Alisol B 23-acetate 是口服活性的原萜烷型三萜化合物。Alisol B 23-acetate 可从泽泻中分离。Alisol B 23-acetate 诱导凋亡 (Apoptosis)，促进 ROS 生成，下调 CDK4/6、MMP-2/9，上调 cleaved PARP，激活 FXR 和抑制 Syk。Alisol B 23-acetate 具有抗炎和保肝活性。Alisol B 23-acetate 保护肾脏免受缺血-再灌注损伤。Alisol B 23-acetate 对卵巢癌、结肠癌、肺癌、胃癌具有抗癌活性。Alisol B 23-acetate 可用于动脉粥样硬化和过敏性哮喘研究。
Alisol B 23-acetate is an orally active prototerpane-type triterpenoid. Alisol B 23-acetate can be isolated from Alisma orientalis. Alisol B 23-acetate induces Apoptosis, promotes ROS generation, downregulates CDK4/6, MMP-2/9, upregulates cleaved PARP, activates FXR and inhibits Syk. Alisol B 23-acetate has anti-inflammatory and hepatoprotective activities. Alisol B 23-acetate protects the kidney from ischemia-reperfusion injury. Alisol B 23-acetate has anticancer activity against ovarian cancer, colon cancer, lung cancer, and gastric cancer. Alisol B 23-acetate can be used in the study of atherosclerosis and allergic asthma[1][2][3][4][5][6][7][8][9][10][11][12][13][14].
Antiplasmodial activity against Plasmodium falciparum K1 infected in human erythrocyte assessed as inhibition of parasite growth incubated for 72 hrs by [3H]-hypoxanthine incorporation based liquid scintillation counting method
Antiplasmodial activity against Plasmodium falciparum K1 infected in human erythrocyte assessed as inhibition of parasite growth incubated for 72 hrs by [3H]-hypoxanthine incorporation based liquid scintillation counting method
Downregulated protein levels of CDK4, CDK6, cyclin D1, MMP-2, MMP-9.
Upregulated Bax/Bcl-2 ratio and cleaved PARP expression.
体内研究 (In Vivo)
Alisol B 23-acetate (2.56 mg/kg；口服；每日一次；90 天) 可激活卵巢切除的 LDLR-/- 小鼠的肝脏 FXR-BSEP 信号传导，增加粪便胆固醇和胆汁酸排泄，减少肝脏脂质沉积，并改善动脉粥样硬化病变[5]。
Alisol B 23-acetate (50-100 mg/kg；口服）可抑制 ICR 小鼠被动皮肤过敏 (PCA) 模型中 IgE 介导的血管通透性和耳肿胀[7]。
Alisol B 23-acetate (15-30 mg/kg；口服；每日一次；9 周) 可降低 ApoE-/- 动脉粥样硬化小鼠血清甘油三酸酯 (TG)、白细胞介素-12 (IL-12)、IFN-γ，升高高密度脂蛋白胆固醇 (HDL-C)，并促进主动脉胆固醇外排基因表达[8]。
Alisol B 23-acetate (10-40 mg/kg；口服；30 天) 可抑制 TLR4/NOX2 通路，减少 LPS 诱导的心脏功能障碍小鼠的心肌炎症和活性氧 (ROS) 生成[9]。
Alisol B 23-acetate (15-60 mg/kg；口服；每日；4 周) 可改善 MCD 诱导的 NASH 小鼠的肝脏脂肪变性、炎症和纤维化，并激活 FXR 靶基因[10]。
Alisol B 23-acetate (12.5-50 mg/kg；口服；每日一次；连用7天）可通过激活法尼醇 X 受体促进小鼠部分肝切除术后的肝脏再生[11]。
Alisol B 23-acetate (10-40 mg/kg；口服；每日一次；7 天) 以剂量依赖性方式减轻 CCl4 (HY-Y0298) 诱发的肝损伤小鼠的肝毒性[12]。
Alisol B 23-acetate (60 mg/kg；腹腔注射；致敏/激发前 30 min) 可降低 OVA 诱发的过敏性哮喘 BALB/c 小鼠的气道高反应性，并降低支气管肺泡灌洗液中的 IL-13 和嗜酸性粒细胞[14]。
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Adult male C57BL/6 mice (6-8 weeks old), LPS-induced sepsis model[9].
Dosage:
10 mg/kg, 20 mg/kg, 40 mg/kg
Administration:
Gavage (p.o.), 30 days
Result:
Significantly improved the 48-hour survival rate of LPS-induced septic mice (80% in the 40 mg/kg group vs. 40% in the LPS group).
Restored left ventricular ejection fraction (LVEF), left ventricular fraction shortening (LVFS), and reduced left ventricular end-systolic diameter (LVESD) in LPS-treated mice.
Reduced inflammatory cell infiltration in myocardial tissue.
Decreased serum levels of TNF-α, IL-6, and IL-1β.
Downregulated TLR4, NOX2, p-P38, and p-ERK protein expression in myocardial tissue.
Animal Model:
Male C57BL/6 mice (8-9 weeks old) with CCl₄-induced acute hepatotoxicity[12]
Dosage:
10 mg/kg, 20 mg/kg, 40 mg/kg
Administration:
Oral gavage; once daily; for 7 days
Result:
Significantly reduced serum ALT and AST activities, decreased hepatic and serum total bile acid levels, ameliorated liver histopathological changes (e.g., congestion, vacuolization, necrosis), reduced TUNEL-positive apoptotic hepatocytes.
Increased BrdU-positive proliferating hepatocytes and mitotic index, upregulated FXR target genes (FoxM1b, Cyclin D1, Cyclin B1, Bsep, Mrp2, Shp), and downregulated Ntcp, Cyp7a1, and Cyp8b1 expression. Enhanced STAT3 phosphorylation and upregulated anti-apoptotic genes (Bcl-xl, SOCS3).
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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