Matrine (Matridin-15-one) 是一种在槐属植物中发现的生物碱,可作为kappa阿片受体和u-受体激动剂。Matrine 具有多种药理作用,包括抗癌、抗氧化应激、抗炎和抗凋亡作用,可用于人类非小细胞肺癌、肝癌、甲状腺乳头状癌和急性肾损伤 (AKI) 等疾病的研究。
生物活性 | Matrine (Matridin-15-one) is an alkaloid found inplantsfrom theSophora genusthat can act as akappaopioid receptorandu-receptoragonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lungcancer, hepatoma, papillary thyroidcancerand acute kidney injury (AKI)[1][2][3][4][5]. |
IC50& Target | κ Opioid Receptor/KOR | μ Opioid Receptor/MOR |
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体外研究 (In Vitro) | Matrine (0-1.5 mg/mL, 24-72 h) inhibits the growth of A549 and SMMC-7721 cells[1].Matrine (25 μg/mL, 6 h) suppresses migration of A549 cells[1].Matrine (0-1 mg/mL, 48 h) induces apoptosis by reducing the Bcl-2/Bax protein ratios in A549 and SMMC-7721 cells[1].Matrine (0-1 mg/mL, 48 h) inhibits miR-182-5p expression and induces the apoptosis of PTC cells[2].Matrine (10 μM, 48 h) inhibits cisplatin-induced oxidative injury and inflammation in HK2 cells by reducing ROS level and pro-inflammatory cytokines including IL-1β, IL-6 and TNF-α[4].Matrine (10 μM, 48 h) reverses mitochondrial function in cisplatin-induced HK2 cells by activating the SIRT3/OPA1 pathway[4].Matrine (0-20 nM, 12 h) promotes HepG2 cell apoptosis by inhibiting mitophagy and PINK1/Parkin pathways[5].
Cell Viability Assay[1] Cell Line: | A549, SMMC-7721 cells | Concentration: | 0-500 μg/mL for A549 cells, 0-1.5 mg/mL for SMMC-7721 cells | Incubation Time: | 24-72 h | Result: | Inhibited the growth of A549 and SMMC-7721 cells. |
Western Blot Analysis[1] Cell Line: | A549, SMMC-7721 cells | Concentration: | 100-250 μg/mL for A549 cells, 0.5-1 mg/mL for SMMC-7721 cells | Incubation Time: | 24 h | Result: | Down-regulated the expression of anti-apoptotic protein (Bcl-2) and up-regulated the level of pro-apoptotic protein (bax). |
Immunofluorescence[4] Cell Line: | HK2 cells | Concentration: | 10 μM | Incubation Time: | 48 h | Result: | Increased SIRT3 expression reduced under cisplatin stimuli. |
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体内研究 (In Vivo) | Matrine (Intragastric administration, 40 and 80 mg/kg for 16 consecutive days, xenograft male C57BL/6mice model) inhibits tumors growth and metastasis without affecting the body weight[3].Matrine (Intraperitoneal injections, 5 mg/kg, daily for four continuous days) attenuates renal injury and apoptosis in cisplatin-induced AKI mice, as well as reducing inflammatory responses and activating SIRT3/OPA1 axis and rescues renal mitochondrial dysfunction[4].
Animal Model: | Xenograft male C57BL/6mice model (LLC cells)[3] | Dosage: | 40 and 80 mg/kg for 16 consecutive days | Administration: | Intragastric administration | Result: | Inhibited tumors growth.Decreased the ratio of CD206+/F4/80+, promoted the expression of CD4+and CD8+T cells, and inhibited the expression of Th2 in tumor and spleen tissues. |
Animal Model: | Cisplatin-induced acute kidney injury (AKI) mice model[4] | Dosage: | 5 mg/kg daily for 4 days | Administration: | Intraperitoneal injections | Result: | Attenuated tubular injury observed in AKI mice, including renal tubular necrosis,formation of tubular casts, cytoplasmic vacuoles and renal infiltrationof inflammatory cells in mice.Decreased serum levels of TNF-a and IL-6 and the phosphorylation of NF-κB, activated SIRT3/OPA1 axis and improved mitochondrial function. |
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结构分类 | - Alkaloids
- Piperidine Alkaloids
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来源 | - Plants
- Leguminosae
- Sophora flavescens
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : ≥ 50 mg/mL(201.32 mM) H2O : 20 mg/mL(80.53 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 4.0264 mL | 20.1321 mL | 40.2641 mL | 5 mM | 0.8053 mL | 4.0264 mL | 8.0528 mL | 10 mM | 0.4026 mL | 2.0132 mL | 4.0264 mL |
*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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: PBS Solubility: 37.5 mg/mL (150.99 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (10.07 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.07 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (10.07 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.07 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (10.07 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (10.07 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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