Heptelidic acid(Synonyms: 萜烯七脂酸; Koningic acid)

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Heptelidic acid (Synonyms: 萜烯七脂酸; Koningic acid)

Heptelidic acid (Koningic acid) 是一种倍半萜类抗生素 (antibiotic)。Heptelidic acid 通过下调 caspase 从而抑制 Etoposide 诱导的细胞凋亡。Koningic acid (KA) 是一种特异性 GAPDH 抑制剂，IC50 为 90 μM。

Heptelidic acid(Synonyms: 萜烯七脂酸; Koningic acid)

Heptelidic acid Chemical Structure

CAS No. : 57710-57-3

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生物活性

Heptelidic acid (Koningic acid) is a sesquiterpene antibiotic[1]. Heptelidic acid inhibits Etoposide-induced apoptosis via downregulation of caspases[2]. Koningic acid (KA) is a specific GAPDH inhibitor with an IC50of 90 μM[3].

IC50 & Target[2]

Caspase-3

 

体外研究
(In Vitro)

Heptelidic acid is a sesquiterpene antibiotic, found in the culture filtrate of three different strains of fungi isolated from soil samples. Heptelidic acid produces organisms, fermentation, isolation and characterization[1].
Heptelidic acid inhibits Etoposide-induced apoptosis in human leukemia U937 cells[2].Heptelidic acid inhibits caspase- 3 induction in U937 cells with an IC50 value of 40 μM after 8 h of Etoposide treatment[2].
Heptelidic acid (Koningic acid; KA), a natural product obtained from the Trichoderma fungus, can directly bind to the active site of human GAPDH. The expression of T. koningii KAr-GAPDH successfully rescued cell viability in human cells treated with Heptelidic acid. HEK293T cells expressing T. koningii KAr-GAPDH exhibited complete cell viability after treatment with 0-200 μM Heptelidic acid with the IC50=5 μM[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.

Cell Viability Assay[3]

Cell Line: HEK293T cells expressing KAr-GAPDH or EV (top left)
Concentration: 0.1, 1, 10, 100, 1000 μM
Incubation Time: 24 hours
Result: IC50=5 μM.

体内研究
(In Vivo)

Heptelidic acid (Koningic acid; KA) is bioavailable and induces dynamic changes to glycolysis in vivo[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: 6-week old female Foxn1nu mice bearing BT-474 tumor[3]
Dosage: 1, 2.5, 5, and 10 mg/kg
Administration: Daily intraperitoneal (IP) injections, 24 hours
Result: 1 mg/kg was determined to be the maximum tolerated dose (MTD) based upon behavioral monitoring and adverse events at higher doses (hemolysis, hematuria, and anemia).

分子量

280.32

Formula

C15H20O5
CAS 号

57710-57-3
中文名称

萜烯七脂酸
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]. Y Itoh, et al. A new sesquiterpene antibiotic, heptelidic acid producing organisms, fermentation, isolation and characterization. J Antibiot (Tokyo). 1980 May;33(5):468-73.

    [2]. Jin Hee Kim, et al. Heptelidic acid, a sesquiterpene lactone, inhibits Etoposide-induced apoptosis in human leukemia U937 cells. J Microbiol Biotechnol. 2009 Aug;19(8):787-91.

    [3]. Maria V Liberti, et al. A Predictive Model for Selective Targeting of the Warburg Effect through GAPDH Inhibition with a Natural Product. Cell Metab. 2017 Oct 3;26(4):648-659.e8.

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