谷维素

谷维素用途

【用途一】
谷维素（11042-64-1）主要作用于间脑的植物神经系统与分泌中枢，从而改善和调节植物神经功能失调、内分泌平衡障碍及精神失调等症状。用于植物神经功能失调、周期性神经病、脑震荡后遗症、妇女更年期综合征、经前期紧张、血管性头痛和胃肠性血管神经官能症等。

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谷维素名称

[ CAS 号 ]:
11042-64-1

[ 中文名 ]:
γ-谷维素

[ 英文名 ]:
γ-Oryzanol

[中文别名 ]:

谷维素

[英文别名 ]:

Cycloartenylferulate
gamma-Oryzanol
MFCD00867548
Oryzanol A
γ-Oryzanol
EINECS 244-285-1

谷维素生物活性

[ 描述 ]:

γ-Oryzanol 有效抑制小鼠纹状体中的 DNA 甲基转移酶 (DNMTs)。抑制 DNMT1 和 DNMT3a,IC50 分别为 3.2 μM 和 22.3 μM。

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> DNA甲基转移酶

研究领域 >> 代谢疾病

[ 靶点 ]

DNMT1:3.2 μM (IC50)

DNMT3A:22.3 μM (IC50)

[体外研究]

γ-谷维素显着抑制DNMT1(IC50 =3.2μM),DNMT 3a(IC50 =22.3μM)和DNMT 3b(最大抑制57％)的活性。相反,γ-谷维素的代谢物阿魏酸的抑制活性远低于γ-谷维素的抑制活性。此外,γ-谷维素可作为ERRγ的部分拮抗剂,ERRγ主要作为DNMT1产生的正调节因子,从而降低DNMT1的活性[1]。

[体内研究]

糙米特异性生物活性成分γ-谷维素(阿魏酸酯和几种植物甾醇的混合物)通过降低下丘脑内质网(ER)应力来减弱对膳食脂肪的偏好。 γ-谷维素改善HFD诱导的小鼠纹状体中D2R启动子区的DNA高甲基化。 γ-谷维素可以以纹状体特异性方式调节DNMT的水平。 γ-谷维素部分降低ERRγ活性(先天值降低约40％)。通过强饲法口服给予雄性小鼠γ-谷维素显着减弱了对HFD的偏好(载体治疗小鼠的93％),导致体重增加明显减弱[1]。

[激酶实验]

为了评估每种化合物对DNA甲基化的抑制活性，在每种化合物（20μM用于筛选测定），S-腺苷甲硫氨酸（SAM;10μM）存在下测量S-腺苷-1-高半胱氨酸（SAH）的形成。）和DNMT底物（4 ng /μL）在37°C下保持90分钟。为了评估Michaelis-Menten动力学，将DNMT1（20μM）与γ-谷维素，SAM（5μM）和指定浓度的聚dI-dC在37℃温育90分钟。将DNMT3a（100μM）和DNMT3b（100μM）与γ-谷维素，SAM（5μM）和指定浓度的聚dG·dC在37℃温育120分钟。测定一式四份进行。将提取的蛋白质（0.75 mg / mL）与SAM（5μM），poly dI-dC（5μg/ mL）和poly dG•dC（5μg/ mL）在40°C孵育120分钟，并形成SAH测量[1]。

[动物实验]

小鼠[1]使用7周龄雄性C57BL / 6J小鼠。为了评估对HFD的偏好，在食物选择测试期间通过管饲法将γ-谷维素施用于8周龄小鼠。对于其他实验，将含有0.4％γ-谷维素的HFD制成粒料。喂食12周后，从纹状体和下丘脑收集组织。根据小鼠的平均食物摄入量估算的γ-谷维素的每日摄入量约为320μg/ g体重。测定γ-谷维素的剂量。

[参考文献]

[1]. Kozuka C, et al. Impact of brown rice-specific γ-oryzanol on epigenetic modulation of dopamine D2 receptors in brain striatum in high-fat-diet-induced obesity in mice. Diabetologia. 2017 Aug;60(8):1502-1511.

[相关活性小分子]

阿扎胞苷 | SGI-1027 | N-酞酰-L-色氨酸 | 泽布拉林 | 罗米鲁曲 | 桧木醇 | DC_517 | DC-05 | 葡萄糖缀合的MGMT抑制剂

谷维素物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
663.2±40.0 °C at 760 mmHg

[ 熔点 ]:
135-137°C

[ 分子式 ]:
C₄₀H₅₈O₄

[ 分子量 ]:
602.886

[ 闪点 ]:
193.8±20.8 °C

[ 精确质量 ]:
602.433533

[ PSA ]:
55.76000

[ LogP ]:
12.85

[ 外观性状 ]:
白色结晶粉末

[ 蒸汽压 ]:
0.0±2.1 mmHg at 25°C

[ 折射率 ]:
1.570

[ 储存条件 ]:
存放于惰性气体之中;避免空气

[ 水溶解性 ]:
水溶性：实际上不溶；可溶于：氯仿,丙酮,苯,乙醚；微溶：醇

谷维素MSDS

详细MSDS(安全技术说明书)

谷维素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RN0050000

CHEMICAL NAME :: gamma-Oryzanol

CAS REGISTRY NUMBER :: 11042-64-1

LAST UPDATED :: 199706

DATA ITEMS CITED :: 17

MOLECULAR FORMULA :: C40-H58-O4

MOLECULAR WEIGHT :: 602.98

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >25 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,297,1995

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Administration onto the skin

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 7,1295,1979

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1250 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea Skin and Appendages - hair

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 7,2781,1973

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >1 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 7,2781,1973

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 382 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,297,1995

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 7,2781,1973

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >25 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,297,1995

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >10 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea Skin and Appendages - hair

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 7,2781,1973

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >2500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 7,2781,1973

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 811 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,297,1995

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 7,2781,1973

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 6,2401,1978

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >5 gm/kg

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 6,2401,1978

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >2500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 6,2401,1978

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Administration onto the skin

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 7,1295,1979 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 54300 mg/kg/26W-I

TOXIC EFFECTS :: Related to Chronic Data - death

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 8,3417,1974 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 36 mg/kg

SEX/DURATION :: female 7-12 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 6,1717,1972

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谷维素安全信息

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
UN 2811 6.1/PG 2

[ RTECS号 ]:
RN0050000

[ 海关编码 ]:
2932999099

谷维素制备

提取方法有吸附法和弱酸取代法。弱酸取代法的生产过程包括碱炼捕集和弱酸沉析分离两大工序。毛糠油中谷维素含量为2%~3%。首先，谷维素（具有酚类物质的性质）与NaOH混合生产钠盐，谷维素钠盐亲水性大大增加，易被碱性皂吸附一起下沉。毛糠油通过两次碱炼，可使油中80%~90%的谷维素富集于二次皂脚中，达到捕集的目的。然后将皂脚补充皂化，改善其物理性能，可使谷维素分离。再利用碱性甲醇能溶解谷素钠盐和脂肪酸皂，而不溶解糠蜡、脂肪醇、甾醇等不皂化物的特点，使谷维素钠盐与粘稠物质不皂化物分离。再利用弱有机酸分解谷维素钠盐，还原谷维素，即得产品。

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谷维素海关

[ 海关编码 ]: 2932999099

[ 中文概述 ]:
2932999099. 其他仅含氧杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2932999099. other heterocyclic compounds with oxygen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

谷维素

谷维素用途

谷维素名称

谷维素生物活性

谷维素物理化学性质

谷维素MSDS

详细MSDS(安全技术说明书)

谷维素毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

谷维素安全信息

谷维素制备

谷维素海关

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