Betulinic acid

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Chemical Structure| 472-15-1 同义名 : 桦木酸 ;Lupatic acid; Betulic acid; Mairin; NSC 113090; ALS-357
CAS号 : 472-15-1
货号 : A200416
分子式 : C30H48O3
纯度 : 98%
分子量 : 456.7
MDL号 : MFCD00009619
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(76.64 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • Topo I

    Eukaryotic topoisomerase I, IC50:5 μM
描述 Betulinic Acid is a natural pentacyclic triterpenoid compound and a eukaryotic topoisomerase I inhibitor with IC50 value of 0.5 mM. It has anti-inflammatory, anti malaria, anti AIDS and anti-tumor activities[3]. Betulinic Acid is also a new activator of NF κB[4]. Betulinic Acid (20, 40 µM) causes decrease in Bcl-2 expression of MDA-MB-231 cells[5]. Betulinic Acid has anti HIV activity. EC50 of H9 lymphocytes infected with Betulinic Acid is 1.4 μ M[6]. Moreover, oral administration of Betulinic Acid reduced the bleeding score at 10 and 30 mg/kg and improved the stool consistency at 30 mg/kg[7].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00346502 Dysplastic Nevus Syndrome Phase 1 Phase 2 Suspended(The study has been t... 展开 >>emporarily suspended due to funding issues) 收起 << December 2015 United States, Illinois ... 展开 >> University of Illinois at Chicago Medical Center Chicago, Illinois, United States, 60612 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.19mL

0.44mL

0.22mL

10.95mL

2.19mL

1.09mL

21.90mL

4.38mL

2.19mL
参考文献

[1]Melzig MF, Bormann H. Betulinic acid inhibits aminopeptidase N activity. Planta Med. 1998 Oct;64(7):655-7.

[2]Fujioka T, Kashiwada Y, et al. Anti-AIDS agents, 11. Betulinic acid and platanic acid as anti-HIV principles from Syzigium claviflorum, and the anti-HIV activity of structurally related triterpenoids. J Nat Prod. 1994 Feb;57(2):243-7.

[3]Chowdhury AR, Mandal S, Mittra B, Sharma S, Mukhopadhyay S, Majumder HK. Betulinic acid, a potent inhibitor of eukaryotic topoisomerase I: identification of the inhibitory step, the major functional group responsible and development of more potent derivatives. Med Sci Monit. 2002 Jul;8(7):BR254-65. PMID: 12118187.

[4]Kasperczyk H, La Ferla-Brühl K, Westhoff MA, Behrend L, Zwacka RM, Debatin KM, Fulda S. Betulinic acid as new activator of NF-kappaB: molecular mechanisms and implications for cancer therapy. Oncogene. 2005 Oct 20;24(46):6945-56. doi: 10.1038/sj.onc.1208842. PMID: 16007147.

[5]Gao Y, Ma Q, Ma YB, Ding L, Xu XL, Wei DF, Wei L, Zhang JW. Betulinic acid induces apoptosis and ultrastructural changes in MDA-MB-231 breast cancer cells. Ultrastruct Pathol. 2018 Jan-Feb;42(1):49-54. doi: 10.1080/01913123.2017.1383548. Epub 2017 Dec 1. PMID: 29192840.

[6]Hashimoto F, Kashiwada Y, Cosentino LM, Chen CH, Garrett PE, Lee KH. Anti-AIDS agents--XXVII. Synthesis and anti-HIV activity of betulinic acid and dihydrobetulinic acid derivatives. Bioorg Med Chem. 1997 Dec;5(12):2133-43. doi: 10.1016/s0968-0896(97)00158-2. PMID: 9459011.

[7]Kalra J, Lingaraju MC, Mathesh K, Kumar D, Parida S, Singh TU, Sharma AK, Kumar D, Tandan SK. Betulinic acid alleviates dextran sulfate sodium-induced colitis and visceral pain in mice. Naunyn Schmiedebergs Arch Pharmacol. 2018 Mar;391(3):285-297. doi: 10.1007/s00210-017-1455-3. Epub 2017 Dec 26. PMID: 29279966.