new cucurbitacin, 3β-(β-d-glucosyloxy)-16α,23α-epoxycucurbita-5,24-diene-11-one. The cytotoxicity of both cucurbitacins on human neutrophils at the assayed concentrations was not statistically significant. In-vitro assays showed that both cucurbitacins can be partly responsible for the analgesic, antipyretic, and anti-inflammatory activities. Evaluation was done of the cytotoxicity of global methanol extract, 23, 24-dihydrocucurbitacin F, aqueous extracts and prunasin against P-388 murine leukaemia, A-549 human lung carcinoma and HT-29 colon carcinoma. Since global methanol extract presented a strong cytotoxicity against P-388 murine leukaemia, A-549 human lung carcinoma, and HT-29 cell lines, it is highly probable that this extract contain one or more cytotoxic compounds that could be investigated for their potential use as an agent against cancer.

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DINAN, Laurence, Pensri WHITING, Jean-Pierre GIRAULT, René LAFONT, S. Tarlochan DHADIALLA, E. Dean CRESS, Bruno MUGAT, Christophe ANTONIEWSKI und Jean-Antoine LEPESANT. „Cucurbitacins are insect steroid hormone antagonists acting at the ecdysteroid receptor“. Biochemical Journal 327, Nr. 3 (01.11.1997): 643–50. http://dx.doi.org/10.1042/bj3270643.

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Two triterpenoids, cucurbitacins B and D, have been isolated from seeds of Iberis umbellata (Cruciferae) and shown to be responsible for the antagonistic activity of a methanolic extract of this species in preventing the 20-hydroxyecdysone (20E)-induced morphological changes in the Drosophila melanogaster BII permanent cell line. With a 20E concentration of 50 nM, cucurbitacins B and D give 50% responses at 1.5 and 10 μM respectively. Both cucurbitacins are able to displace specifically bound radiolabelled 25-deoxy-20-hydroxyecdysone (ponasterone A) from a cell-free preparation of the BII cells containing ecdysteroid receptors. The Kd values for cucurbitacins B and D (5 and 50 μM respectively) are similar to the concentrations required to antagonize 20E activity with whole cells. Cucurbitacin B (cucB) prevents stimulation by 20E of an ecdysteroid-responsive reporter gene in a transfection assay. CucB also prevents the formation of the Drosophila ecdysteroid receptor/Ultraspiracle/20E complex with the hsp27 ecdysteroid response element as demonstrated by gel-shift assay. This is therefore the first definitive evidence for the existence of antagonists acting at the ecdysteroid receptor. Preliminary structure/activity studies indicate the importance of the Δ23-22-oxo functional grouping in the side chain for antagonistic activity. Hexanorcucurbitacin D, which lacks carbon atoms C-22 to C-27, is found to be a weak agonist rather than an antagonist. Moreover, the side chain analogue 5-methylhex-3-en-2-one possesses weak antagonistic activity.

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Sikander, Mohammed, Shabnam Malik, Neeraj Chauhan, Parvez Khan, Sonam Kumari, Vivek Kashyap, Sheema Khan et al. „Cucurbitacin D Reprograms Glucose Metabolic Network in Prostate Cancer“. Cancers 11, Nr. 3 (14.03.2019): 364. http://dx.doi.org/10.3390/cancers11030364.

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Prostate cancer (PrCa) metastasis is the major cause of mortality and morbidity among men. Metastatic PrCa cells are typically adopted for aberrant glucose metabolism. Thus, chemophores that reprogram altered glucose metabolic machinery in cancer cells can be useful agent for the repression of PrCa metastasis. Herein, we report that cucurbitacin D (Cuc D) effectively inhibits glucose uptake and lactate production in metastatic PrCa cells via modulating glucose metabolism. This metabolic shift by Cuc D was correlated with decreased expression of GLUT1 by its direct binding as suggested by its proficient molecular docking (binding energy −8.5 kcal/mol). Cuc D treatment also altered the expression of key oncogenic proteins and miR-132 that are known to be involved in glucose metabolism. Cuc D (0.1 to 1 µM) treatment inhibited tumorigenic and metastatic potential of human PrCa cells via inducing apoptosis and cell cycle arrest in G2/M phase. Cuc D treatment also showed inhibition of tumor growth in PrCa xenograft mouse model with concomitant decrease in the expression of GLUT1, PCNA and restoration of miR-132. These results suggest that Cuc D is a novel modulator of glucose metabolism and could be a promising therapeutic modality for the attenuation of PrCa metastasis.

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Song, Yuan, Ning Ding, Tamotsu Kanazawa, Uki Yamashita und Yasuhiro Yoshida. „Cucurbitacin D is a new inflammasome activator in macrophages“. International Immunopharmacology 17, Nr. 4 (Dezember 2013): 1044–50. http://dx.doi.org/10.1016/j.intimp.2013.10.003.

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Zubair, Muhammad Sulaiman, Walied Mohamed Alarif, Mohamed Ali Ghandourah, Syariful Anam und Ibrahim Jantan. „Cytotoxic Activity of 2-O-β-glucopyranosil Cucurbitacin D from Benalu Batu (Begonia sp.) Growing in Morowali, Central Sulawesi“. Indonesian Journal of Chemistry 20, Nr. 4 (10.06.2020): 766. http://dx.doi.org/10.22146/ijc.43626.

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Benalu batu (Begonia sp.) had been used traditionally as an anticancer medicinal plant by Wana tribe in Morowali, Central Sulawesi, This study aims to evaluate the cytotoxic activity of 2-O-β-glucopyranosil cucurbitacin D, isolated from the ethyl acetate soluble fraction of Benalu batu (Begonia sp.) and to determine its action on apoptosis induction. Benalu batu (Begonia sp.) herb was extracted by maceration using ethanol 96% as a solvent. Vacuum liquid column chromatography and preparative thin layer chromatography have been applied on fractionation and isolation of the compound. The structure elucidation was performed by extensive analysis of 1D/2D nuclear magnetic resonance (NMR) and Mass Spectrophotometer (MS). Cytotoxic activity against human breast adenocarcinoma (MCF-7) and human colon colorectal carcinoma (HCT-116) cell lines were performed by 5-diphenyltetrazolium bromide (MTT) method. Annexin V-FITC assay was employed to determine the apoptosis induction. 2-O-β-glucopyranosil cucurbitacin D showed potent cytotoxic activity against MCF-7 and HCT-116 with the IC50 of 19.913 and 0.002 μg/mL, respectively. Annexin V-FITC assay clearly exhibited the cytotoxic mechanism on MCF-7 and HCT-116 via apoptosis induction with a significant percentage of early and late apoptosis of 75.8 and 78.4%, respectively. This study reveals the potential cytotoxic activity of 2-O-β-glucopyranosil cucurbitacin D isolated from Benalu batu and its mechanism via apoptosis induction.

