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Verbascoside

MCE China：Verbascoside

Brand：MedChemExpress (MCE)

Cat. No.HY-N0021

CAS：61276-17-3

Synonyms：Acteoside; Kusaginin; TJC160

Purity：99.83%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：Verbascoside acts as an ATP-competitive inhibitor of PKC, with an IC50 of 25 μM. Verbascoside shows Kis 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].

Animal Administration：Rats[2] To induce atopic dermatitis (AD)-like symptoms, 2,4-dinitrochlorobenzene (DNCB) is used. Briefly, the dorsal hair of the mice is removed using an electronic clipper 2 days before DNCB treatment. An application of 200 µL of 1% DNCB (in acetone:olive oil = 4:1) is made to the shaved dorsal skin for sensitization. The repeated challenge is performed on the same site with 0.2% DNCB once every 3 days for about 2 weeks. The mice are divided into 4 groups (n = 6 per group): (1) vehicle-treated controls, (2) DNCB-treated only, (3) 1% Verbascoside (in acetone:olive oil 4:1)-treated only, and (4) DNCB + 1% Verbascoside-treated group[2].

Cell Assay：The lymphocytic mouse leukemia L1210 cells (ATCC, CCL 219) are plated sparsely at 104 cells per well in 24-well cluster plates in Dulbecco’s modified Eagle medium containing 10% fetal calf serum, 4 mM glutamine, 100 U/mL penicillin, 100 µg/mL streptomycin sulfate, and Verbascoside (solubilized in DMSO). After a 2-day incubation period at 37°C in a humidified atmosphere (5% CO2 in air), growth is monitored by counting cell numbers in a Coulter-counter. IC50 values are calculated on the basis of the linear regression lines established for each compound tested[1].

IC50 & Target：PKC 25 μM (IC50)

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References：

[1]. Herbert JM, et al. Verbascoside isolated from Lantana camara, an inhibitor of protein kinase C. J Nat Prod. 1991 Nov-Dec;54(6):1595-600.  [Content Brief]

[2]. Li Y, et al. Verbascoside Alleviates Atopic Dermatitis-Like Symptoms in Mice via Its Potent Anti-Inflammatory Effect. Int Arch Allergy Immunol. 2018;175(4):220-230.  [Content Brief]

[3]. Amin B, et al. The Effect of Verbascoside in Neuropathic Pain Induced by Chronic Constriction Injury in Rats. Phytother Res. 2016 Jan;30(1):128-35.  [Content Brief]