In vitro and in vivo anticancer activity of 2-deacetoxytaxinine J and synthesis of novel taxoids and their in vitro anticancer activity☆

Isolation and cytotoxicity evaluation of taxanes from the barks of Taxus wallichiana var. mairei

“…Compared to 4-6 and 16, the introduction of an O-b-xylose in R 2 (7)(8)(9)(10)(11) or loss of the C-13 ester side chain (14-15) greatly decrease their activities, which is consistent with the reported SAR of taxol analogues. 27 Interestingly, despite of the general low activity, the O-b-xylose bearing compounds 7-11 reserved their anti-proliferative activity and showed selective cytotoxicity towards certain cancer cell lines.…”

“…Thus, there is continuously demanding of new information facilitating the novel taxane-based drug design and discovery. However, previous pharmaceutical study on taxanes mainly focused on the modification of the taxol prototype with a 6/8/6-ring system, [2][3][4][5][6][7] and systematically evaluation of the anticancer properties of taxanes with different sub-types remains scarce.…”

Review on ethnomedicinal, phytochemical and pharmacological evidence of Himalayan anticancer plants

“…2-deacetoxytaxinine J (2-DAT-J) (13) (Fig. 7) isolated from Taxus wallichiana bark given orally to Virgin female Sprague Dawley rats at a concentration of 10 mg/ml/kg for 30 days inhibited 60% DMBA induced mammary tumors (Reddy et al, 2009). …”

“…Compound isolated from the stem bark of Taxus wallichiana have significant in-vitro activity against MCF-7 and MDA-MB-231 cell lines. Anticancer secondary metabolites may be diterpneoid 2-deacetoxytaxinine J (Reddy et al, 2009). Lignans mixture EVn-50 extracted from seeds of Vitex negundo is composed of 70% lignans, of which VB1 and VB2 are the most abundant lignans.…”

Anticancer Potential of Some Ayurvedic Plants of North Eastern India: A Comprehensive Pharmacological Review

“…2-DAT-J showed significant in-vitro activity against breast cancer cell line at a concentration of 20µM and 10µM in MCF-7 and MDA-MB-231, respectively. 2-DAT-J was also tested for its in-vivo activity on DMBA-induced mammary tumors in virgin female Sprague Dawley rats at a dose of 10mg/kg body weight orally for 30 days and showed significant regression in mammary tumors as compared to vehicle treated group 18 .…”