Cucurbitacins-type triterpene with potent activity on mouse embryonic fibroblast from Cucumis prophetarum, cucurbitaceae

Ayyad, Seif Eldin N; Abdel‐Lateff, Ahmed; Basaif, Salem A.; Shier, Thomas W.

doi:10.4103/0974-8490.85006

Cited by 20 publications

(14 citation statements)

References 12 publications

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“…as described in Supplementary Table S1. The structure of CuB was elucidated on the basis of spectroscopic analysis described in Supplementary Table S1, which was in good agreement with that of previously reported (20).…”

Section: Isolation Of Cubsupporting

confidence: 76%

Cucurbitacin B Alters the Expression of Tumor-Related Genes by Epigenetic Modifications in NSCLC and Inhibits NNK-Induced Lung Tumorigenesis

Shukla

Khan

Kumar

et al. 2015

Cancer Prevention Research

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Non-small cell lung cancer (NSCLC) represents almost 85% of total diagnosed lung cancer. Studies have shown that combination of DNA methyltransferase (DNMT) and histone deacetylase (HDAC) inhibitors is effective against various cancers, including lung cancer. However, optimizing the synergistic dose regime is very difficult and involves adverse side effects. Therefore, in this study, we have shown that cucurbitacin B (CuB), a single bioactive triterpenoid compound, inhibits both DNMTs and HDACs starting at a very low dose of 60 nmol/L in NSCLC H1299 cells. The CuB-mediated inhibition of DNMTs and HDACs in H1299 cells leads to the reactivation of key tumor suppressor genes (TSG) such as CDKN1A and CDKN2A, as well as downregulation of oncogenes c-MYC and K-RAS and key tumor promoter gene (TPG), human telomerase reverse transcriptase (hTERT). The upregulation of TSGs and downregulation of TPG were consistently correlated with the alterations in their promoter methylation and histone modifications. This altered expression of TPG and TSGs is, at least in part, responsible for the inhibition of cellular proliferation and induction of cellular apoptosis in NSCLC. Furthermore, CuB treatment significantly inhibited the tumor incidence and multiplicity in 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK)-induced lung tumorigenesis in A/J mice, which was associated with the induction of apoptosis and inhibition of hyperproliferation in the lung tissues. Together, our study provides new insight into the CuB-mediated epigenetic alterations and its chemotherapeutic effects on lung cancer. Cancer Prev Res; 8(6); 552-62. Ó2015 AACR.

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Section: Isolation Of Cubsupporting

confidence: 76%

Cucurbitacin B Alters the Expression of Tumor-Related Genes by Epigenetic Modifications in NSCLC and Inhibits NNK-Induced Lung Tumorigenesis

Shukla

Khan

Kumar

et al. 2015

Cancer Prevention Research

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“…Interaction of protein and ligand were shown in Figures 6 – 8 . Some previous study suggested that anti-tumor activity of Bacopa due to bacosides,[ 9 22 ] cucurbitacins,[ 23 24 ] and also betulinic acid. [ 25 ] This docking study presented probable mechanism of action of anti-tumor activity of DBM.…”

Section: Resultsmentioning

confidence: 99%

Exploring the cytotoxic potential of triterpenoids-enriched fraction of Bacopa monnieri by implementing In vitro, In vivo, and In silico approaches

