Forskolin 是一種有效的腺苷酸環(huán)化酶激活劑，對 I 型腺苷酸環(huán)化酶 [1] 的 IC50 為 41 nM。 Forskolin，EC50 為 0.5 μM，也是細(xì)胞內(nèi) cAMP 形成的誘導(dǎo)劑 [2] Forskolin 誘導(dǎo)多種細(xì)胞分化，激活黃體酮 X 受體 (PXR) 和 FXR[3] Forskolin 具有對心臟有收縮作用，并具有抗血小板聚集和降壓作用毛喉素還誘導(dǎo)自噬[4][5]。

毛喉素 (Coleonol) 也是前列腺癌 (PC) 細(xì)胞中有效的外泌體生物發(fā)生和/或分泌激活劑[7]。毛喉素對人紅細(xì)胞膜自由基應(yīng)激的調(diào)控及其治療心血管疾病和糖尿病的前景[8]。毛喉素通過增加cAMP減弱細(xì)胞毒性和細(xì)胞凋亡。

體內(nèi)研究表明，毛喉素主要降低健康大鼠的基礎(chǔ)葡萄糖，并減輕糖尿病大鼠的高血糖癥的嚴(yán)重程度[6]。 Mrp4(-/-) 小鼠在視網(wǎng)膜血管發(fā)育方面沒有表現(xiàn)出明顯的異常，但 Mrp4(-/-) 小鼠的視網(wǎng)膜血管發(fā)育在毛喉素給藥后受到抑制。經(jīng)毛喉素處理的 Mrp4(-/- ) 小鼠顯示 Ki67 陽性和裂解半胱天冬酶 3 陽性 EC 數(shù)量增加，周細(xì)胞覆蓋量顯著減少，空袖數(shù)量減少[2]。

產(chǎn)品性質(zhì)：

Cas No.：66575-29-9

別名：毛喉素; Coleonol; Colforsin

化學(xué)名： [(3R,4aR,5S,6S,6aS,10S,10aR,10bS)-3-ethenyl-6,10,10b-trihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-5,6,6a,8,9,10-hexahydro-2H-benzo[f]chromen-5-yl] acetate

Canonical SMILES CC(=O)OC1C(C2C(CCC(C2(C3(C1(OC(CC3=O)(C)C=C)C)O)C)O)(C)C)O

分子式：C22H34O7

分子量：410.5

溶解度：≥ 20.525mg/mL in DMSO

儲存條件：-20°C, protect from light

注意事項：

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References:

[1]: Robbins JD, Boring DL, et,al. Forskolin carbamates: binding and activation studies with type I adenylyl cyclase. J Med Chem. 1996 Jul 5;39(14):2745-52. doi: 10.1021/jm960191+. PMID: 8709105.

[2]: Matsumiya W, Kusuhara S, et,al. Forskolin modifies retinal vascular development in Mrp4-knockout mice. Invest Ophthalmol Vis Sci. 2012 Dec 7;53(13):8029-35. doi: 10.1167/iovs.12-10781. PMID: 23154460; PMCID: PMC3517270.

[3]: Mayati A, Moreau A, et,al. Functional polarization of human hepatoma HepaRG cells in response to forskolin. Sci Rep. 2018 Oct 31;8(1):16115. doi: 10.1038/s41598-018-34421-8. PMID: 30382126; PMCID: PMC6208432.

[4]: Awad JA, Johnson RA, et,al. Interactions of forskolin and adenylate cyclase. Effects on substrate kinetics and protection against inactivation by heat and N-ethylmaleimide. J Biol Chem. 1983 Mar 10;258(5):2960-5. PMID: 6681815.

[5]: Seamon KB, Daly JW, et,al. Structure-activity relationships for activation of adenylate cyclase by the diterpene forskolin and its derivatives. J Med Chem. 1983 Mar;26(3):436-9. doi: 10.1021/jm00357a021. PMID: 6681845.

[6]: Ríos-Silva M, Trujillo X, et,al. Effect of chronic administration of forskolin on glycemia and oxidative stress in rats with and without experimental diabetes. Int J Med Sci. 2014 Mar 11;11(5):448-52. doi: 10.7150/ijms.8034. PMID: 24688307; PMCID: PMC3970096.

[7]: Datta A, Kim H, et,al. High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. Sci Rep. 2018 May 25;8(1):8161. doi: 10.1038/s41598-018-26411-7. PMID: 29802284; PMCID: PMC5970137.

[8]:Niaz MA, Singh RB. Modulation of free radical stress in human red blood cell membrane by forskolin and the prospects for treatment of cardiovascular disease and diabetes. Cell Mol Biol (Noisy-le-grand). 1999 Dec;45(8):1203-7. PMID: 10643969.