Exploration of anticancer potential of Lantadenes from weed Lantana camara: Synthesis, in silico, in vitro and in vivo studies

被引:2
作者
Chauhan, Monika [1 ,6 ]
Dhar, Zahid Ahmad [1 ]
Gorki, Varun [2 ]
Sharma, Sonia [3 ]
Koul, Ashwani [4 ]
Bala, Shashi [4 ]
Kaur, Ramandeep [3 ]
Kaur, Sukhbir [2 ]
Sharma, Manu [5 ]
Dhingra, Neelima [1 ,7 ]
机构
[1] Panjab Univ, Univ Inst Pharmaceut Sci, Chandigarh 160014, India
[2] Panjab Univ, Dept Zool, Parasitol Lab, Chandigarh 160014, India
[3] Punjab Univ, Dept Cum Natl Ctr Human Genome Studies & Res, Chandigarh 160014, India
[4] Panjab Univ, Dept Biophys, Chandigarh 160014, India
[5] Natl Forens Sci Univ, Delhi Campus, Delhi, India
[6] Univ Petr & Energy Studies, Sch Hlth Sci & Technol, Dehra Dun 248007, Uttarakhand, India
[7] Panjab Univ, Dept Pharmaceut Chem, Univ Inst Pharmaceut Sci, Chandigarh 160014, India
关键词
Lantana camara; Verbenaceae; Lantadenes; Weed; Natural products; Drug development; Cytotoxicity; Molecular docking; Anticancer; NF-KAPPA-B; LUNG ADENOCARCINOMA; DRUG-METABOLISM; HIGH-THROUGHPUT; CANCER; PREDICTION; CYTOTOXICITY; INHIBITION; DISCOVERY; DESIGN;
D O I
10.1016/j.phytochem.2022.113525
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Naturally occurring pentacyclic triterpenoids and their semisynthetic analogues have engrossed increasing attention for their anticancer potential and exhibiting promising role in discovery of new anticancer agents. Present study include the semi synthetic modifications of Lantadenes from the weed Lantana carama and their structures delineation by FT-IR, 1H-NMR, 13C-NMR & mass spectroscopy. All the compounds were scrutinized for in vitro cytotoxicity, ligand receptor interaction and in vivo anticancer studies. Most of the novel analogues displayed potent antiproliferative activity against A375 & A431 cancer cell lines and found superior to parent Lantadenes. In particular, 3 beta-(4-Methoxybenzoyloxy)-22 beta-senecioyloxy-olean-12-en-28-oic acid was found to be most suitable compound, with IC50 value of 3.027 mu M aganist A375 cell line having least docking score (-69.40 kcal/mol). Promising anticancer potential of the lead was further indicated by significant reduction in tumor volume and burden in two stage carcinoma model. These findings suggests that the Lantadene derivatives may hold promising potential for the intervention of skin cancers.
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页数:12
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