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Hall, Jessica A., Sahithi Seedarala, Nichole Rice, Lucas Kopel, Fathi Halaweish und Brian S. J. Blagg. „Cucurbitacin D Is a Disruptor of the HSP90 Chaperone Machinery“. Journal of Natural Products 78, Nr. 4 (10.03.2015): 873–79. http://dx.doi.org/10.1021/acs.jnatprod.5b00054.

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Maatooq, Galal, Saleh El-Sharkawy, M. S. Afifi und J. P. N. Rosazza. „Microbial Transformation of Cucurbitacin E 2-O-β-D-Glucopyranoside“. Journal of Natural Products 58, Nr. 2 (Februar 1995): 165–71. http://dx.doi.org/10.1021/np50116a001.

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DeMilo, A. B., C. J. Lee, R. F. W. Schroder, W. F. Schmidt und D. J. Harrison. „Spectral Characterization of Cucurbitacins in a Bitter Mutant of Hawkesbury Watermelon (Citrullus vulgaris Schrad) that Elicit a Feeding Response to Diabroticite Beetles (Coleoptera: Chrysomelidae)2“. Journal of Entomological Science 33, Nr. 4 (01.10.1998): 343–54. http://dx.doi.org/10.18474/0749-8004-33.4.343.

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Fractions obtained by open-column flash chromatography of a crude methanolic extract of the rind of a bitter mutant of Hawkesbury watermelon, Citrullus vulgaris Schrad, were further purified by preparative high-performance liquid chromatography (HPLC) to isolate chemical component(s) that elicit a visitation/feeding stimulancy response to the southern corn rootworm, Diabrotica undecimpunctata howardi Barber. Activity of chromatographic fractions were followed with a laboratory bioassay involving total insect-response counts. The chemical structure of the most active component in C. vulgaris was confirmed by chemical ionization mass spectrometry and proton nuclear magnetic resonance spectroscopy to be cucurbitacin-E glycoside. Two other cucurbitacin-like compounds were isolated and structures for them postulated. A procedure to prepare a crude, biologically active, extract of C. vulgaris is reported. Dose-response data for the crude extract in laboratory tests against two diabroticite beetles D. undecimpunctata howardi and D. virgifera virgifera LeConte are also reported.

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Mei, Jianfeng, Xia Wu, Sujing Zheng, Xiang Chen, Zhuliang Huang und Yichun Wu. „Improvement of Cucurbitacin B Content in Cucumis melo Pedicel Extracts by Biotransformation Using Recombinant β-Glucosidase“. Separations 8, Nr. 9 (01.09.2021): 138. http://dx.doi.org/10.3390/separations8090138.

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For the efficient biotransformation of cucurbitacin B 2-o-β-d-glucoside (CuBg) to cucurbitacin B (CuB) in Cucumis melo pedicel extracts, the β-glucosidase gene bglS—consisting of 1344 bp (447 amino acids) from Streptomyces sp. RW-2—was cloned and expressed in Escherichia coli BL21(DE3). The activity of recombinant β-glucosidase with p-nitrophenyl-β-d-glucoside (pNPG) as a substrate was 3.48 U/mL in a culture. Using the recombinant β-glucosidase for the biotransformation of C. melo pedicel extracts, CuBg was converted into CuB with a conversion rate of 87.6% when the concentration of CuBg was 0.973 g/L in a reaction mixtures. The concentration of CuB in C. melo pedicel extracts was improved from 13.6 to 20.2 g/L after biotransformation. The present study provides high-efficiency technology for the production of CuB from its glycoside by biotransformation.

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Salom, Scott M., Jodi A. Gray, A. Randall Alford, Melinda Mulesky, Chris J. Fettig und Steve A. Woods. „Evaluation of Natural Products as Antifeedants for the Pales Weevil (Coleoptera: Curculionidae) and as Fungitoxins for Leptographium procerum“. Journal of Entomological Science 31, Nr. 4 (01.10.1996): 453–65. http://dx.doi.org/10.18474/0749-8004-31.4.453.

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Four natural plant compounds (limonin, S (+) and R (−) carvone, and cucurbitacin) and one insect pheromone (verbenone) were evaluated for antifeedant activity against the pales weevil, Hylobius pales (Herbst), on Pinus strobus seedlings and for toxic activity against the pathogenic fungus, Leptographium procerum (Kendrick) Wingfield, which is vectored by H. pales to P. strobus. All compounds demonstrated significant antifeedant activity in a choice test on treated pine seedlings, but none completely eliminated feeding. Only cucurbitacin elicited a linear dose-response relationship, with significant activity occurring at concentrations as low as 0.10 μg/ml. The other compounds significantly reduced feeding at concentrations as low as 1 μg/ml (the lowest concentration at which they were tested). Total feeding activity was unaffected for all but one treatment (S (+) carvone at 1 μg/ml) when compared with feeding on the untreated control seedlings. It is, therefore, unlikely that the compounds in this study were toxic to the weevils during the 2 d evaluation period. In the fungitoxin test, all compounds except cucurbitacin suppressed germination of L. procerum spores. R (−) carvone was the most effective, allowing only 5% germination at 1 μg/ml, compared to 96% germination in the water solvent.

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Seger, Christoph, Sonja Sturm, Ernst Haslinger und Hermann Stuppner. „NMR Signal Assignment of 22-Deoxocucurbitacin D and Cucurbitacin D from Ecballium elaterium L. (Cucurbitaceae)“. Monatshefte für Chemie - Chemical Monthly 136, Nr. 9 (12.08.2005): 1645–49. http://dx.doi.org/10.1007/s00706-005-0347-2.

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Ali, Mohammad Ajmal, Mohammad Abul Farah, Joongku Lee, Khalid M. Al-Anazi und Fahad M. A. Al-Hemaid. „Molecular Insights into the Interaction of Ursolic Acid and Cucurbitacin from Colocynth with Therapeutic Targets of Mycobacterium tuberculosis“. Letters in Drug Design & Discovery 17, Nr. 10 (12.10.2020): 1309–18. http://dx.doi.org/10.2174/1570180817999200514102750.

