Lamivudine
(Synonyms: 拉米夫定; BCH-189) 目录号 : GC10317
Lamivudine是一种口服核苷类似物，作为核苷类逆转录酶抑制剂，抗乙肝病毒（HBV）活性的EC50值为0.07±0.02μg/ml。
Cas No.:134678-17-4
Sample solution is provided at 25 µL, 10mM.
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Lamivudine is an oral nucleoside analogue, which acts as the nucleoside reverse transcriptase inhibitor, with an EC50 of 0.07±0.02μg/ml for anti-hepatitis B virus (HBV) activity[1]. Lamivudine undergoes anabolic phosphorylation by intracellular kinases to form Lamivudine 5′-triphosphate, the active anabolite which prevents HIV-1 and HBV replication by competitively inhibiting viral reverse transcriptase and terminating proviral DNA chain extension [2]. Lamivudine has been used in viral and antitumor studies in various cell and animal models[3].
In vitro, Lamivudine treatment at 300μM in HepG2.2.15 cells for 72 hours significantly reduced the expression of MMP-9, HBsAg, HBeAg, and inhibited the replication of HBV[4]. Treatment of 4μg/ml Lamivudine for 6 days significantly inhibted SDAU1005 virus replication in chick embryo fibroblasts (CEFs) without affecting cell viability[5]. Lamivudine treatment with 500μM for 8 days can stimulate the proliferation of dendritic cells (DC) derived from patients with chronic hepatitis B (CHB), promote the secretion of IL-12 and IL-6, and restore cellular immune function[6].
In vivo, Lamivudine treatment via daily gastric infusion (100mg/kg) in senescence-accelerated mouse prone 8 (SAMP8) mice for 4 weeks significantly improved the ageing status of the mice and alleviated the decline in cognitive ability[7]. Oral administration of 2mg/kg Lamivudine daily for one week reduced the severity of gastric ulcers in a mouse model of ethanol-induced gastric ulcers, and improved the histological features of the gastric mucosa and maintained the integrity of the gastric mucosal barrier[8].
References:
[1] Ying, Clercq D, Neyts. Lamivudine, adefovir and tenofovir exhibit long‐lasting anti‐hepatitis B virus activity in cell culture[J]. Journal of viral hepatitis, 2000, 7(1): 79-83.
[2] Perry C M, Faulds D. Lamivudine: a review of its antiviral activity, pharmacokinetic properties and therapeutic efficacy in the management of HIV infection[J]. Drugs, 1997, 53(4): 657-680.
[3] Johnson M A, Moore K H P, Yuen G J, et al. Clinical pharmacokinetics of lamivudine[J]. Clinical pharmacokinetics, 1999, 36(1): 41-66.
[4] Zhang J, Yu H, Sun F Y, et al. Effects of lamivudine on cell proliferation of liver cancer and expressions of HBsAg, HBeAg, and MMP-9 in patients[J]. Eur. Rev. Med. Pharmacol. Sci, 2019, 23: 9093-9098.
[5] Wang Y, Xu S, Li S, et al. Lamivudine inhibits the replication of ALV-J associated acutely transforming virus and its helper virus and tumor growth in vitro and in vivo[J]. Frontiers in Microbiology, 2015, 6: 1306.
[6] Zheng P Y, Zhang D Y, Lu G F, et al. Effects of lamivudine on the function of dendritic cells derived from patients with chronic hepatitis B virus infection[J]. World Journal of Gastroenterology: WJG, 2007, 13(34): 4641.
[7] Li M, Zhao J, Tang Q, et al. Lamivudine improves cognitive decline in SAMP8 mice: Integrating in vivo pharmacological evaluation and network pharmacology[J]. Journal of Cellular and Molecular Medicine, 2021, 25(17): 8490-8503.
[8] Meng X, Liu J, Kang J, et al. Lamivudine protects mice from gastric ulcer by activating PGK1 to suppress ferroptosis[J]. Biochemical Pharmacology, 2024, 227: 116440.