Mallick¹,

Khan²,

Parveen³

et al. 2017

Phcog Mag

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Background:Bacopa monnieri (BM) is a herbaceous plant traditionally used from time immemorial in Ayurvedic and folklore medicines. We hypothesized that the extract of the whole plant might contain numerous molecules with having antitumor activities that could be very effective in killing of human cancer cells.Objectives:This work investigated anticancer activity of bioactive fraction of BM.Materials and Methods:The hydroalcoholic extract of BM was fractionated with different solvent, namely, hexane, dichloromethane (DCM), acetone, methanol, and water. The in vitro anticancer activity was performed against various Human Cancer Cell lines, namely, Colon (HT29, Colo320, and Caco2), Lung (A549), Cervix (HeLa, SiHa), and Breast (MCF-7, MDAMB-231). Further, DCM fraction was evaluated in vivo for anticancer activity against Ehrlich ascites carcinoma (EAC) tumor-bearing mice since it showed the best cytotoxicity at 72 h (IC50 41.0–60.0 µg/mL). The metabolic fingerprinting of these extract were carried out using high-performance thin-layer chromatography along with quantification of bacoside A, bacoside B, cucurbitacin B, cucurbitacin E, and bittulinic acid.Results:Oral administration of DCM fraction at a dose of 40 mg/kg rendered prominent reduction of tumor regression parameters such as tumor weight, packed cell volume, tumor volume and viable tumor cell count as compared to the untreated mice of the EAC control group. The anticancer activity of DCM fraction may be due to the presence of large amount of bacoside A, B and cucurbitacins. The molecular docking studies of major metabolites with targeted proteins predicted the anticancer activity of DCM fraction which was in support of in vivo activity.Conclusion:The in vitro, in vivo, analytical and in silico studies on DCM fraction of Bacopa monieri has proved its great potential for development of anticancer phytopharmaceuticals.SUMMARY A new HPTLC method has been developed and validated for the qualitative and quantitative analysis of bacoside A, B, cucurbitacin B, D, E and bittulinic acid in Bacopa monnieri extract. Enrichment of active anticancer metabolites was done by polarity based fractionations of hydroalcoholic extract of Bacopa. DCM fraction of a hydroalcoholic extract of Bacopa showed anticancer potential against human cancer cell line (IC50 41.0-60.0 µg/mL) and in EAC treated mice (at a dose of 40 mg/kg body weight). The anticancer activity of Bacopa may be due to the presence of bacosides and cucurbitacin and it was confirmed by in silico screening. Abbreviations used: DBM: DCM fraction of Bacopa monnieri; DCM: Dichloromethane; EAC: Ehrlich ascites carcinoma; HCT: Hematocrit; HGB: Hemoglobin; HPTLC: High performance thin layer chromatography; ICH: International council for Harmonisation; LOD: Limit of detection; LOQ: Limit of quantification; LYM: Lymphocytes; MCH: Mean corpuscular hemoglobin; MCHC: Mean corpuscular haemoglobin concentration (MCHC); MCV: Mean corpuscular volume; MTT: 3-(4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide; PLT: Platelet;...

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“…Compound-2 (25.5 mg) was isolated from fraction 78. It was a light-orange solid (Figure 12 Comparing the spectral data of compound-2 with reported data of cucurbitacin B indicated that compound-2 was identified as one of the cucurbitacin group, the cucurbitacin B [28]. Recently, these compounds were exploited for their differential cytotoxicity toward renal, brain tumor, inhibition of cell adhesion [28].…”

Section: Compound-2mentioning

confidence: 97%

“…Cucurbitacin B is most widely used for in-vitro studies on tumor inhibition [28]. (13) were also reported from the fruits of Cucumis melo [32].…”

Section: Biological Activitiesmentioning

confidence: 99%

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Isolation, Characterization, Structural Elucidation and Anti-Bacterial Activities of Roots Extracts of Cucumis Ficifolius

Nigussie

Ashenef

2020

Preprint

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Cucumis ficifolius (family Cucurbitaceae) is traditionally used for the treatment of diarrhea, teeth-ach, wound, burns, bleeding from external cuts and against different infectious diseases. With the absence of previous scientific report on the roots of the plant, this study was focused on isolation of chemical constituents and evaluation of their anti-bacterial activities of the roots of C. ficifolius. The n-hexane, ethyl acetate and methanol extracts of the roots of C. ficifolius were investigated for their phytochemical constituents and the results revealed that C. ficifolius is rich in many secondary metabolites such as saponins, terpenoids, glycosides, and steroids. But tannins and alkaloids were not observed. The ethyl acetate extract was subjected to column chromatography over silica gel and furnished three compounds namely compound-1, compound- 2 and compound-3. The structures of these compounds were characterized using FTIR, 1H-NMR, 13C-NMR and DEPT-135. The crude extracts and the isolated compounds were tested against four bacteria strains (Gram negative, E. coli and p. aeruginosa; Gram positive, S. aureus and B. subtilis) using Agar well diffusion method, the results showed that the methanol extracts and compound-2 were active against all the tested bacteria. Accordingly, 12.34, 18.25 and 23.75 mm zone of inhibition against B. subtilis were found at the concentration of 20, 30 and 40 μg/mL MeOH extract respectively. Similarly 9.5, 13.25 and 17.25 mm zone of inhibition were found for the same bacteria strains and concentrations of compound-2. These results showed the increase of inhibition zone with concentration. However, the n-hexane crude extract was found not to have anti-bacterial activity towards the tested bacteria strains.

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Cucurbitacins-type triterpene with potent activity on mouse embryonic fibroblast from Cucumis prophetarum, cucurbitaceae

Cited by 20 publications

References 12 publications

Cucurbitacin B Alters the Expression of Tumor-Related Genes by Epigenetic Modifications in NSCLC and Inhibits NNK-Induced Lung Tumorigenesis

Cucurbitacin B Alters the Expression of Tumor-Related Genes by Epigenetic Modifications in NSCLC and Inhibits NNK-Induced Lung Tumorigenesis

Exploring the cytotoxic potential of triterpenoids-enriched fraction of Bacopa monnieri by implementing In vitro, In vivo, and In silico approaches

Isolation, Characterization, Structural Elucidation and Anti-Bacterial Activities of Roots Extracts of Cucumis Ficifolius

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