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Aims: Medicinal plants like Citrullus colocynthis are a potential choice to produce helpful novel antimycobacterial drugs. The existence of a range of natural products in the plants, especially Ursolic Acid (UA) and cucurbitacin E 2-0-β-d-glucopyranoside (CEG), with promising antibacterial activity against a variety of bacteria, prompted the need to check its actions against Mycobacterium tuberculosis (Mtb). Background: Mycobacterium tuberculosis (Mtb), an obligate human pathogen causes tuberculosis and is one of the major causes of death worldwide. A few combinations of drugs are currently accessible for treating TB patients, but these are inadequate to tackle worldwide TB cases. Objective: The molecular interactions between ursolic acid and cucurbitacin E with the eight potential Mtb target proteins were investigated with the objective of finding drug-like inhibitors. Methods: Avogadro v.1.2.0 and Openbabel v.2.4.1 were used for creating file formats required for docking analysis. Molecular docking was performed with eight different proteins essential for Mtb metabolism and survival. AutoDock v.4.2 and AutoDock vina v.1.1.2 were used for docking and Gromacs 5.1.4 was used for simulation studies. Results and Discussion: Among the two ligands used in this research, cucurbitacin E showed a better docking score relative to the drugs presently available for all the target proteins. Rifampicin showed the best binding affinity (among known inhibitors) i.e. -10.8 kcal/mol with C terminal caspase recruitment domain. Moreover, ursolic acid and cucurbitacin E showed uniform binding score (above -7.5 kcal/mol) with all the target proteins, acknowledged its availability as a potential multi-target drug. Conclusion: Ursolic acid can be useful in the creation of novel, multi-targeted and effective anti- TB medicines since it showed stable structure with FabH.

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Eddy, Nicholas A., und Gabriel Fenteany. „Model studies directed to the synthesis of cucurbitacin I C/D rings“. Tetrahedron Letters 56, Nr. 36 (September 2015): 5079–81. http://dx.doi.org/10.1016/j.tetlet.2015.07.044.

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Sarker, Satyajit D., René Lafont, Vladimir Šik und Laurence Dinan. „Arvenin I (Cucurbitacin B 2-O-β-d-Glucopyranoside) from Iberis umbellata“. Biochemical Systematics and Ecology 25, Nr. 4 (Juni 1997): 365–66. http://dx.doi.org/10.1016/s0305-1978(97)00017-3.

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Seger, Christoph, Sonja Sturm, Ernst Haslinger und Hermann Stuppner. „A New Cucurbitacin D Related 16,23-Epoxy Derivative and Its Isomerization Products“. Organic Letters 6, Nr. 4 (Februar 2004): 633–36. http://dx.doi.org/10.1021/ol036469r.

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Barbercheck, M. E., und J. Wang. „Effect of Cucurbitacin D onin VitroGrowth ofXenorhabdusandPhotorhabdusspp., Symbiotic Bacteria of Entomopathogenic Nematodes“. Journal of Invertebrate Pathology 68, Nr. 2 (September 1996): 141–45. http://dx.doi.org/10.1006/jipa.1996.0071.

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Ventura, Maurício Ursi, Claudio Cezar Mariano Resta, Daiane Heloísa Nunes und Fabio Fujimoto. „Trap attributes influencing capture of Diabrotica speciosa (Coleoptera: Chrysomelidae) on common bean fields“. Scientia Agricola 62, Nr. 4 (August 2005): 351–56. http://dx.doi.org/10.1590/s0103-90162005000400008.

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Refinements in trap characteristics may improve ability to monitor and mass-trap beetles. Field assays were conducted in common bean fields to assess responses of Diabrotica speciosa (Germar) to some trap characteristics. Golden yellow plastic cups (750 mL) traps caught more D. speciosa females and males than did clear traps. Carrot slices in Petri dishes baited with Lagenaria vulagaris L. powder (cucurbitacin source - 0.28%) caught more beetles than did dishes with carrot alone. Dispensers for the floral volatile attractant 1,4-dimethoxybenze were also compared. Rubber septa dispenser attracted more beetles than did control (dental wicks saturated with acetone). Captures on dental wick, starch matrix and feminine pad dispensers were intermediate and did not differ from those on rubber septa and unbaited controls. Perforated bottle traps (2000 mL), when baited with the floral attractant, caught more beetles than did window bottle traps (both traps contained L. vulgaris powder) in most assessments done from two to ten days after trap placement in the field. Traps with the insecticide carbaryl captured more beetles than did traps without it, 2-4 and 8-10 days after trap placement in the field, but not in the remaining periods (0-2, 4-6 and 6-8 days). Traps baited with 1,4-dimethoxybenzene captured more beetles than did the unbaited ones in all assessments (each other day from two to ten days after trap placement in the field). Finally, similar amounts of beetles were captured using plastic bottle traps (2000 mL): perforated, window (both with cucurbitacin) and sticky (without cucurbitacin) traps, when were baited with the floral attractant.

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Xing, Hongtao, Siwei Zhang, H. Phillip Koeffler und Ming Chiu Fung. „Cucurbitacin D Upregulates Fetal Hemoglobin Expression in K562 Cells and Human Erythroid Progenitors.“ Blood 110, Nr. 11 (16.11.2007): 3833. http://dx.doi.org/10.1182/blood.v110.11.3833.3833.

