Betulinic-acid-Lupatic-acid-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBetulinic acidCat. No.: HY-10529CAS No.: 472-15-1Synonyms: Lupatic acid; Betulic acid分式: CHO分量: 456.7作靶點(diǎn): Apoptosis; Topoisomerase; HIV; Autophagy; Mitophagy作通路: Apoptosis; Cell Cycle/DNA Damage; Anti-infection; Autophagy儲存式: 4C

2、, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實驗 DMSO : 60 mg/mL (131.38 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.47 mM); Suspended solution; Need ultrasonic2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubi

3、lity: 2.5 mg/mL (5.47 mM); Suspended solution; Need ultrasonic3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (5.47 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Betulinic acid種天然的五環(huán)三萜類化合物，為真核細(xì)胞拓?fù)洚悩?gòu)酶 I (topoisomerase I) 的抑制劑，IC50值為 5 M，具有抗炎，抗瘧疾，抗

4、艾滋病和抗腫瘤等活性。IC50 & Target Topoisomerase I HIV-15 M (IC50) 1.4 M (EC50)體外研究 Betulinic acid is a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 M, and prevents topoisomerase I-DNA interaction 1. Betulinic acid (10, 20, 40, 80, and 160 M) significantly suppresses MDA-MB-231 cellviability in a t

5、ime- and dose-dependent manner after treatment for 24 or 48 h. Betulinic acid (20, 40 M)causes decrease in Bcl-2 expression of MDA-MB-231 cells. Betulinic acid also induces morphologicalchanges of MDA-MB-231 cells at 20 M, and leads to ultrastructure changes of MDA-MB-231 cells at 40 M2. Betulinic a

6、cid shows anti-HIV activities, with an EC50 of 1.4 M in acutely infected H9 lymphocytes 4.體內(nèi)研究 Betulinic acid (10 and 30 mg/kg, p.o.) significantly abrogates colon shortening, and reduces malondialdehyde(MDA) and lipid hydroperoxide levels in dextran sulfate sodium (DSS)-induced colitis in mice. Bet

7、ulinic acid(30 mg/kg, p.o.) restores superoxide dismutase (SOD), catalase activity and glutathione (GSH) content tocontrol levels in DSS-induced colitis in mice. Betulinic acid (30 mg/kg, p.o.) also inhibits the DSS-inducedincrease in inflammatory markers. Betulinic acid (3, 10, 30 mg/kg, p.o.) supp

8、resses acetic acid-inducedwrithing responses and mustard oil (MO)-induced visceral nociception in mice 3.PROTOCOLCell Assay 2 CCK-8 is used in the assay. MDA-MB-231 cells are cultured in 96-well plates at a density of 2 103cells/well and then treated with DMSO vehicle or various concentrations of Be

9、tulinic acid ranging from 5 Mto 160 M in 100 L of medium for the indicated times. After the treatment period, the medium in each well isreplaced with 110 L of medium containing 10 L of the CCK-8 mixture, and the plates are incubated for 1 hand 30 min at 37C. The absorbance at a wavelength of 450 nm

10、is measured with a microplate reader 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Female Swiss albino mice are administered vehicle (5% v/v DMSO in peanut oil) or Betulinic acid (3, 10 or 30Administration 3 mg/kg) in vehicle, orally. After 1

11、 h, acetic acid (300 mg/kg) is administered by intraperitoneal route andnumber of writhing response of each animal is counted for 20 min by an observer who is blind to thetreatments. Writhing response is when animal rubs its abdomen on surface of table/floor with elongation ofthe body and extension

12、of the hind limbs 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn)2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE Green Chem. 2019 May. Fuel. 2018 Dec 15, 234:110-119. J Mol Med (Berl). 2019 Jun 14. Microb Cell Fact. 2019 May 3;18(1):77.S

13、ee more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Chowdhury AR, et al. Betulinic acid, a potent inhibitor of eukaryotic topoisomerase I: identification of the inhibitory step, the majorfunctional group responsible and development of more potent derivatives. Med Sci Monit. 2002 Jul

14、;8(7):BR254-65.2. Gao Y, et al. Betulinic acid induces apoptosis and ultrastructural changes in MDA-MB-231 breast cancer cells. Ultrastruct Pathol. 2018Jan-Feb;42(1):49-54.3. Kalra J, et al. Betulinic acid alleviates dextran sulfate sodium-induced colitis and visceral pain in mice. Naunyn Schmiedebergs ArchPharmacol. 2017 Dec 26.4. Hashimoto F, et al. Anti-AIDS agents-XXVII. Synthesis and anti-HIV activity of betulinic acid and dihydrobetulinic acid derivatives.Bioorg Med Chem. 1997