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(Synonyms: 梓醇; Catalpinoside) 目录号 : GN10094

Catalpol是一种在Rehmannia glutinosa中发现的环烯醚萜苷,具有神经保护、抗糖尿病、抗炎、抗氧化和抗病毒等作用。

Catalpol Chemical Structure

Cas No.:2415-24-9

规格 价格 库存 购买数量
20mg
¥714.00
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Sample solution is provided at 25 µL, 10mM.

Description

Catalpol is an iridoid glycoside found in Rehmannia glutinosa, which has neuroprotective, anti-diabetic, anti-inflammatory, antioxidant and antiviral effects[1, 2]. Catalpol can activate AMP-activated protein kinase to regulate lipid metabolism and reduce hepatic steatosis[3].

In vitro, Catalpol (1, 10, 100μM) treatment of human induced pluripotent stem cells (iPSCs) for 24 h increased cell viability in a dose-dependent manner and reduced intracellular lactate dehydrogenase (LDH) levels and lipid peroxidation levels[4]. Catalpol (10μM) treatment of oligodendrocyte precursor cells (OPCs) promoted OPC proliferation, cell migration and differentiation into mature oligodendrocytes[5].

In vivo, Catalpol (5, 10, 20mg/kg) was intraperitoneally injected into gerbils with cerebral ischemia-reperfusion injury for 3 days, which significantly improved the stroke index, significantly increased brain tissue SOD activity, reduced MDA content, and reduced plasma ET-1 content[6]. Catalpol (25-100mg/kg) was injected intraperitoneally into mice with renal ischemia-reperfusion injury, which reduced the blood urea nitrogen and serum creatinine levels, the expression of PI3K, Akt and eNOS, and inhibited the activity of TNF-α, IL-1β, IL-6 and IL-10[7].

References:
[1] Xia Y, Lu Y W, Hao R J, et al. Catalpol relieved angiotensin II-induced blood–brain barrier destruction via inhibiting the TLR4 pathway in brain endothelial cells[J]. Pharmaceutical Biology, 2022, 60(1): 2210-2218.
[2] Bai Y, Zhu R, Tian Y, et al. Catalpol in diabetes and its complications: a review of pharmacology, pharmacokinetics, and safety[J]. Molecules, 2019, 24(18): 3302.
[3] Tian X, Ru Q, Xiong Q, et al. Catalpol attenuates hepatic steatosis by regulating lipid metabolism via AMP‐activated protein kinase activation[J]. BioMed Research International, 2020, 2020(1): 6708061.
[4] Yang L, Feng X, Li Y, et al. Therapeutic efficacy of catalpol against apoptosis in cardiomyocytes derived from human induced pluripotent stem cells[J]. AMB Express, 2020, 10(1): 56.
[5] Yuan C X, Chu T, Liu L, et al. Catalpol induces oligodendrocyte precursor cell-mediated remyelination in vitro[J]. American Journal of Translational Research, 2015, 7(11): 2474.
[6] Liu Y, Li P, Suo J, et al. Catalpol provides protective effects against cerebral ischaemia/reperfusion injury in gerbils[J]. Journal of Pharmacy and Pharmacology, 2014, 66(9): 1265-1270.
[7] Zhu J, Chen X, Wang H, et al. Catalpol protects mice against renal ischemia/reperfusion injury via suppressing PI3K/Akt-eNOS signaling and inflammation[J]. International Journal of Clinical and Experimental Medicine, 2015, 8(2): 2038.

Catalpol是一种在Rehmannia glutinosa中发现的环烯醚萜苷,具有神经保护、抗糖尿病、抗炎、抗氧化和抗病毒等作用[1, 2]。Catalpol能够激活AMP活化蛋白激酶调节脂代谢减轻肝脂肪变性[3]

在体外,Catalpol(1, 10, 100μM)处理人诱导多能干细胞(iPSC)24h,以剂量依赖性方式提高了细胞活力,降低了细胞内乳酸脱氢酶(LDH)水平和脂质过氧化水平[4]。Catalpol(10μM)处理少突胶质细胞前体细胞(OPC),促进了OPC增殖、细胞迁移和分化为成熟的少突胶质细胞[5]

