Rehmapicroside
(Synonyms: 地黄苦苷) 目录号 : GC60319
Rehmapicroside是从Rehmannia glutinosa的根茎中分离的紫罗兰酮糖苷,具有抗肿瘤、抗氧化、抗炎和神经保护等活性。
Cas No.:104056-82-8
Sample solution is provided at 25 µL, 10mM.
Rehmapicroside is an ionone glycoside isolated from the rhizome of Rehmannia glutinosa, which has antitumor, antioxidant, anti-inflammatory and neuroprotective activities[1, 2, 3].
In vitro, Rehmapicroside (0-100μM) treatment of hepatocellular carcinoma (HCC) cell lines (HepG2, SNU-739 cells) for 24h inhibited cell proliferation in a dose-dependent manner, inhibited cell migration and invasion, induced cell G2/M phase arrest, and had no toxicity to normal cells[4]. Rehmapicroside (12.5-100μM) treatment of PC12 cells cultured under oxygen-glucose deprivation and reoxygenation (OGD/RO) conditions for 24h increased cell viability in a dose-dependent manner, reduced intracellular O2− and ONOO−, upregulated the expression of Bcl-2 but downregulated the expression of Bax and Caspase-3, and reduced the ratio of LC3-II to LC3-I[5].
In vivo, Rehmapicroside (10mg/kg) was intraperitoneally injected into rats that underwent middle cerebral artery occlusion (MCAO) surgery, which reduced the area of cerebral infarction, improved the neurological deficit score, and inhibited the formation of 3-nitrotyrosine, Drp1 nitration, and the expression of NADPH oxidase and iNOS in the rat brain tissue[5].
References:
[1] Anh N T H, Sung T V, Franke K, et al. Phytochemical studies of Rehmannia glutinosa rhizomes[J]. Die Pharmazie-An International Journal of Pharmaceutical Sciences, 2003, 58(8): 593-595.
[2] Zhao L, Cai R. Cracking the Bioactive Code of Rehmannia glutinosa: Analysis and Functions of Active Components[J]. Biological Evidence, 2024, 14.
[3] Zhang R X, Li M X, Jia Z P. Rehmannia glutinosa: review of botany, chemistry and pharmacology[J]. Journal of ethnopharmacology, 2008, 117(2): 199-214.
[4] Zhao X, Bai Z, Song Y. Targeting suppression of AKT activation boosts chemosensitivity of hepatocarcinoma cells via regulation of inflammation and metastasis: Functional protection of Rehmapicroside[J]. Journal of Functional Foods, 2024, 122: 106487.
[5] Zhang Y, He Y, Wu M, et al. Rehmapicroside ameliorates cerebral ischemia-reperfusion injury via attenuating peroxynitrite-mediated mitophagy activation[J]. Free Radical Biology and Medicine, 2020, 160: 526-539.
Rehmapicroside是从Rehmannia glutinosa的根茎中分离的紫罗兰酮糖苷,具有抗肿瘤、抗氧化、抗炎和神经保护等活性[1, 2, 3]。
在体外,Rehmapicroside(0-100μM)处理肝细胞癌(HCC)细胞系(HepG2、SNU-739细胞)24h,以剂量依赖性方式抑制了细胞增殖,抑制了细胞的迁移和侵袭,诱导了细胞G2/M期阻滞,对正常细胞无毒性[4]。Rehmapicroside(12.5-100μM)处理氧糖剥夺再氧合(OGD/RO)条件培养的PC12细胞24h,以剂量依赖性方式提高了细胞活力,降低了细胞内O2−和 ONOO−,上调了Bcl-2 但下调了Bax、Caspase-3的表达,降低了LC3-II与LC3-I的比率[5]。
在体内,Rehmapicroside(10mg/kg)通过腹腔注射治疗经过大脑中动脉闭塞(MCAO)手术处理的大鼠,减少了大鼠的脑梗死面积,改善了神经功能缺损评分,抑制了大鼠脑组织中3-硝基酪氨酸的形成、Drp1硝化以及NADPH氧化酶和iNOS的表达[5]。
Cell experiment [1]: | |
Cell lines | HepG2、SNU-739 cells |
Preparation Method | HepG2 and SNU-739 cells were incubated with 0-100μM Rehmapicroside, cisplatin (cDDP) alone, or the two in combination at the indicated concentrations for 24h. Then, all cells were collected for cell viability calculation using CCK-8 analysis. |
Reaction Conditions | 0-100μM; 24h |
Applications | Rehmapicroside inhibits the proliferation of Hepatocellular carcinoma (HCC) cells in a dose-dependent manner. |
Animal experiment [2]: | |
Animal models | Sprague-Dawley (SD) rats |
Preparation Method | Experimental Groups and Drug TreatmentRats were randomly divided into following groups including sham control, shamcontrol plus Rehmapicroside (10mg/kg), middle cerebral artery occlusion (MCAO), MCAO plus Rehmapicroside (2.5, 5, 10mg/kg wt) and MCAO plus FeTMPyP (peroxynitrite decomposition catalyst, PDC) (3mg/kg). Rehmapicroside was injected into the peritoneum at the beginning of reperfusion after 2h of MCAO ischemia. FeTMPyP (3mg/kg wt) was used as positivecontrol. Both Rehmapicroside and PDC dissolved in saline at designed dosages wereintraperitoneally administrated into the rats at the onset of reperfusion. The volumefor the injection treatment was 5mL/kg. In a parallel experiment, the same volume of saline was used as a control. |
Dosage form | 2.5, 5, 10mg/kg; i.p. |
Applications | Rehmapicroside alleviates mitophagy activation and apoptosis in MCAO ischemia-reperfused rats. Rehmapicroside suppresses 3-nitrotyrosine formation, Drp1 nitration as well as NADPH oxidases and iNOS expression in MCAO ischemia-reperfused rat brains. |
References: |
Cas No. | 104056-82-8 | SDF | |
别名 | 地黄苦苷 | ||
Canonical SMILES | CC([C@]1([H])O[C@@H]2O[C@@H]([C@@H](O)[C@H](O)[C@H]2O)CO)=C(C(C)(C)CC1)C(O)=O | ||
分子式 | C16H26O8 | 分子量 | 346.37 |
溶解度 | 储存条件 | Store at 2-8°C,protect from light | |
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1 mg | 5 mg | 10 mg |
1 mM | 2.8871 mL | 14.4354 mL | 28.8709 mL |
5 mM | 0.5774 mL | 2.8871 mL | 5.7742 mL |
10 mM | 0.2887 mL | 1.4435 mL | 2.8871 mL |
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