期刊
REVISTA BRASILEIRA DE FARMACOGNOSIA-BRAZILIAN JOURNAL OF PHARMACOGNOSY
卷 30, 期 5, 页码 723-728出版社
SPRINGERNATURE
DOI: 10.1007/s43450-020-00102-9
关键词
Isowithametelin; Cytotoxicity; TNF-alpha; Protein kinase inhibition; NF-kappa B; NOproduction; Solanaceae
资金
- Higher Education Commission, Pakistan
Datura innoxia Mill., Solanaceae, an underexplored ethnomedicinal plant, has been empirically evaluated in the current study for the isolation of bioactive agents. A crude extract of D. innoxia leaves was subjected to normal-phase medium pressure and vacuum liquid chromatography which led to the purification of a withanolide, isowithametelin. The chemical structure was established based on single-crystal X-ray diffraction. Isowithametelin exhibited substantial cytotoxicity against tested human cancer cell lines (breast cancer MCF-7 (ATCC (R) HTB-22), lung carcinoma LU-1 (human lung carcinoma established in the Department of Surgical Oncology, University of Illinois at Chicago), and prostate adenocarcinoma PC-3 (ATCC (R) CRL-1435)) with IC50 values of 4.3 +/- 0.93, 6.9 +/- 1.3, and 0.01 +/- 0.001 mu g/ml, respectively. It also inhibited nitric oxide production in lipopolysaccharide-activated murine macrophage RAW264.7 cells (IC50 value of 18.5 +/- 1.8 mu g/ml) and demonstrated moderate protein kinase inhibition. This work suggests a possible anticancer role of isowithametelin; in vivo studies remain necessary to corroborate in vitro efficacy.
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