在体内,Catalpol(5, 10, 20mg/kg)通过腹腔注射治疗脑缺血再灌注损伤沙鼠3天,显著改善了卒中指数,显著提高了脑组织SOD活性,降低了MDA含量,降低了血浆ET-1含量[6]。Catalpol(25-100mg/kg)通过腹腔注射治疗肾缺血再灌注损伤小鼠,降低了小鼠的血尿素氮和血清肌酐水平,降低了PI3K、Akt和eNOS的表达,抑制了TNF-α、IL-1β、IL-6和IL-10的活性[7]

实验参考方法

Cell experiment [1]:

Cell lines

Human-induced pluripotent stem cells (iPSCs)

Preparation Method

The study included five groups: Group I, normal control, human iPSCs incubated with dimethyl sulfoxide (DMSO) for 24h; Group II, treatment control, human iPSCs incubated with 8 µM aconitine for 24h; Group III, low-dose treatment, human iPSCs incubated with 8 µM aconitine and 1µM Catalpol for 24h; Group IV, medium-dose treatment, human iPSCs incubated with 8µM aconitine and 10µM Catalpol for 24h; and Group V, high-dose treatment, human iPSCs incubated with 8µM aconitine and 100µM Catalpol for 24h.

Reaction Conditions

1, 10, 100μM; 24h

Applications

Compared with the treatment control group, Catalpol supplementation (1, 10, and 100µM) increased iPSC cell viability by 7.5, 27.3, and 65.8%, respectively; reduced the LDH levels by 10.4, 31.3, and 75.2%, respectively; and reduced the lipid peroxidation levels by 7.7, 33.0, and 62.6%, respectively.

Animal experiment [2]:

Animal models

Mongolian gerbils

Preparation Method

A gerbil model of CI/R was prepared by bilateral common carotid occlusion for 10min followed by 6h reperfusion. Catalpol (5, 10 or 20mg/kg per day) was injected intraperitoneally for 3 days before the carotid occlusion. Stroke index was measured during the reperfusion. The contents of endogenous neuropeptides, endothelin-1 (ET-1) and calcitonin gene-related peptide in plasma were evaluated by radioimmunoassay. Superoxide dismutase (SOD) and malondialdehyde (MDA) in brain tissue homogenate were also examined.

Dosage form

5, 10, 20mg/kg; 3 days; i.p.

Applications

Catalpol significantly improved the stroke index compared with CI/R control group. Catalpol significantly increased the activity of SOD at the doses of 10 and 20mg/kg, decreased the brain MDA content and the plasma level of ET-1 at the doses of 10 and 20mg/kg.

References:
[1] Yang L, Feng X, Li Y, et al. Therapeutic efficacy of catalpol against apoptosis in cardiomyocytes derived from human induced pluripotent stem cells[J]. AMB Express, 2020, 10(1): 56.
[2]Liu Y, Li P, Suo J, et al. Catalpol provides protective effects against cerebral ischaemia/reperfusion injury in gerbils[J]. Journal of Pharmacy and Pharmacology, 2014, 66(9): 1265-1270.

化学性质

Cas No. 2415-24-9 SDF
别名 梓醇; Catalpinoside
化学名 (2S,3R,4S,5S,6R)-2-[[(1aS,1bS,2S,5aR,6S,6aS)-6-hydroxy-1a-(hydroxymethyl)-2,5a,6,6a-tetrahydro-1bH-oxireno[5,6]cyclopenta[1,3-c]pyran-2-yl]oxy]-6-(hydroxymethyl)oxane-3,4,5-triol
Canonical SMILES C1=COC(C2C1C(C3C2(O3)CO)O)OC4C(C(C(C(O4)CO)O)O)O
分子式 C15H22O10 分子量 362.33
溶解度 DMF: 30 mg/ml,DMSO: 30 mg/ml,PBS (pH 7.2): 10 mg/ml 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 2.7599 mL 13.7996 mL 27.5991 mL
5 mM 0.552 mL 2.7599 mL 5.5198 mL
10 mM 0.276 mL 1.38 mL 2.7599 mL
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