Gnetol

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Gnetol  纯度: ≥98.0%

Gnetol 是从 Gnetum ula Brongn 的根中分离出来的酚类化合物。Gnetol 有效抑制 COX-1 (IC50 为 0.78 μM) 和 HDAC。Gnetol 是一种有效的酪氨酸酶抑制剂，对鼠酪氨酸酶的 IC50 为 4.5 μM，可抑制黑色素的生物合成。Gnetol 具有抗氧化，抗增殖，抗癌和保肝活性。Gnetol 还具有浓度依赖性的 α-淀粉酶，α-葡萄糖苷酶和脂肪形成活性。

Gnetol

Gnetol Chemical Structure

CAS No. : 86361-55-9

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生物活性

Gnetol is a phenolic compound isolated from the root of Gnetum ula Brongn. Gnetol potently inhibits COX-1 (IC50 of 0.78 μM) and HDAC. Gnetol is a potent tyrosinase inhibitor with an IC50 of 4.5 μM for murine tyrosinase and suppresses melanin biosynthesis. Gnetol has antioxidant, antiproliferative, anticancer and hepatoprotective activity. Gnetol also possesses concentration-dependent α-Amylase, α-glucosidase, and adipogenesis activities[1][2][3].

IC50 & Target[1][2]

COX-1

0.78 μM (IC50)

Tyrosinase

4.5 μM (IC50)

HDAC

 

体外研究
(In Vitro)

The antiproliferative activities of Gnetol are tested in HCT-116, Hep-G2, MDA-MB-231, and PC-3 cell lines by measuring cell viability after treatment with 4.1 μM, 40.9 μM, 204.7 μM, 409.4 μM, and 1023.6 μM. Gnetol shows concentration-dependent reductions in cell viability in cancer cell lines with greatest activity in colorectal cancer[1].
Gnetol at 200 µg/mL significantly offers the highest protection of 54.3% against the toxicant. A lower dose of Gnetol (50 µg/mL) also shields the cell line from the toxic effects of CCl4[3].
The ligand molecule TGF-β and PPARα protein show that Gnetol has the binding affinity of 7.0 and 8.4, respectively[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Male Sprague-Dawley rats were cannulated and dosed either intravenously with Gnetol (10 μg/kg) or orally (100 mg/kg). After oral and intravenous administration, Gnetol is detected in both serum and urine as the parent compound and as a glucuronidated metabolite. The bioavailability of Gnetol is determined to be 6%. Gnetol is rapidly glucuronidated and is excreted in urine and via nonrenal routes[1].
Pretreatment of Male NIH Swiss mice (20-35 g) with Gnetol (50mg/kg, SC) is able to increase the latency period to response in analgesia models[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

244.24

Formula

C14H12O4
CAS 号

86361-55-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献

  • [1]. Remsberg CM, et al. Preclinical Pharmacokinetics and Pharmacodynamics and Content Analysis of Gnetol in Foodstuffs. Phytother Res. 2015 Aug;29(8):1168-79.

    [2]. Ohguchi K, et al. Gnetol as a potent tyrosinase inhibitor from genus Gnetum. Biosci Biotechnol Biochem. 2003 Mar;67(3):663-5.

    [3]. Jinadatta P, et al. In silico, in vitro: antioxidant and antihepatotoxic activity of gnetol from Gnetum ula Brongn. Bioimpacts. 2019;9(4):239-249.

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