Vicenin 2

Vicenin 2 is an orally active angiotensin-converting enzyme (ACE) inhibitor with the IC₅₀ value of 43.83 ± 3.01μM^[1]. Vicenin 2 has anti-inflammatory and antioxidant properties which make it potential applications in various fields, including skin health and cancer therapy.

In vitro, Vicenin 2 (6.25–400μM) incubated human dermal fibroblast (HDF) cell for 24h. Vicenin 2 treatment on HDF cells enhanced cell proliferation in a dose-dependent up to 50μM, but the higher concentrations inhibited proliferation. Low concentrations of Vicenin 2 (12.5 and 25μM) have significantly induced the cell migration and wound closure, while higher concentrations (50 and 100µM) reduced these effects. In addition, treatment with 100μM of Vicenin 2 on HDF significantly increased the expression of inflammatory cytokines and higher expression for inflammatory mediators (NF-κB, iNOS, and COX-2) and healing growth factors (VEGF and TGF-β) proteins^[2]. Vicenin 2 (40μM) incubation for 24 hours can restore the antioxidant defense of human gastric epithelial cells (GES-1) by modulating key signaling pathways (PI3K/AKT and MAPK) and upregulating Nrf2 expression, effectively protecting them from cytotoxicity, oxidative stress, DNA damage, and inflammation induced by Helicobacter pylori. These findings suggest that Vicenin 2 could serve as a potential therapeutic agent for preventing H. pylori-induced gastric carcinogenesis^[3]. NCI-H23 cells were treated with 10–100µM of Vicenin 2 for 24h. There was a gradual reduction in the percent surviving cells from 60µM to 100µM. NCI-H23 cells treated with radiation exposure with and without 80µM Vicenin 2 suggested that there was greater reduction in percent cell survival with Vicenin 2 treatment. Vicenin 2 showed a potent radiosensitizing property while also showing chemotherapeutic property against Non-small cell lung cancer (NSCLC) cell line NCI-H23^[4].

In vivo,Vicenin 2 (50mg/kg/day) administered orally via oral gavage tube into dextran sulfate sodium-induced colitis mice model for 7 days exerted therapeutic effects by the inhibition of pro-inflammatory mediators (iNOS and COX-2) and suppression of specific inflammatory markers expression^[5]. In a study on ovariectomy (OVX)-induced osteoporosis rat models, Vicenin 2 orally administered at doses of 5mg/kg/day or 10mg/kg/day for 12 consecutive weeks significantly improved body mass, uterus index, lipid profiles, and inflammatory markers. Vicenin 2 also reduced bone turnover markers and increased serum calcium levels in the OVX rats. These results suggested that Vicenin 2 could be an excellent candidate to treat and manage bone related disease or disorders^[6]. The administration of Vicenin 2 (23.8µg/mouse) into LPS-induced lethal endotoxemia model given twice at 12 and 50 hours post-LPS injection, significantly increased survival rates, reduced endothelial cell protein C receptor shedding, decreased pro-inflammatory cytokine expression, protected vascular barrier integrity, and inhibited leukocyte migration. These findings suggest that Vicenin 2 could serve as a potential therapeutic agent for treating severe vascular inflammatory diseases ^[7].

References:
[1] Zhang YQ, et al. Bioassay-guided preparative separation of angiotensin-converting enzyme inhibitory C-flavone glycosides from Desmodium styracifolium by recycling complexation high-speed counter-current chromatography. J Pharm Biomed Anal. 2015 Jan;102:276-81.
[2] Tan W S, Arulselvan P, Ng S F, et al. Healing Effect of Vicenin-2 (Vicenin-2) on Human Dermal Fibroblast (HDF) and Development Vicenin-2 Hydrocolloid Film Based on Alginate as Potential Wound Dressing. Biomed Res Int. 2020 Apr 23:2020:4730858.
[3] Zhang Y F, Sun J, Dong Y, et al. Vicenin-2 inhibits the Helicobacterium pylori infection associated gastric carcinogenic events through modulation of PI3K/AKT and Nrf2 signaling in GES-1 cells. J Biochem Mol Toxicol. 2021 Mar;35(3):e22680.
[4] Baruah T J, Sharan R N, Kma L. Vicenin-2: a potential radiosensitizer of non-small cell lung cancer cells. Mol Biol Rep. 2018 Oct;45(5):1219-1225.
[5] Yin Y T, Ye L, Niu Z B, Fang W H.Anti-inflammatory effects of Vicenin-2 on dextran sulfate sodium-induced colitis in mice. Drug Dev Res. 2019 Aug;80(5):546-555.
[6] Zhang Z P, Zhao Q P, Liu T J,et al. Effect of Vicenin-2 on ovariectomy-induced osteoporosis in rats. Biomed Pharmacother. 2020 Sep:129:110474.
[7] Kang H J, Ku S K, Jung B K, BaeJ S. Anti-inflammatory effects of vicenin-2 and scolymoside in vitro and in vivo. Inflamm Res. 2015 Dec;64(12):1005-21.