Synthesis of madecassic acid derivatives and their cytotoxic activity

2018 ◽  
Vol 73 (2) ◽  
pp. 91-98 ◽  
Author(s):  
Tran Van Loc ◽  
Vo Thi Quynh Nhu ◽  
Tran Van Chien ◽  
Le Thi Thu Ha ◽  
Tran Thi Phuong Thao ◽  
...  

AbstractFifteen new 28-amide derivatives of madecassic acid, isolated from the tropical medicinal herb Centella asiatica (Apiaceae), have been synthesised, and their cytotoxicity on three cancer cell lines, KB (carcinoma cancer), HepG2 (liver cancer) and Lu-1 (lung cancer), was evaluated. The results showed that acetylation of the 2,3,23-hydroxyl group and/or amidation of the 28-COOH group strongly increased the cytotoxicity of the synthesised compounds.


1992 ◽  
Vol 35 (26) ◽  
pp. 4854-4857 ◽  
Author(s):  
John C. Ruckdeschel ◽  
Sandeep P. Modi ◽  
Wageeh El-Hamouly ◽  
Enrico Portuese ◽  
Sydney Archer


2012 ◽  
Vol 227 (10) ◽  
pp. 3389-3396 ◽  
Author(s):  
Anna Tesei ◽  
Giovanni Brigliadori ◽  
Silvia Carloni ◽  
Francesco Fabbri ◽  
Paola Ulivi ◽  
...  


2018 ◽  
Vol 54 (2C) ◽  
pp. 502
Author(s):  
Le Duc Anh

Two new conjugates of murrayafoline A with zerumbone and artemisinin 3, 11 wereprepared by N-alkylation, in which, compound 3 was synthesized from two consecutive Nalkylationreactions. Their cytotoxicity was evaluated on four human cancer cell lines Hep-G2,LU, RD and Fl. The result showed that both compounds exhibited no activity against the testedcell lines.



Author(s):  
Habeela Jainab N ◽  
Mohan Maruga Raja Mk

 Objective: Cancer is a molecularly heterogeneous diseaseand the leading cause of death worldwide. The methanol extract of Clerodendrum phlomidis leaf has been reported for cytotoxicity. Hence, the current investigation was planned to evaluate the cytotoxic activity of the chemical constituents isolated from the methanol extract of the C. phlomidis leaf against the Michigan cancer foundation-7 (MCF-7) breast cancer and adenocarcinomic human alveolar basal epithelial cells (A549) lung cancer cell lines by the apoptotic study.Methods: Cytotoxic activity of the chemical constituents of the methanol extract of the C. phlomidis leaf was evaluated by the 3-(4,5-dimethylthiazol- 2-yl)-5-diphenyltetrazolium bromide (MTT) assay against breast cancer (MCF-7) and lung cancer (A549) cell lines. The MCF-7 and A549 cell lines were tested at different concentrations to determine 50% of growth inhibition (inhibitory concentration [IC50]) by MTT assay. Apoptosis of nuclei was detected by 4’,6-diamidino-2-phenylindole staining assay.Results: In MCF-7 breast cancer cell line study, Compounds 6 and 9 exhibited good cytotoxic activity with an IC50 value of 83.80 and 75.16 μg/ml, respectively. In A549 lung cancer cell line, again Compounds 6 and 9 exhibited good cytotoxic activity with an IC50 value of 84.46 and 78.60 μg/ml, respectively. Percentage of apoptosis induced by the Compounds 6 and 9 in the MCF-7 cancer cells was found to be 74.50 and 85.48, respectively.Conclusion: The results of the current study prove that the Compounds 6 and 9 are potential agents for breast and lung cancer. In future research, these potential agents can further be evaluated by animal studies and their mechanism of action apart from the induction of apoptosis of the cancer cells can be determined.



Marine Drugs ◽  
2020 ◽  
Vol 18 (8) ◽  
pp. 418 ◽  
Author(s):  
Supakarn Chamni ◽  
Natchanun Sirimangkalakitti ◽  
Pithi Chanvorachote ◽  
Khanit Suwanborirux ◽  
Naoki Saito

Two new series of synthetic renieramycins including 22-O-amino ester and hydroquinone 5-O-amino ester derivatives of renieramycin M were semi-synthesized and evaluated for their cytotoxicity against the metastatic non-small-cell lung cancer H292 and H460 cell lines. Interestingly, the series of 22-O-amino ester derivatives displayed a potent cytotoxic activity greater than the hydroquinone derivatives. The most cytotoxic derivative of the series was the 22-O-(N-Boc-l-glycine) ester of renieramycin M (5a: IC50 3.56 nM), which showed 7-fold higher potency than renieramycin M (IC50 24.56 nM) and 61-fold more than jorunnamycin A (IC50 217.43 nM) against H292 cells. In addition, 5a exhibited a significantly higher cytotoxic activity than doxorubicin (ca. 100 times). The new semi-synthetic renieramycin derivatives will be further studied and developed as potential cytotoxic agents for non-small-cell lung cancer treatment.







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