Lamivudine是一种口服核苷类似物，作为核苷类逆转录酶抑制剂，抗乙肝病毒（HBV）活性的EC50值为0.07±0.02μg/ml[1]。Lamivudine通过细胞内激酶发生磷酸化生成活性代谢物拉米夫定三磷酸酯，可竞争性抑制病毒逆转录酶并终止前病毒DNA链延伸，从而阻止HIV-1和HBV复制[2]。Lamivudine已广泛应用于多种细胞和动物模型的病毒及抗肿瘤研究[3]。
在体外，300μM的Lamivudine处理HepG2.2.15细胞72小时可显著降低MMP-9、HBsAg和HBeAg表达，并抑制HBV复制[4]。4μg/ml的Lamivudine处理鸡胚成纤维细胞（CEFs）6天能显著抑制SDAU1005病毒复制且不影响细胞活力[5]。500μM的Lamivudine处理慢性乙肝（CHB）患者来源的树突状细胞（DC）8天可刺激细胞增殖，促进IL-12和IL-6分泌，恢复细胞免疫功能[6]。
在体内，加速衰老SAMP8小鼠经每日胃灌注Lamivudine（100mg/kg，持续4周）后，小鼠的衰老状态显著改善且认知能力下降缓解[7]。乙醇诱导胃溃疡小鼠模型每日口服2mg/kg剂量的Lamivudine（持续1周）可减轻溃疡严重程度，改善胃黏膜组织学特征并维持胃黏膜屏障完整性[8]。
| Cell experiment [1]: | |
Cell lines | HepG2.2.15 cells |
Preparation Method | The HepG2.2.15 cells were cultured with a culture solution of 10% fetal bovine serum in a 37°C incubator with 5% CO2 concentration. They were washed with PBS after 85% of the cells were attached. Then the cells were digested with 1ml of 25% trypsin, and cultured with a concentration of 10% in a culture solution for 48h at 37°C with 5% CO2 concentration for subculture. The cells and supernatants were collected after 72h of Lamivudine intervention (100, 200, and 300μM). The cells were digested with trypsin and centrifuged at 8000r/min for 3min. The supernatant was then discarded, and the cells were collected and resuspended with 200μL of PBS before the detection. The MMP-9, HBsAg, and HBeAg levels were detected using ELISA method. |
Reaction Conditions | 100, 200, and 300μM; 72h |
Applications | Lamivudine treatment significantly inhibited the MMP-9, HBsAg, and HBeAg levels in dose-dependent manner within HepG2.2.15 cells. |
| Animal experiment [2]: | |
Animal models | Kunming mice |
Preparation Method | Healthy male Kunming mice, 4 weeks old (20±2g), were housed in appropriate cages and allowed to adapt to the laboratory environment for one week. The environmental temperature was maintained at 25°C, and the daily light-dark cycle was 12 hours. The animals had free access to water and standard feed pellets. The mice were randomly divided into 4 groups (n = 8). The control group (Control) and the ethanol group (Ethanol) were given 0.9% physiological saline (1mL/100g/day); the positive drug group (CIM) was orally administered cimetidine (80mg/kg/day); the Lamivudine group was orally administered 2mg/kg/day of Lamivudine. The mice were treated continuously for 1 week. Approximately 2 hours after the last administration, the mice were fasted for 24 hours without restricting water intake. The mice in the ethanol group, the ethanol + CIM group, and the ethanol + Lamivudine (2mg/kg) group (1mL/100g body weight) were intragastrically administered anhydrous ethanol. Meanwhile, the remaining mice were intragastrically administered the same volume of physiological saline. 2 hours later, the mice were dislocated at the cervical vertebra and sacrificed, and the gastric tissues were collected for further biochemical and histopathological examinations. |
Dosage form | 2mg/kg/day for 7 days; p.o. |
Applications | Lamivudine treatment improved histopathological features of gastric mucosa in mice under ethanol stress. |
References: | |
| Cas No. | 134678-17-4 | SDF | |
| 别名 | 拉米夫定; BCH-189 | ||
| 化学名 | 4-amino-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one | ||
| Canonical SMILES | C1C(OC(S1)CO)N2C=CC(=NC2=O)N | ||
| 分子式 | C8H11N3O3S | 分子量 | 229.26 |
| 溶解度 | ≥ 10.5mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 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。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.3619 mL | 21.8093 mL | 43.6186 mL |
| 5 mM | 872.4 μL | 4.3619 mL | 8.7237 mL |
| 10 mM | 436.2 μL | 2.1809 mL | 4.3619 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
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Quality Control & SDS
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- Purity: >98.00%
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