In-vitro and in-vivo antitumour activity of physalins B and D fromPhysalis angulata

Abstract

We have evaluated the in-vitro and in-vivo antitumour activity of physalin B and physalin D isolated from the aerial parts of Physalis angulata. In-vitro, both compounds displayed considerable cytotoxicity against several cancer cell lines, showing IC50 values in the range of 0.58 to 15.18 microg mL(-1) for physalin B, and 0.28 to 2.43 microg mL(-1) for physalin D. The antitumour activity of both compounds was confirmed in-vivo using mice bearing sarcoma 180 tumour cells. The in-vivo antitumour activity was related to the inhibition of tumour proliferation, as observed by the reduction of Ki67 staining in tumours of treated animals. Histopathological examination of the kidney and liver showed that both organs were affected by physalin treatment, but in a reversible manner. These compounds were probably responsible for the previously described antitumour activity of ethanol extracts of P. angulata, and their identification and characterization presented here could explain the ethnopharmacological use of this species in the treatment of cancer.

Withanolides and Related Steroids

“…Among the physalins, physalins B (463), D (313), F (450), and H (312) showed strong cytotoxicity against multiple tumor cell lines, while physalins G (314), I (510), and physanolide A (367) were inactive. Physalins J (457) and U (304) were marginally active (55,134,146,244,245). The 18-nor-physalin, withaphysanolide A (438), also was weakly active (186).…”

“…The 18-nor-physalin, withaphysanolide A (438), also was weakly active (186). For physalins B and D, the antineoplastic activity was confirmed in vivo by inhibition of tumor proliferation in mice bearing sarcoma 180 tumor cells (245). Both physalins B and F have been shown to inhibit hedgehog (Hh)/GLI-mediated transcriptional activation, which is involved directly in tumor formation and progression (246).…”

Effects of seco-steroids purified from Physalis angulata L., Solanaceae, on the viability of Leishmania sp

“…Magalhães (2006) also showed that both physalins B and D have antitumoral activity, although Chiang (1992) reported lack of activity of physalin D in human leukemia cells in vitro.…”

Plants from Solanaceae family with possible anxiolytic effect reported on 19th century's Brazilian medical journal

“…Phytochemical: seco-steroids (physalins) (Soares et al, 2006;Abe et al, 2006;Kuo et al, 2006;Magalhães et al, 2006a;Magalhães et al, 2006b;Damu et al, 2007), alkaloids (Edeoga et al, 2005), tannins and flavonoids (Edeoga et al, 2005;Wollenweber et al, 2005), the withanolides withangulatin (Lee et al, 2008) and physagulins . Patents that were reported, both in the European Patent Office and the Brazilian National Institute of industrial Property databases, most of which concern inflammatory, allergic, parasitic, infectious or digestive diseases, including extracts from P. angulata (Balbani et al, 2009 (Zakaria et al, 2006); can cause a central nervous system depression which may be correlated with an increased parasympathetic tone (Perez et al, 1998), antioxidant (Al-Fatimi et al, 2007); antipyretic and anticancer agent (Hsieh et al, 2008;Hsu et al, 2009;Yang et al, 2010;Li et al, 2008;Li et al, 2009), mutagenic activity (Almeida et al, 2010).…”