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。
| 生物活性 | Heptelidic acid (Koningic acid) is a sesquiterpeneantibiotic[1]. Heptelidic acid inhibits Etoposide-inducedapoptosisvia downregulation ofcaspases[2]. Koningic acid (KA) is a specificGAPDHinhibitor with anIC50of 90 μM[3]. |
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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 IC50value of 40 μM after 8 h of Etoposide treatment[2].
Heptelidic acid (Koningic acid; KA), a natural product obtained from theTrichodermafungus, can directly bind to the active site of human GAPDH. The expression ofT. koningiiKAr-GAPDH successfully rescued cell viability in human cells treated with Heptelidic acid. HEK293T cells expressingT. koningiiKAr-GAPDH exhibited complete cell viability after treatment with 0-200 μM Heptelidic acid with the IC50=5 μM[3].
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. |
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体内研究
(In Vivo) | Heptelidic acid (Koningic acid; KA) is bioavailable and induces dynamic changes to glycolysis in vivo[3].
| Animal Model: | 6-week old femaleFoxn1numice 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). |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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