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Abstract The search for novel therapeutic candidates causing reactivation of fetal hemoglobin (a2g2; HbF) to reduce the imbalance of globin gene expression is important in order to develop effective approach for the clinical management of sickle cell anemia and b-thalassemia. For the first time, we have identified cucurbitacin D (CuD), a naturally occurring oxygenated tetracyclic triterpenoid, as a molecular entity inducing g-globin gene expression and HbF synthesis in K562 cells and human erythroid progenitors from either peripheral blood or bone marrow. The upregulation of HbF induced by CuD was dose- and time- dependent. CuD was compared to hydroxyurea (HU), 5-azacytidine, amifostine, recombinant human erythropoietin (rhEPO), and sodium phenylbutyrate. At their optimal dosage, CuD (12.5 ng/mL) and HU (25.0 μg/mL) induced nearly 70% K562 cells to express total hemoglobin after 6 days culture, which was higher than the induction by Amifostine (30%), 5-azacytidine (36%), rhEPO (16%), sodium phenylbutyrate (23%) at their optimal concentrations and negative control (11%). Fetal hemoglobin ELISA showed that CuD (12.5 ng/mL) and 5-azacytidine (400 ng/mL) induced higher levels of fetal hemoglobin in K562 cells (15.4 ng/μL and 29.3 ng/μL, respectively), compared to HU (10.3 ng/μL), amifostine (7.8 ng/μL), rhEPO (10.9 ng/μL), sodium phenylbutyrate (9.9 ng/μL) at their optimal concentrations and negative control (5.3 ng/μL). CuD induced a significantly higher fetal cell percentage than HU in K562 cells (65% vs 37% maximum) and primary erythroid progenitors (36% vs 21% maximum) based on the immunofluorescence imaging and flow cytometry analysis. Real-time PCR results showed that the amount of γ-globin mRNA increased from 2.5-fold in CuD-optimal-treated cells (12.5 ng/mL, 48 hours) compared with 1.5-fold in HU-optimal-treated cells (25.0 μg/mL, 48 hours). Growth inhibition assay (MTT) demonstrated that CuD at its optimal γ-globin inducing dosage (12.5 ng/mL) inhibited proliferation of K562 by less than 10% of untreated control cells; while hydroxyurea at its optimal dosage (25.0 μg/mL) inhibited 80% of cell division. The in vitro therapeutic index (calculated by dividing the dose inhibiting 50% cell growth (IC50) by dose inducing 50% maximal HbF production (ED50)) of CuD was 40-fold greater than HU. Taken together, the results suggest that CuD has the potential to be a therapeutic agent for treatment of sickle cell anemia and b-thalassemia.

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Rizvi, Tania Shamim, Liaqat Ali, Sahar Sulaiman Al-Rawahi und Ahmed Al-Harrasi. „New p-Terphenyl from the Fruit of Citrullus colocynthis (Cucurbitaceae)“. Natural Product Communications 12, Nr. 7 (Juli 2017): 1934578X1701200. http://dx.doi.org/10.1177/1934578x1701200724.

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One new substituted p-terphenyl (1) has been isolated along with the known metabolites; cucurbitacin E 2-O-β-D-glucoside (2) and α-amyrin (3) from ethyl acetate and dichloromethane fractions of fruit extract of Citrullus colocynthis. The structure of the new metabolite was elucidated by combined analysis of 1D (1H and 13C) and 2D (HSQC and HMBC correlations) NMR and MS spectral data. The known metabolites were characterized by comparison of the spectral data with those reported in literature.

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Sikander, Mohammed, Shabnam Malik, Sheema Khan, Sonam Kumari, Neeraj Chauhan, Parvez Khan, Fathi T. Halaweish et al. „Novel Mechanistic Insight into the Anticancer Activity of Cucurbitacin D against Pancreatic Cancer (Cuc D Attenuates Pancreatic Cancer)“. Cells 9, Nr. 1 (31.12.2019): 103. http://dx.doi.org/10.3390/cells9010103.

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Pancreatic cancer (PanCa) is one of the leading causes of death from cancer in the United States. The current standard treatment for pancreatic cancer is gemcitabine, but its success is poor due to the emergence of drug resistance. Natural products have been widely investigated as potential candidates in cancer therapies, and cucurbitacin D (Cuc D) has shown excellent anticancer properties in various models. However, there is no report on the therapeutic effect of Cuc D in PanCa. In the present study, we investigated the effects of the Cuc D on PanCa cells in vitro and in vivo. Cuc D inhibited the viability of PanCa cells in a dose and time dependent manner, as evident by MTS assays. Furthermore, Cuc D treatment suppressed the colony formation, arrest cell cycle, and decreased the invasion and migration of PanCa cells. Notably, our findings suggest that mucin 13 (MUC13) is down-regulated upon Cuc D treatment, as demonstrated by Western blot and qPCR analyses. Furthermore, we report that the treatment with Cuc D restores miR-145 expression in PanCa cells/tissues. Cuc D treatment suppresses the proliferation of gemcitabine resistant PanCa cells and inhibits RRM1/2 expression. Treatment with Cuc D effectively inhibited the growth of xenograft tumors. Taken together, Cuc D could be utilized as a novel therapeutic agents for the treatment/sensitization of PanCa.

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Ding, Ning, Uki Yamashita, Hidetada Matsuoka, Tsutomu Sugiura, Junichi Tsukada, Junko Noguchi und Yasuhiro Yoshida. „Apoptosis induction through proteasome inhibitory activity of cucurbitacin D in human T-cell leukemia“. Cancer 117, Nr. 12 (23.12.2010): 2735–46. http://dx.doi.org/10.1002/cncr.25711.

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Tavares, Marina R., Klára Hrabánková, Rafał Konefał, Martin Kaňa, Blanka Říhová, Tomáš Etrych, Milada Šírová und Petr Chytil. „HPMA-Based Copolymers Carrying STAT3 Inhibitor Cucurbitacin-D as Stimulus-Sensitive Nanomedicines for Oncotherapy“. Pharmaceutics 13, Nr. 2 (28.01.2021): 179. http://dx.doi.org/10.3390/pharmaceutics13020179.

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The study describes the synthesis, physicochemical properties, and biological evaluation of polymer therapeutics based on N-(2-hydroxypropyl)methacrylamide (HPMA) copolymers intended for a tumor-targeted immuno-oncotherapy. Water-soluble linear and cholesterol-containing HPMA precursors were synthesized using controlled reversible addition–fragmentation chain transfer polymerization to reach molecular weight Mn about 2 × 104 g·mol−1 and low dispersity. These linear or self-assembled micellar conjugates, containing immunomodulatory agent cucurbitacin-D (CuD) or the anticancer drug doxorubicin (Dox) covalently bound by the hydrolytically degradable hydrazone bond, showed a hydrodynamic size of 10–30 nm in aqueous solutions. The CuD-containing conjugates were stable in conditions mimicking blood. Importantly, a massive release of active CuD in buffer mimicking the acidic tumor environment was observed. In vitro, both the linear (LP-CuD) and the micellar (MP-CuD) conjugates carrying CuD showed cytostatic/cytotoxic activity against several cancer cell lines. In a murine metastatic and difficult-to-treat 4T1 mammary carcinoma, only LP-CuD showed an anticancer effect. Indeed, the co-treatment with Dox-containing micellar polymer conjugate and LP-CuD showed potentiation of the anticancer effect. The results indicate that the binding of CuD, characterized by prominent hydrophobic nature and low bioavailability, to the polymer carrier allows a safe and effective delivery. Therefore, the conjugate could serve as a potential component of immuno-oncotherapy schemes within the next preclinical evaluation.

