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My CartCAS：472-15-1
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 472-15-1 |
| Name | Betulinic acid |
| Molecular Formula | C30H48O3 |
| Molecular Weight | 456.7 |
| Solubility | Soluble in DMSO ≥10mg/mL |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 207-448-8 |
| MDL | MFCD00009619 |
| SMILES | [H][C@@]12CC[C@@]3(C)[C@]4(C)CC[C@]5(C(O)=O)[C@@]([C@H](C(C)=C)CC5)([H])[C@@](CC[C@@]([H])3[C@@]1(C)CC[C@H](O)C2(C)C)4[H] |
| InChIKey | QGJZLNKBHJESQX-FZFNOLFKSA-N |
| InChI | InChI=1S/C30H48O3/c1-18(2)19-10-15-30(25(32)33)17-16-28(6)20(24(19)30)8-9-22-27(5)13-12-23(31)26(3,4)21(27)11-14-29(22,28)7/h19-24,31H,1,8-17H2,2-7H3,(H,32,33)/t19-,20+,21-,22+,23-,24+,27-,28+,29+,30-/m0/s1 |
| PubChem CID | 64971 |
| Target Point | Topoisomerase |
| Passage | DNA Damage/DNA Repair |
| Background | Betulinic acid is an inhibitor of eukaryotic topoisomerase I (topoisomerase I). |
| Biological Activity | Betulinic acid 是一种天然的五环三萜类化合物，为真核细胞拓扑异构酶 I (topoisomerase I) 的抑制剂，IC50 值为 5 μM，具有抗炎，抗疟疾，抗艾滋病和抗肿瘤等活性。[1-4] |
| IC50 | Topoisomerase I:5μM;HIV-1:1.4μM(EC50)[1-4] |
| In Vitro | 桦木酸是一种真核拓扑异构酶I抑制剂，IC50为5μM，可阻止拓扑异构酶I-DNA的相互作用[1]。在处理24或48小时后，桦木酸(10，20，40，8和160μM)以时间和剂量依赖性方式显著抑制MDA-MB-231细胞活力。桦木酸(20，40μM)导致MDA-MB-231细胞的Bcl-2表达降低。桦木酸还诱导20μM的MDA-MB-231细胞的形态学变化，并导致MDA-MB-231细胞在40μM时的超微结构变化[2]。桦木酸显示出抗HIV活性，在急性感染的H9淋巴细胞中EC50为1.4μM[4]。 |
| In Vivo | 桦木酸(10和30mg/kg，po)显著消除结肠缩短，并降低小鼠中葡聚糖硫酸钠(DSS)诱导的结肠炎中的丙二醛(MDA)和脂质氢过氧化物水平。桦木酸(30mg/kg，po)恢复超氧化物歧化酶(SOD)，过氧化氢酶活性和谷胱甘肽(GSH)含量以控制小鼠DSS诱导的结肠炎中的水平。桦木酸(30mg/kg，口服)也抑制DSS诱导的炎症标志物的增加。桦木酸(3，10，30 mg/kg，po)抑制乙酸诱导的扭体反应和芥子油(MO)诱导的小鼠内脏伤害感受[3]。 |
| Cell Experiment | CCK-8用于测定。 MDA-MB-231细胞在96孔板中以2×103细胞/孔的密度培养，然后用DMSO载体或各种浓度的桦木酸在100μL培养基中处理5μM至160μM，用于指示倍。在处理期后，用110μL含有10μLCCK-8混合物的培养基替换每个孔中的培养基，并将板在37℃温育1小时30分钟。用酶标仪[2]测量波长450nm处的吸光度。 |
| Animal Experiment | 雌性瑞士白化病小鼠口服给予载体(花生油中的5％v/v DMSO)或载体中的桦木酸(3，10或30mg/kg)。 1小时后，通过腹膜内途径给予乙酸(300mg/kg)，并且对治疗无视的观察者计数每只动物的扭体反应次数，持续20分钟。扭曲的反应是当动物的腹部在桌子/地板的表面上摩擦时，身体伸长和后肢伸展[3]。 |
| Data Literature Source | [1]. Chowdhury AR，et al. 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. [2]. Gao Y，et al. Betulinic acid induces apoptosis and ultrastructural changes in MDA-MB-231 breast cancer cells. Ultrastruct Pathol. 2018 Jan-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 Arch Pharmacol. 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 Dec;5(12):2133-43 |
| Unit | Bottle |
| Specification | 100mg 20mg 10mM*1mL in DMSO |
Betulinic acid 是一种真核细胞拓扑异构酶 I (topoisomerase I) 的抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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