Cepharanthine | 千金藤碱

MCE 国际站：Cepharanthine

中文名：千金藤碱

CAS：481-49-2

品牌：MedChemExpress (MCE)

存储条件：Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.

生物活性： Cepharanthine 是从植物 Stephania?cephalantha?Hayata 中分离得到的天然产物。 Cepharanthine 具有抗严重急性呼吸系统综合症冠状病毒 2 (anti-SARS-CoV-2) 活性。 Cepharanthine 具有良好的抑制病毒增殖的效果（半数最大 (50%) 抑制浓度 (IC₅₀) 和 90% 抑制浓度 (IC_{90< /sub>}) 值为 1.90 和 4.46?μM^[1]。

体外：Cepharanthine (CEP) (2 μM，48 小时) 抑制细胞活力和集落形成，并通过线粒体途径诱导人 TNBC 细胞凋亡[2]。 Cepharanthine (2 μM，48 小时) 会损害 MDA-MB-231 细胞中线粒体的功能，导致线粒体分裂和凋亡[2]。 Cepharanthine (5 μM，24 小时) 可增强 K562 细胞 对抗癌剂 Doxorubicin (HY-15142A) 和 Vincristine (HY-N0488) 的敏感性，并可增强抗癌剂诱导下的凋亡[2]。 Cepharanthine (10-50 μM，0.5-1 h) 通过抑制细胞质细胞器的酸化改变了 K562 细胞中 Doxorubicin (HY-15142A) 从细胞质液泡到核质的分布[3]。 Cepharanthine (0-50 μM，30 min) 在体外显示出对人肝细胞色素 P450 酶 CYP3A4，CYP2E1 和 CYP2C9的抑制作用[4]。 Cepharanthine (0-4 μM，48 小时) 阻止恶性疟原虫在环状阶段的发育，对 FCM29，W2，3D7 和 K1 的IC50 分别为 3.059，0.927，2.276 和 1.803 μM[5]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内：Cepharanthine (CEP) (12 mg/kg，腹腔注射，每日 1 次，持续 36 天) 增强 Epirubicin (HY-13624) 在 MDA-MB-231 细胞异种移植物中的治疗效果[2]。 Cepharanthine (10 mg/kg，腹腔注射，单次给药) 通过抑制白细胞活化来预防 LPS 诱导的大鼠肺血管损伤[6]。 Cepharanthine (10 mg/kg，腹腔注射，单次给药) 通过 NF-kB 抑制 LPS 诱导的大鼠全身炎症模型发挥抗炎作用[7]。 Cepharanthine (20-180 mg/kg，腹腔注射) 在小鼠疼痛模型可产生剂量依赖性镇痛作用，ED50 值为 24.5 mg/kg [8]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: MDA-MB-231 cell xenografts in mice[1] Dosage: 12 mg/kg Administration: Intraperitoneal injection (i.p.), once daily for 36 days Result: Combinated with Epirubicin (HY-13624) greatly enhanced the therapeutic efficacy compared with administration of either drug alone. Animal Model: LPS-induced pulmonary vascular injury in male Wistar rats[6] Dosage: 10 mg/kg Administration: Intraperitoneal injection (i.p.), single dose Result: Decreased LPS-induced pulmonary vascular injury. Significantly inhibited the increases in plasma tumor necrosis factor-a (TNF-a) concentrations. Animal Model: LPS-induced Wistar rat model of systemic inflammation[7] Dosage: 10 mg/kg Administration: Intraperitoneal injection (i.p.), single dose Result: Significantly inhibited the increase in LPS-induced IL-6, TNF-α and nitrate/nitrite levels. Reduced interstitial edema and inflammatory cell compared with the control group. Reduced pathologic abnormalities, such as vacuolization, dot necrosis, striped necrosis, and bridging necrosis appeared, and inflammatory cells compared with the control group. group compared with the LPS group. Animal Model: Mice pain models in Kunming (KM) strain male and female mice [8] Dosage: 10 mg/kg Administration: Intraperitoneal injection (i.p.) Result: Resulted in a dose-dependent antinociceptive effect with an ED50 value of 24.5 mg/kg in mice pain models. Significantly decreased the intestinal propulsion with maximal inhibition at 33.6%. Clinical Trial

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研究领域：Anti-infection  |  Metabolic Enzyme/Protease  |  Apoptosis

作用靶点：SARS-CoV  |  Cytochrome P450  |  Apoptosis  |  Parasite

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides

参考文献：[1]. Hijikata A, et al. Evaluating cepharanthine analogues as natural drugs against SARS-CoV-2. FEBS Open Bio. 2022;12(1):285-294

[2]. Shen LW, et.al. Cepharanthine sensitizes human triple negative breast cancer cells to chemotherapeutic agent epirubicin via inducing cofilin oxidation-mediated mitochondrial fission and apoptosis. Acta Pharmacol Sin. 2022 Jan;43(1):177-193.

[3]. Ikeda R, et.al. Cepharanthine potently enhances the sensitivity of anticancer agents in K562 cells. Cancer Sci. 2005 Jun;96(6):372-6. 

[4]. Zhang X, et.al. In vitro inhibitory effects of cepharanthine on human liver cytochrome P450 enzymes. Pharm Biol. 2020 Dec;58(1):247-252.

 [5]. Hua P, et.al. Cepharanthine induces apoptosis through reactive oxygen species and mitochondrial dysfunction in human non-small-cell lung cancer cells. Biochem Biophys Res Commun. 2015 May 1;460(2):136-42. 

[6]. Desgrouas C, et.al. In vitro antiplasmodial activity of cepharanthine. Malar J. 2014 Aug 22;13:327.

 [7]. Murakami K, et.al. The prevention of lipopolysaccharide-induced pulmonary vascular injury by pretreatment with cepharanthine in rats. Am J Respir Crit Care Med. 2000 Jan;161(1):57-63.

 [8]. Wei XY, et,al. Antinociceptive activities and mechanism of action of Cepharanthine. Biochem Biophys Res Commun. 2022 Jul 23;614:219-224.