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Kodidela, Sunitha, Namita Sinha, Asit Kumar und Santosh Kumar. „Anti-HIV Activity of Cucurbitacin-D against Cigarette Smoke Condensate-Induced HIV Replication in the U1 Macrophages“. Viruses 13, Nr. 6 (27.05.2021): 1004. http://dx.doi.org/10.3390/v13061004.

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Chemodietary agents are emerging as promising adjuvant therapies in treating various disease conditions. However, there are no adjuvant therapies available to minimize the neurotoxicity of currently existing antiretroviral drugs (ARVs). In this study, we investigated the anti-HIV effect of a chemodietary agent, Cucurbitacin-D (Cur-D), in HIV-infected macrophages using an in-vitro blood–brain barrier (BBB) model. Since tobacco smoking is prevalent in the HIV population, and it exacerbates HIV replication, we also tested the effect of Cur-D against cigarette smoke condensate (CSC)-induced HIV replication. Our results showed that Cur-D treatment reduces the viral load in a dose-dependent (0–1 μM) manner without causing significant toxicity at <1 μM concentration. Further, a daily dose of Cur-D (0.1 μM) not only reduced p24 in control conditions, but also reduced CSC (10 μg/mL)-induced p24 in U1 cells. Similarly, Cur-D (single dose of 0.4 μM) significantly reduced the CSC (single dose of 40 μg/mL)-induced HIV replication across the BBB model. In addition, treatment with Cur-D reduced the level of pro-inflammatory cytokine IL-1β. Therefore, Cur-D, as an adjuvant therapy, may be used not only to suppress HIV in the brain, but also to reduce the CNS toxicity of currently existing ARVs.

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Takahashi, Norito, Yasuhiro Yoshida, Tsutomu Sugiura, Koji Matsuno, Akihiro Fujino und Uki Yamashita. „Cucurbitacin D isolated from Trichosanthes kirilowii induces apoptosis in human hepatocellular carcinoma cells in vitro“. International Immunopharmacology 9, Nr. 4 (April 2009): 508–13. http://dx.doi.org/10.1016/j.intimp.2009.01.006.

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Yoshida, Yasuhiro, und Ding Ning. „PS3-59 Enhanced effect of new proteasome inhibitor cucurbitacin D on LPS-Induced IL-1“. Cytokine 52, Nr. 1-2 (Oktober 2010): 94. http://dx.doi.org/10.1016/j.cyto.2010.07.398.

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Wan, Jiang, Xiao-Juan Wang, Nan Guo, Xi-Ying Wu, Juan Xiong, Yi Zang, Chun-Xiao Jiang, Bing Han, Jia Li und Jin-Feng Hu. „Highly Oxygenated Triterpenoids and Diterpenoids from Fructus Rubi (Rubus chingii Hu) and Their NF-kappa B Inhibitory Effects“. Molecules 26, Nr. 7 (29.03.2021): 1911. http://dx.doi.org/10.3390/molecules26071911.

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During a phytochemical investigation of the unripe fruits of Rubus chingii Hu (i.e., Fructus Rubi, a traditional Chinese medicine named “Fu-Pen-Zi”), a number of highly oxygenated terpenoids were isolated and characterized. These included nine ursane-type (1, 2, and 4–10), five oleanane-type (3, 11–14), and six cucurbitane-type (15–20) triterpenoids, together with five ent-kaurane-type diterpenoids (21–25). Among them, (4R,5R,8R,9R,10R,14S,17S,18S,19R,20R)-2,19α,23-trihydroxy-3-oxo-urs-1,12-dien-28-oic acid (rubusacid A, 1), (2R*,4S*,5R*,8R*,9R*,10R*,14S*,17S*, 18S*,19R*,20R*)-2α,19α,24-trihydroxy-3-oxo-urs-12-en-28-oic acid (rubusacid B, 2), (5R,8R,9R,10R, 14S,17R,18S,19S)-2,19α-dihydroxy-olean-1,12-dien-28-oic acid (rubusacid C, 3), and (3S,5S,8S,9R, 10S,13R,16R)-3α,16α,17-trihydroxy-ent-kaur-2-one (rubusone, 21) were previously undescribed. Their chemical structures and absolute configurations were elucidated on the basis of spectroscopic data and electronic circular dichroism (ECD) analyses. Compounds 1 and 3 are rare naturally occurring pentacyclic triterpenoids featuring a special α,β-unsaturated keto-enol (diosphenol) unit in ring A. Cucurbitacin B (15), cucurbitacin D (16), and 3α,16α,20(R),25-tetrahydroxy-cucurbita-5,23- dien-2,11,22-trione (17) were found to have remarkable inhibitory effects against NF-κB, with IC50 values of 0.08, 0.61, and 1.60 μM, respectively.

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Ishii, Terukazu, Naoko Kira, Toshie Yoshida und Hisashi Narahara. „Cucurbitacin D induces growth inhibition, cell cycle arrest, and apoptosis in human endometrial and ovarian cancer cells“. Tumor Biology 34, Nr. 1 (14.11.2012): 285–91. http://dx.doi.org/10.1007/s13277-012-0549-2.

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Kim, Soon Re, Hye Sook Seo, Han-Seok Choi, Sung-Gook Cho, Yong Kuk Kim, Eun Hee Hong, Yong Cheol Shin und Seong-Gyu Ko. „Trichosanthes kirilowiiEthanol Extract and Cucurbitacin D Inhibit Cell Growth and Induce Apoptosis through Inhibition of STAT3 Activity in Breast Cancer Cells“. Evidence-Based Complementary and Alternative Medicine 2013 (2013): 1–9. http://dx.doi.org/10.1155/2013/975350.

