Coixol (6-Methoxy-2-benzoxazolinone)
(Synonyms: 6-甲氧基-2-苯唑啉酮,6-Methoxy-2-benzoxazolinone; 6-MBOA) 目录号 : GC30144
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。
Cas No.:532-91-2
Sample solution is provided at 25 µL, 10mM.
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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]。
| Cell experiment [1]: | |
Cell lines | PC12 cells |
Preparation Method | Differentiated PC12 cells were treated with Coixol at 0.125μM, 0.25μM, 0.5μM, 1μM, and 2μM for 48h. Then, cells were further exposed to Abeta25-35 at 20μM for 24h. MTT assay to measure cell viability. |
Reaction Conditions | 0.125, 0.25, 0.5, 1, 2μM; 48h |
Applications | Coixol pretreatments at 0.25-2μM increased cell survival when compared with Abeta groups. |
| Animal experiment [2]: | |
Animal models | SD rats |
Preparation Method | The experimental rats were divided into four groups (n=5 rats/group): Group I, Untreated diabetic rats (Db); Group II, Diabetic rats treated with Coixol 25mg/kg(CX-25); Group III, Diabetic rats treated with Coixol 50mg/kg (CX-50); Group IV, Diabetic rats treated with Glibenclamide 5mg/kg (GB) once daily for 15 days. Coixol were given orally in 1ml of water suspension by gavage to the experimental groups. The fasting blood glucose was measured with on day 1, 7, and 15, respectively. |
Dosage form | 25, 50mg/kg; for 15 days; p.o. |
Applications | Coixol improves glucose tolerance and stimulates glucose-induced plasma insulin in non-diabetic and diabetic rats. |
References: | |
| Cas No. | 532-91-2 | SDF | |
| 别名 | 6-甲氧基-2-苯唑啉酮,6-Methoxy-2-benzoxazolinone; 6-MBOA | ||
| Canonical SMILES | O=C1OC2=CC(OC)=CC=C2N1 | ||
| 分子式 | C8H7NO3 | 分子量 | 165.15 |
| 溶解度 | DMSO : ≥ 30 mg/mL (181.65 mM) | 储存条件 | Store at 2-8°C,protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 6.0551 mL | 30.2755 mL | 60.551 mL |
| 5 mM | 1.211 mL | 6.0551 mL | 12.1102 mL |
| 10 mM | 0.6055 mL | 3.0276 mL | 6.0551 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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