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。
| 生物活性 | Hygrolidin is a 16-memberedmacrolideantibioticproduced byStreptomyces hygroscopicusD-1166. Hygrolidin hasanti-fungusactivity againstValsa ceratosperma. Hygrolidin induces p21 expression and abrogates cell cycle progression at G1 and S phases. Hygrolidin has antitumor activity[1][2][3]. |
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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 onTrypanosoma cruzi(IC50=1.1 nM),Trypanosoma brucei brucei(IC50=77 nM), andLeishmania donovani(IC50=72.5 nM)[3].
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. |
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| 结构分类 | - Antibiotics
- Macrolide Antibiotics
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| 来源 | Streptomyces hygroscopicus |
| 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. |
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