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Trichosanthes kirilowiituber is a traditional medicine which exhibits various medicinal effects including antidiabetic and anticancer activities in several cancer cells. Recently, it was reported that Cucurbitacin D (CuD) isolated fromTrichosanthes kirilowiialso induces apoptosis in several cancer cells. Constitutive signal transducer and activator of transcription 3 (STAT3), which is an oncogenic transcription factor, is often observed in many human malignant tumor, including breast cancer. In the present study, we tested whetherTrichosanthes kirilowiiethanol extract (TKE) or CuD suppresses cell growth and induces apoptosis through inhibition of STAT3 activity in breast cancer cells. We found that both TKE and CuD suppressed proliferation and induced apoptosis and G2/M cell cycle arrest in MDA-MB-231 breast cancer cells by inhibiting STAT3 phosphorylation. In addition, both TKE and CuD inhibited nuclear translocation and transcriptional activity of STAT3. Taken together, our results indicate that TKE and its derived compound, CuD, could be potent therapeutic agents for breast cancer, blocking tumor cell proliferation and inducing apoptosis through suppression of STAT3 activity.

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Kim, Myeong-Sun, Kangwook Lee, Jin Mo Ku, Yu-Jeong Choi, Kyungyul Mok, Doori Kim, Chunhoo Cheon und Seong-Gyu Ko. „Cucurbitacin D Induces G2/M Phase Arrest and Apoptosis via the ROS/p38 Pathway in Capan-1 Pancreatic Cancer Cell Line“. Evidence-Based Complementary and Alternative Medicine 2020 (22.09.2020): 1–10. http://dx.doi.org/10.1155/2020/6571674.

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Pancreatic cancer has a poor prognosis with a five-year survival rate of less than 10%. Moreover, chemotherapy is mostly rendered ineffective owing to chemotherapy resistance and cytotoxicity. Therefore, the development of effective therapeutic strategies and novel drugs against pancreatic cancer is an urgent need. Cucurbitacin D (CuD), a plant steroid derived from Trichosanthes kirilowii, is an anticancer agent effective against various cancer cell lines. However, the anticancer activity and molecular mechanism of CuD in pancreatic cancer remain unknown. Therefore, we aimed to investigate the anticancer activity and molecular mechanism of CuD in the human pancreatic cancer cell line, Capan-1. CuD induced cell cycle arrest at the G2/M phase, apoptosis, and reactive oxygen species generation in Capan-1 cell line. In addition, CuD induced the activation of the p38 MAPK signaling pathway that regulates apoptosis, which was also inhibited by N-acetyl-L-cysteine and the p38 inhibitor SB203580. These data suggest that CuD induces cell cycle arrest and apoptosis via the ROS/p38 pathway in Capan-1 pancreatic cancer cell line; hence, CuD is a promising candidate that should be explored further for its effectiveness as an anticancer agent against pancreatic cancer.

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Garg, Sukant, He Huifu, Anjani Kumari, Durai Sundar, Sunil C. Kaul und Renu Wadhwa. „Induction of Senescence in Cancer Cells by a Novel Combination of Cucurbitacin B and Withanone: Molecular Mechanism and Therapeutic Potential“. Journals of Gerontology: Series A 75, Nr. 6 (21.05.2019): 1031–41. http://dx.doi.org/10.1093/gerona/glz077.

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Abstract Cancer, an uncontrolled proliferation syndrome, is treated with synthetic chemotherapeutic drugs that are associated with severe adverse effects. Development and application of new natural compounds is warranted to deal with the exponentially increasing incidence of cancer worldwide. Keeping selective toxicity to cancer cells as a priority criterion, we developed a combination of Cucurbitacin B and Withanone, and analyzed its anticancer potential using non-small cell lung cancer cells. We demonstrate that the selective cytotoxicity of the combination, called CucWi-N, to cancer cells is mediated by induction of cellular senescence that was characterized by decrease in Lamin A/C, CDK2, CDK4, Cyclin D, Cyclin E, phosphorylated RB, mortalin and increase in p53 and CARF proteins. It compromised cancer cell migration that was mediated by decrease in mortalin, hnRNP-K, vascular endothelial growth factor, matrix metalloproteinase 2, and fibronectin. We provide in silico, molecular dynamics and experimental data to support that CucWi-N (i) possesses high capability to target mortalin–p53 interaction and hnRNP-K proteins, (ii) triggers replicative senescence and inhibits metastatic potential of the cancer cells, and (iii) inhibits tumor progression and metastasis in vivo. We propose that CucWi-N is a potential natural anticancer drug that warrants further mechanistic and clinical studies.

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Nakanishi, Tsukasa, Yuan Song, Cuiying He, Duo Wang, Kentaro Morita, Junichi Tsukada, Tamotsu Kanazawa und Yasuhiro Yoshida. „Relationship between triterpenoid anticancer drug resistance, autophagy, and caspase-1 in adult T-cell leukemia“. PeerJ 4 (12.05.2016): e2026. http://dx.doi.org/10.7717/peerj.2026.

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We previously reported that the inflammasome inhibitor cucurbitacin D (CuD) induces apoptosis in human leukemia cell lines. Here, we investigated the effects of CuD and a B-cell lymphoma extra-large (Bcl-xL) inhibitor on autophagy in peripheral blood lymphocytes (PBL) isolated from adult T-cell leukemia (ATL) patients. CuD induced PBL cell death in patients but not in healthy donors. This effect was not significantly inhibited by treatment with rapamycin or 3-methyladenine (3-MA). The Bcl-xL inhibitor Z36 induced death in primary cells from ATL patients including that induced by CuD treatment, effects that were partly inhibited by 3-MA. Similarly, cell death induced by the steroid prednisolone was enhanced in the presence of Z36. A western blot analysis revealed that Z36 also promoted CuD-induced poly(ADP ribose) polymerase cleavage. Interestingly, the effects of CuD and Z36 were attenuated in primary ATL patient cells obtained upon recurrence after umbilical cord blood transplantation, as compared to those obtained before chemotherapy. Furthermore, cells from this patient expressed a high level of caspase-1, and treatment with caspase-1 inhibitor-enhanced CuD-induced cell death. Taken together, these results suggest that rescue from resistance to steroid drugs can enhance chemotherapy, and that caspase-1 is a good marker for drug resistance in ATL patients.

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Ku, Jin Mo, Soon Re Kim, Se Hyang Hong, Han-Seok Choi, Hye Sook Seo, Yong Cheol Shin und Seong-Gyu Ko. „Cucurbitacin D induces cell cycle arrest and apoptosis by inhibiting STAT3 and NF-κB signaling in doxorubicin-resistant human breast carcinoma (MCF7/ADR) cells“. Molecular and Cellular Biochemistry 409, Nr. 1-2 (14.07.2015): 33–43. http://dx.doi.org/10.1007/s11010-015-2509-9.

