Herboxidiene(Synonyms: GEX1A)

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Herboxidiene (Synonyms: GEX1A)

Herboxidiene (GEX1A) 是一种有效的植物毒性聚酮类化合物，来源于链霉菌 A7847，具有多种活性，包括除草、抗胆固醇、抗肿瘤等。Herboxidiene 通过与剪接体相关蛋白 (SAP) 155 结合抑制前 mRNA 剪接 (pre-mRNA splicing) 过程，SAP 是剪接体中 SF3b 的一个亚单位。

Herboxidiene(Synonyms: GEX1A)

Herboxidiene Chemical Structure

CAS No. : 142861-00-5

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生物活性

Herboxidiene (GEX1A) is a potent phytotoxic polyketide from Streptomyces sp. A7847 with a diverse range of activities, including herbicidal, anti-cholesterol, anti-tumor effects. Herboxidiene inhibits the pre-mRNA splicing process by binding to spliceosome-associated protein (SAP) 155, a subunit of SF3b, in the splicesome[1][2].

体外研究
(In Vitro)

Herboxidiene (24 hours) induces both G1 and G2/M arrest in a human normal fibroblast cell line, WI-38, with an IC50 of 7.6 nM[3].
Herboxidiene exhibits cytotoxicity against A431, A549, and DLD-1 cells with IC50s of 3.7, 21, 51 nM, respectively[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Herboxidiene (GEX1A) (1 mg/kg; i.p.; once) shows significant antitumor activity[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c mice (bearing SVT2 murine fibrosarcoma)[3]
Dosage: 1 mg/kg
Administration: I.p.; once
Result: Showed significant antitumor activity on day 4.

分子量

438.60

Formula

C25H42O6
CAS 号

142861-00-5
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Pokhrel AR, et al. Herboxidiene biosynthesis, production, and structural modifications: prospect for hybrids with related polyketide. Appl Microbiol Biotechnol. 2015;99(20):8351‐8362.

    [2]. Sakai Y, et al. GEX1 compounds, novel antitumor antibiotics related to herboxidiene, produced by Streptomyces sp. I. Taxonomy, production, isolation, physicochemical properties and biological activities. J Antibiot (Tokyo). 2002;55(10):855‐862.

    [3]. Miller-Wideman M, et al. Herboxidiene, a new herbicidal substance from Streptomyces chromofuscus A7847. Taxonomy, fermentation, isolation, physico-chemical and biological properties. J Antibiot (Tokyo). 1992;45(6):914‐921.

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