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Background: Pinnatane A from the bark of Walsura pinnata was investigated for its anti-cancer properties by analyzing the cytotoxic activities and cell cycle arrest mechanism induced in two different liver cancer cell lines. Methods: A 3-(4,5-Dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay was used to analyze the pinnatane A selectivity in inducing cell death in cancer and normal cells. Various biological assays were carried out to analyze the anti-cancer properties of pinnatane A, such as a live/dead assay for cell death microscopic visualization, cell cycle analysis using propidium iodide (PI) to identify the cell cycle arrest phase, annexin V-fluorescein isothiocyanate (annexin V-FITC)/PI flow cytometry assay to measure percentage of cell populations at different stages of apoptosis and necrosis, and DNA fragmentation assay to verify the late stage of apoptosis. Results: The MTT assay identified pinnatane A prominent dose- and time-dependent cytotoxicity effects in Hep3B and HepG2 cells, with minimal effect on normal cells. The live/dead assay showed significant cell death, while cell cycle analysis showed arrest at the G0/G1 phase in both cell lines. Annexin V-FITC/PI flow cytometry and DNA fragmentation assays identified apoptotic cell death in Hep3B and necrotic cell death in HepG2 cell lines. Conclusions: Pinnatane A has the potential for further development as a chemotherapeutic agent prominently against human liver cells.

Background Cestrum diurnum L. (Solanaceae), locally known as buno-Hasnahena, is widely used in different traditional medicinal practices to treat pain, burn, swelling and related disorders. Adequate evidence is not available to support its medicinal properties for further use and drug development. Present study was designed to evaluate its traditional use in pain and inflammation with further characterisation of its chemical constituents through liquid chromatography-mass spectroscopic (LC-MS) analysis. Methods Antinociceptive and analgesic potential of methanol extract of the aerial parts of C. diurnum was carried out using carrageenan induced paw oedema and formalin induced paw licking test in mice at the oral doses of 150 and 300 mg/kg body weight. Inhibition of the inflammatory mediator nuclear factor kappa B (NF-κB) was evaluated by tumour necrosis factor α (TNF-α) induced NF-κB activation assay in macrophage cells at the concentration of 100 μg/ml. LC-MS analysis of the extract was performed to characterise the active component responsible for bioactivities. Results The extract significantly inhibited (p < 0.05) carrageenan induced paw oedema at both doses tested and the effect persisted throughout the entire experimental period of 3 h with the highest activity (50% inhibition) observed at 3rd h. Further, the extract significantly inhibited (p < 0.05) formalin induced paw licking both in the early and late phase at the aforementioned dose levels. The extract also downregulated the expression of NF-κB p65 protein in the TNF-α induced NF-κB activation assay. LC-MS analysis of the extract indicated the presence of some important secondary metabolites including nicotine, nornicotine, ursolic acid, vitamin D3 and its derivatives. Conclusions The results of this study supported the folkloric uses of the plant in pain and inflammations. The insights and observations suggest the action might involve downregulation of NF-κB p65 protein expression and/or inhibition of autacoids (histamine, serotonin, prostaglandin).

A phytochemical study on the bark of Walsura pinnata has led to the isolation of a new oleanane triterpene acid, 3-oxo-olean-9(11),12-dien-28-oic acid (1), together with nine known compounds (2–10). Their structures were established on the basis of the detailed spectroscopic analysis, including one- and two-dimensional NMR, ESI-MS and HR-ESI-MS techniques. Compounds 2, 3, 5, 6 and 8 were isolated from W. pinnata for the first time. Compounds 3 and 4 showed in vitro growth inhibitory activity against two human cancer cell lines MCF-7 and SK-OV-3 with IC50 values within the range of 8.85 - 18.28 μg/mL. To the best of our knowledge, this is the first report on the cytotoxic activity of compound 3 towards both cancer cell lines.

Background Cestrum diurnum L. (Solanaceae) is used in various traditional medicine for pain and related disorders. The Malayali tribe of Tamil Nadu in India use the leaf in joint pain. In the Chinese traditional medicine it is used for the treatment of burns and swellings. Present study was designed to evaluate its traditional use in pain and inflammation. Methods Methanol extract of the aerial parts of C. diurnum was tested by carrageenan induced paw oedema and formalin induced paw licking test in mice at the oral doses of 150 and 300 mg/kg body weight. NF-κB inhibitory activity was evaluated by TNF-α induced NF-κB activation assay in RAW 264.7 macrophage cells at the concentration of 100 µg/ml. Results The extract, at the doses of 150 and 300 mg/kg, showed significant inhibition (p < 0.05) of carrageenan induced paw oedema and the effect persisted throughout the entire experimental period of 3 h with the highest activity (50% inhibition) at 3rd h. In formalin induced paw licking test, the extract exhibited significant (p < 0.05) inhibition of paw licking, both in the early and late phase of the experiment at the aforementioned dose levels. At the concentration of 100 µg/ml, the extract did not inhibit the nuclear translocation of NF-κB. Rather, the extract was found to downregulate NF-κB p65 protein expression. Conclusions The present work supports the folkloric use of the plant for its analgesic and anti-inflammatory action which might involve downregulation of NF-κB p65 protein expression and/or inhibition of autacoid (histamine, serotonin, prostaglandin) synthesis.