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Liu, Kan, Hongtao Xing, Siwei Zhang, Shuk ming Liu und Ming chiu Fung. „Cucurbitacin D induces fetal hemoglobin synthesis in K562 cells and human hematopoietic progenitors through activation of p38 pathway and stabilization of the γ-globin mRNA“. Blood Cells, Molecules, and Diseases 45, Nr. 4 (Dezember 2010): 269–75. http://dx.doi.org/10.1016/j.bcmd.2010.09.004.

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Hussain, Hidayat, Ivan R. Green, Muhammad Saleem, Khanzadi F. Khattak, Muhammad Irshad und Maroof Ali. „Cucurbitacins as Anticancer Agents: A Patent Review“. Recent Patents on Anti-Cancer Drug Discovery 14, Nr. 2 (02.08.2019): 133–43. http://dx.doi.org/10.2174/1574892813666181119123035.

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Background: Cucurbitacins belong to a group of tetracyclic triterpenoids that display a wide range of biological effects. In the past, numerous cucurbitacins have been isolated from natural sources and many active compounds have been synthesized using the privileged scaffold in order to enhance its cytotoxic effects. Objective: his review covers patents on the therapeutic effects of natural cucurbitacins and their synthetic analogs published during the past decade. By far, the majority of patents published are related to cancer and Structure-Activity Relationships (SAR) of these compounds are included to lend gravitas to this important class of natural products. Methods: The date about the published patents was downloaded via online open access patent databases. Results: Cucurbitacins display significant cytotoxic properties, in particular cucurbitacins B and D which possess very potent effects towards a number of cancer cells. Numerous cucurbitacins isolated from natural sources have been derivatized through chemical modification at the C(2)-OH and C(25)- OH groups. Most importantly, an acyl ester of the C(25)-OH and, iso-propyl, n-propyl and ethyl ether groups of the C(2)-OH demonstrated the most increased cytotoxic activity. Conclusion: The significant cytotoxic effects of natural and semi-synthetic cucurbitacins make them attractive as new drug candidates. Moreover, cucurbitacins have the capability to form conjugates with other anticancer drugs which will synergistically enhance their anticancer effects. The authors believe that in order to get lead compounds, there should be a greater focus on the synthesis of homodimers, heterodimers, and halo derivatives of cucurbitacins. In the opinion of the authors the analysis of the published patents on the cucurbitacins indicates that these compounds can be developed into a regimen to treat a wide spectrum of cancers.

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Mikami, Adriana Yatie, und Maurício Ursi Ventura. „Isca amilácea de cucurbitacina (Lagenaria vulgaris L.) promove maior eficiência do inseticida carbaril no controle de Diabrotica speciosa, em laboratório“. Ciência Rural 38, Nr. 8 (November 2008): 2119–23. http://dx.doi.org/10.1590/s0103-84782008000800005.

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Diabrotica speciosa (Germar, 1824) (Coleoptera: Chrysomelidae: Galerucinae) é uma importante praga polífaga na América Latina. Seu controle é realizado com inseticidas sintéticos, o que causa problemas ambientais. Desse modo, o objetivo do trabalho foi avaliar a isca amilácea de cucurbitacina (Lagenaria vulgaris L.) associada ao inseticida carbaril no controle de D. speciosa em laboratório. Foram realizados testes de múltipla escolha pareados e confinamento com insetos adultos. Os tratamentos foram: isca amilácea de cucurbitacina, isca + carbaril, apenas carbaril e a testemunha (água destilada). As soluções foram pulverizadas em plantas de milho mantidas em casa-de-vegetação. Folhas foram retiradas para realização dos ensaios em laboratório e sete avaliações (três, cinco, sete, dez, 12, 14 e 17 dias após a aplicação) foram realizadas. Foram avaliados o consumo foliar e a mortalidade. A isca de cucurbitacina exerceu efeito fagoestimulante aos adultos de D. speciosa. A adição da isca ao carbaril aumentou a eficiência do inseticida.

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Kirkegaard, Signe Skyum, Ian Henry Lambert, Steen Gammeltoft und Else Kay Hoffmann. „Activation of the TASK-2 channel after cell swelling is dependent on tyrosine phosphorylation“. American Journal of Physiology-Cell Physiology 299, Nr. 4 (Oktober 2010): C844—C853. http://dx.doi.org/10.1152/ajpcell.00024.2010.

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The swelling-activated K+ currents ( IK,vol) in Ehrlich ascites tumor cells (EATC) has been reported to be through the two-pore domain (K2p), TWIK-related acid-sensitive K+ channel 2 (TASK-2). The regulatory volume decrease (RVD), following hypotonic exposure in EATC, is rate limited by IK,vol indicating that inhibition of RVD reflects inhibition of TASK-2. We find that in EATC the tyrosine kinase inhibitor genistein inhibits RVD by 90%, and that the tyrosine phosphatase inhibitor monoperoxo(picolinato)-oxo-vanadate(V) [mpV(pic)] shifted the volume set point for inactivation of the channel to a lower cell volume. Swelling-activated K+ efflux was impaired by genistein and the Src kinase family inhibitor 4-amino-5-(4-chloro-phenyl)-7-( t-butyl)pyrazolo[3,4- d]pyrimidine (PP2) and enhanced by the tyrosine phosphatase inhibitor mpV(pic). With the use of the TASK-2 inhibitor clofilium, it is demonstrated that mpV(pic) increased the volume-sensitive part of the K+ efflux 1.3 times. To exclude K+ efflux via a KCl cotransporter, cellular Cl− was substituted with NO3−. Also under these conditions K+ efflux was completely blocked by genistein. Thus tyrosine kinases seem to be involved in the activation of the volume-sensitive K+ channel, whereas tyrosine phosphatases appears to be involved in inactivation of the channel. Overexpressing TASK-2 in human embryonic kidney (HEK)-293 cells increased the RVD rate and reduced the volume set point. TASK-2 has tyrosine sites, and precipitation of TASK-2 together with Western blotting and antibodies against phosphotyrosines revealed a cell swelling-induced, time-dependent tyrosine phosphorylation of the channel. Even though we found an inhibiting effect of PP2 on RVD, neither Src nor the focal adhesion kinase (FAK) seem to be involved. Inhibitors of the epidermal growth factor receptor tyrosine kinases had no effect on RVD, whereas the Janus kinase (JAK) inhibitor cucurbitacin inhibited the RVD by 40%. It is suggested that the cytokine receptor-coupled JAK/STAT pathway is upstream of the swelling-induced phosphorylation and activation of TASK-2 in EATC.

