Hygrolidin

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Hygrolidin 

Hygrolidin 是一种 16 元大环内酯类抗生素,来自于吸水链霉菌 (Streptomyces hygroscopicus) D-1166。Hygrolidin 对 Valsa ceratosperma 具有抗真菌活性。Hygrolidin 诱导 p21 表达并中止 G1 和 S 期的细胞周期进程。Hygrolidin 具有抗肿瘤活性。

Hygrolidin

Hygrolidin Chemical Structure

CAS No. : 83329-73-1

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生物活性

Hygrolidin is a 16-membered macrolide antibiotic produced by Streptomyces hygroscopicus D-1166. Hygrolidin has anti-fungus activity against Valsa ceratosperma. Hygrolidin induces p21 expression and abrogates cell cycle progression at G1 and S phases. Hygrolidin has antitumor activity[1][2][3].

体外研究
(In Vitro)

Hygrolidin (0.1, 1 μg/ml; for 24 h) increases both G1 and S phase populations and decreases M phase population[1].
Hygrolidin (0.1, 1, 10 μg/ml; for 24 h) decreases the amounts of cdk4, cyclin D, cyclin B and increases the amounts of cyclin E and p21. Hygrolidin-induced p21 preferentially associates with cyclin A-cdk2 complex and inhibits it[1].
Hygrolidin (0.1, 1 μg/ml; for 24 h) selectively induces p21 in DLD-1 cells at mRNA level, but not in WI-38 fibroblasts[1].
Hygrolidin, for 3 days, inhibits growth of various cell lines including DLD-1 colon cancer, LNCaP prostate cancer, K562 leukemia cells, LNCaP prostate cancer, EL-4 lymphoma (IC50s = 1.0-33 ng/ml, respectively)[1].
Hygrolidin shows growth inhibition on Trypanosoma cruzi (IC50=1.1 nM), Trypanosoma brucei brucei (IC50=77 nM), and Leishmania donovani (IC50=72.5 nM)[3].

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

Cell Cycle Analysis[1]

Cell Line: DLD-1 cells
Concentration: 0.1, 1 μg/ml
Incubation Time: For 24 hours
Result: Increased both G1 and S phase populations and decreased M phase population.

Western Blot Analysis[1]

Cell Line: DLD-1 cells
Concentration: 0.1, 1, 10 μg/ml
Incubation Time: For 24 hours
Result: Decreased the amounts of cdk4, cyclin D, cyclin B and increased the amounts of cyclin E and p21.

RT-PCR[1]

Cell Line: DLD-1 or WI-38 cells
Concentration: 0.1, 1 μg/ml
Incubation Time: For 24 hours
Result: Selectively induced p21 in DLD-1 cells at mRNA level, but not in WI-38 fibroblasts.

分子量

690.86

Formula

C38H58O11

CAS 号

83329-73-1

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]. Manabu Kawada, et al. Hygrolidin induces p21 expression and abrogates cell cycle progression at G1 and S phases. Biochem Biophys Res Commun. 2002 Oct 18;298(1):178-83.

    [2]. H Seto, et al. The isolation and structures of hygrolidin amide and defumarylhygrolidin. J Antibiot (Tokyo). 1984 May;37(5):610-3.

    [3]. F Annang, et al. High-throughput screening platform for natural product-based drug discovery against 3 neglected tropical diseases: human African trypanosomiasis, leishmaniasis, and Chagas disease. J Biomol Screen. 2015 Jan;20(1):82-91.

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