Sesamoside

Sesamoside is an orally active anti-inflammatory, anti-hypoxic and analgesic agent. Sesamoside inhibits the phosphorylation of ERK and JNK, downregulates NLRP3 expression, restricts the nuclear localization of P65, regulates AKR1B1 expression, and reduces the expression of TRPV1 gene in the spinal cord. Sesamoside reduces the production of TNF-α, IL-6, IL-1β, iNOS and NO, restores cellular metabolism and organ function, and alleviates cold and mechanical hyperalgesia. Sesamoside can be used in research related to septic shock, high-altitude pulmonary edema and neuropathic pain^[1][2][3][4]. In Vitro:Sesamoside (25-500 µM; 12 h) shows no cytotoxicity in mouse Raw264.7 cells even at concentrations up to 200 µM, with an IC₅₀ of 246.4 µM, and only induces significant apoptosis at the concentration of 500 µM^[1].
Sesamoside (25-200 µM; 6-24 h) dose-dependently and time-dependently inhibits the LPS (HY-D1056)-induced upregulation of TNF-α, IL-6, IL-1β and iNOS mRNA expression as well as NO production in mouse Raw264.7 cells^[1].
Sesamoside (200 µM; 6-24 h) inhibits LPS-induced activation of the NF-κB/MAPK pathway in mouse Raw264.7 cells by reducing the phosphorylation levels of ERK and JNK, and downregulating NLRP3 protein expression in a time-dependent manner^[1].
Sesamoside (200 µM; 6-24 h) inhibits LPS-induced nuclear localization of P65 in murine Raw264.7 cells in a time-dependent manner at the concentration of 200 µM^[1].
Sesamoside binds tightly to human aldose reductase (AR/AKR1B1) with a binding energy of -5.5 kcal/mol^[2].
Pretreatment of human bronchial epithelial BEAS-2B cells with sesamoside (200 μM; 6 h) significantly attenuates hypoxia-induced upregulation of AR, ERK, VEGF-α and TNF-α mRNA expression, elevates hypoxia-downregulated IL-10 mRNA expression, and reduces hypoxia-induced IL-6 secretion, but exerts no significant effect on HIF-1α mRNA expression^[2].
Pretreatment of human bronchial epithelial BEAS-2B cells with sesamoside (200 μM; 6 h) reduces hypoxia-induced IL-6 secretion^[2]. In Vivo:Sesamoside (1-10 mg/kg; i.p.; single dose) dose-dependently reduces LPS-induced inflammatory responses and multi-organ damage in septic shock mice by inhibiting the NF-κB/MAPK signaling pathway^[1].
Sesamoside (5-7.5 mg/kg; i.p., p.o.; single dose) alleviates Paclitaxel (HY-B0015)-induced cold and mechanical peripheral neuropathy in mice, with 7.5 mg/kg doses (both intraperitoneal and oral) showing consistent efficacy, and oral 7.5 mg/kg sesamoside reducing spinal TRPV1 gene expression^[3].