Evaluation of CYP2D, CYP1A2 and distribution of tetrandrine, fangchinoline in the brain, liver, and kidney of wistar rats after short-term exposure to Cyclea peltata

Anuja, G. I.; Latha, P. G.; Suja, S. R.; Abraham, Swapna Susan; Nair, Vinodkumar T G.; Rajasekharan, S.

doi:10.4103/pm.pm_166_20

Cited by 1 publication

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“…2 The plant is also traditionally used by tribal communities in India to treat diarrhea, wounds, and certain skin diseases. 4−6 The plant is known to possess many pharmacological properties, including antidiabetic, anticancer potential at an extract level, 7,8 nephroprotective activity, 9 hepatoprotective potential, 10 antibacterial activity, 11,12 gastric antisecretory, and antiulcer property. 13 Additionally, C. peltata root extract is effective in neutralizing the venom of Naja naja 14 and also shows significant antipyretic and analgesic activity, 15 and the ethyl acetate extract is shown to have anti-inflammatory potential.…”

Section: ■ Introductionmentioning

confidence: 99%

Exploration of Phaeanthine: A Bisbenzylisoquinoline Alkaloid Induces Anticancer Effect in Cervical Cancer Cells Involving Mitochondria-Mediated Apoptosis

et al. 2023

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Natural-product-based pharmacophores possess considerably more structural diversity, attractive physicochemical features, and relatively less toxicity than synthesized drug entities. In this context, our studies on phaeanthine, a bisbenzylisoquinoline alkaloid isolated from the rhizomes of Cyclea peltata (Lam) Hook.f & Thoms., showed selective cytotoxicity toward cervical cancer cells (HeLa) with an IC50 of 8.11 ± 0.04 μM. Subsequent investigation with in silico molecular docking of phaeanthine displayed preferential binding to the antiapoptotic protein Akt as reflected by a docking score of −5.023. Interestingly, the follow-up in vitro assessment of the compound correlated with mitochondria-mediated apoptosis specifically by downregulating the expression of Akt and p-Akt, including other antiapoptotic proteins MCl-1, IGF-2, and XIAP. In the complementary in vitro assessment, mitochondrial membrane polarization and dynamics of intercellular cytochrome c validated the intrinsic mechanism of the apoptotic phenomenon. To the best of our knowledge, this is the first comprehensive anticancer profiling study of phaeanthine against HeLa cells.

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