Coixol (6-Methoxy-2-benzoxazolinone) is a polyphenol compound extracted from Coix lacryma-jobi, which has anti-tumor, anti-inflammatory and antioxidant activities[1]. Coixol can act as a central muscle relaxant and has anticonvulsant effects[2]. Coixol can improve lung injury caused by Toxoplasma infection by interfering with the Toxoplasma HSP70/TLR4/NF-κB signaling pathway[3].
In vitro, pretreatment of PC12 cells with Coixol (0.25-2μM) for 48h protected PC12 cells from Abeta25-35-induced neurotoxicity, increased Bcl-2 mRNA expression, mitochondrial membrane potential and Na+-K+ ATPase activity, and decreased Bax mRNA expression, caspase-3 activity and intracellular Ca2+ release[4]. Coixol (0-33.035mg/L) treatment of A549 cells for 24-72h inhibited cell proliferation in a concentration-dependent manner, induced cell morphological changes, upregulated the expression of intracellular caspase-3, caspase-8, caspase-9 and Bax proteins, and downregulated the expression of Bcl-2 protein[5].
In vivo, Coixol (25, 50mg/kg) was orally treated with non-diabetic and diabetic rats for 15 days, which improved glucose tolerance in non-diabetic and diabetic rats and increased plasma insulin levels within 30min[6].
References:
[1] Hu Y, Zhou Q, Liu T, et al. Coixol suppresses NF-κB, MAPK pathways and NLRP3 inflammasome activation in lipopolysaccharide-induced RAW 264.7 cells[J]. Molecules, 2020, 25(4): 894.
[2] Wei T H, Hsieh C L. Headaches, migraine, and herbal medicine[M]//Treatments, nutraceuticals, supplements, and herbal medicine in neurological disorders. Academic Press, 2023: 401-419.
[3] Shen X Y, Lu J M, Lu Y N, et al. Coixol ameliorates Toxoplasma gondii infection-induced lung injury by interfering with T. gondii HSP70/TLR4/NF-κB signaling pathway[J]. International Immunopharmacology, 2023, 118: 110031.
[4] Chen J Y, Li C Y, Mong M C, et al. Preventive effects of coixol, an active compound of adlay seed, in NGF-differentiated PC12 cells against beta-amyloid25-35-induced neurotoxicity[J]. Asian Biomedicine: Research, Reviews and News, 2024, 18(5): 224.
[5] Wang X C, Shen X Y, Chen L, et al. Preparation, characterization, and anticancer effects of an inclusion complex of coixol with β-cyclodextrin polymers[J]. Pharmaceutical Biology, 2024, 62(1): 2294331.
[6] Hameed A, Hafizur R M, Khan M I, et al. Coixol amplifies glucose-stimulated insulin secretion via cAMP mediated signaling pathway[J]. European Journal of Pharmacology, 2019, 858: 172514.
Coixol (6-Methoxy-2-benzoxazolinone)是一种从薏苡仁（Coix lacryma-jobi）中提取的多酚类化合物，具有抗肿瘤、抗炎和抗氧化活性[1]。Coixol能够作为一种中枢肌肉松弛剂，具有抗惊厥作用[2]。Coixol能够通过干扰弓形虫HSP70/TLR4/NF-κB信号通路改善弓形虫感染引起的肺损伤[3]。
在体外，Coixol（0.25-2μM）预处理PC12细胞48h，对Abeta25-35诱导的神经毒性发挥了保护作用，增加了Bcl-2 mRNA表达、线粒体膜电位和Na+-K+ ATPase活性，降低了Bax mRNA表达、caspase-3活性和细胞内Ca2+释放[4]。Coixol（0-33.035mg/L）处理A549细胞24-72h，以浓度依赖性方式抑制了细胞增殖，诱导了细胞形态变化，上调了细胞内caspase-3、caspase-8、caspase-9和Bax蛋白的表达，下调了Bcl-2蛋白的表达[5]。
在体内，Coixol（25, 50mg/kg）通过口服处理非糖尿病和糖尿病大鼠15天，改善了非糖尿病和糖尿病大鼠的葡萄糖耐受性，并在30分钟内提高了血浆胰岛素水平[6]。