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Bar-Nun, Nurit, und Alfred M. Mayer. „Cucurbitacins protect cucumber tissue against infection by Botrytis cinerea“. Phytochemistry 29, Nr. 3 (1990): 787–91. http://dx.doi.org/10.1016/0031-9422(90)80019-d.

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Jung, Michael E., und Rebecca M. Lui. „Studies toward the Total Syntheses of Cucurbitacins B and D“. Journal of Organic Chemistry 75, Nr. 21 (05.11.2010): 7146–58. http://dx.doi.org/10.1021/jo101242e.

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Chatzisideri, Theodora, Panagiotis Dalezis, George Leonidis, Spyridon Bousis, Dimitrios Trafalis, Francesca Bianchini und Vasiliki Sarli. „Synthesis and biological studies of c(RGDyK) conjugates of cucurbitacins“. Future Medicinal Chemistry 13, Nr. 10 (Mai 2021): 877–95. http://dx.doi.org/10.4155/fmc-2020-0309.

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Cucurbitacins (CUCUs) are triterpenoids known to display potent cytotoxic effects; however, their clinical application is limited due to poor pharmacokinetics and systemic toxicity. This work focuses on the development of c(RGDyK)–CUCU conjugates for the selective delivery of CUCUs to integrin-overexpressing cancer cells. The activity of the conjugates against various cancer cells was studied. They exhibited a mild cytostatic effect to six cancer cell lines and a cytotoxic effect against integrin-overexpressing MCF-7 and A549 cells. Their chemical and metabolic stability was extensively studied using LC–MS analysis. The conjugates maintained high affinity for αvβ3 integrin receptors. c(RGDyK) conjugation via a PEG linker was beneficial for CUCU-D and the resulting conjugate was approximately three-times more active than the free CUCU-D in MCF7 cells.

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Andersen, J. F., R. D. Plattner und D. Weisleder. „Metabolic transformations of cucurbitacins by Diabrotica virgifera virgifera leconte and D. undecimpunctata howardi Barber“. Insect Biochemistry 18, Nr. 1 (Januar 1988): 71–77. http://dx.doi.org/10.1016/0020-1790(88)90038-8.

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Polanczyk, R. A., E. D. Grecco, G. S. Andrade, F. N. Celestino, W. F. Barbosa, C. R. Franco und D. Pratissoli. „DESEMPENHO DE TRICHOGRAMMA SPP. (HYMENOPTERA: TRICHOGRAMMATIDAE) EM OVOS DE DIAPHANIA HYALINATA (L.) (LEPIDOPTERA: PYRALIDAE) TRATADOS COM METARHIZIUM ANISOPLIAE E BEAUVERIA BASSIANA“. Arquivos do Instituto Biológico 76, Nr. 3 (September 2009): 495–99. http://dx.doi.org/10.1590/1808-1657v76p4952009.

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RESUMO Diaphania hyalinata (L., 1758) é uma das principais pragas de Cucurbitacea e ênfase tem sido dada ao controle biológico desta praga em substituição ao controle químico. A compatibilidade de agentes de controle biológico foi avaliada pelo desempenho de fêmeas de Trichogramma atopovirilia Oatman & Platner, 1983 e Trichogramma pretiosum Riley, 1879 em ovos de D. hyalinata pulverizados com os fungos entomopatogênicos Metarhizium anisopliae (Metsh.) Sorok, 1883 e Beauveria bassiana (Balls.) Vuill. Vinte ovos de D. hyalinata foram imersos em suspensão de Metarril®, Boveril® e água destilada (testemunha) e oferecidos diariamente para o parasitismo por 24h até a morte dos parasitoides. Foram avaliados o parasitismo diário, acumulado e total, número de ovos parasitados, viabilidade, razão sexual e longevidade. Os fungos entomopatogênicos M. anisopliae e B. bassiana não afetaram as características reprodutivas e de sobrevivência das duas espécies do gênero Trichogramma, sendo que T. pretiosum apresentou maior parasitismo que T. atopovirilia em ovos de D. hyalinata. Os resultados obtidos neste trabalho mostram que é possível a integração de T. atopovirilia e os fungos entomopatogênicos M. anisopliae e B. bassiana em programas de manejo integrado de pragas de cucurbitáceas.

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HIMENO, Eiji, Tsuneatsu NAGAO, Junko HONDA, Hikaru OKABE, Nobuto IRINO und Tetsuo NAKASUMI. „Structures of cayaponosides A, B, C and D, glucosides of new nor-cucurbitacins in the roots of Cayaponia tayuya.“ CHEMICAL & PHARMACEUTICAL BULLETIN 40, Nr. 10 (1992): 2885–87. http://dx.doi.org/10.1248/cpb.40.2885.

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Isabirye, B. E., A. M. Akol, A. Mayamba, C. K. Nankinga und I. Rwomushana. „Species composition and community structure of fruit flies (Diptera: Tephritidae) across major mango-growing regions in Uganda“. International Journal of Tropical Insect Science 35, Nr. 02 (23.04.2015): 69–79. http://dx.doi.org/10.1017/s1742758415000089.

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The species diversity of tephritid fruit flies in major mango-growing regions in Uganda was monitored over a 2-year period (2010–2012) using fruit bait and lure traps. A total of 368,332 specimens belonging to 10 species in four genera (Bactrocera,Ceratitis,TrirhithrumandDacus) were collected. Of these, 98.9% belonged toBactrocera invadens, while the second and third most common species wereDacus bivittatus(0.4%) andCeratitis anonae(0.3%), respectively. Significant differences in the evenness and diversity of fruit fly species were noted across the regions. Fruit fly community structure was significantly different across the three regions. The Lake Victoria Crescent and Mbale Farmlands harboured significantly moreD. ciliatus,T. coffeae,D. bivittatusandB. cucurbitaein contrast to the Northern Moist Farmlands and the Western Medium High Farmlands.Ceratitis rosacontributed the highest difference in regional structure, followed byC. fasciventrisandC. cosyra. Rank abundance curves depicted a geometric series distribution of the species composition in the three regions, confirming a scenario of competitive displacement of native fruit fly species byB. invadens. A comprehensive and sustainable response strategy toB. invadensand other fruit flies needs to be urgently devised to protect the horticulture industry in Uganda.

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