Verbascoside

Verbascoside is isolated from Acanthus mollis, acts as an ATP-competitive inhibitor of PKC, with an IC₅₀ of 25 µM, and has antitumor, anti-inflammatory and antineuropathic pain activity. IC50 & Target:IC50: 25 µM (PKC)^[1] In Vitro: Verbascoside acts as an ATP-competitive inhibitor of PKC, with an IC₅₀ of 25 µM. Verbascoside shows K_is of 22 and 28 µM with respect to ATP and histone, respectively. Verbascoside has potent antitumor activity against L-1210 cells, with an IC₅₀ of 13 µM^[1]. Verbascoside (5, 10 µM) suppresses 2,4-dinitrochlorobenzene (DNCB)-induced T cell costimulatory factors CD86 and CD54, proinflammatory cytokines, and NFκB pathway activation in THP-1 cells^[2]. In Vivo: Verbascoside (1%) reduces the overall scratching behavior incidence as well as the severity of the skin lesions in 2,4-dinitrochlorobenzene (DNCB)-induced atopic dermatitis (AD) mice model. Verbascoside also blocks DNCB-induced expression of proinflammatory cytokine TNF-α, IL-6, and IL-4 mRNA in skin lesions^[2]. Verbascoside (50, 100 mg/kg, i.p.) does not modify chronic constriction injury (CCI)-induced cold allodynia. Verbascoside (200 mg/kg, i.p.) decreases hyper-sensitivity to cold stimulus, acetone, on day 3 in rats. Verbascoside also significantly reduces behavioral changes associated with neuropathy. Moreover, Verbascoside decreases Bax and increases Bcl-2 on day 3^[3].