Worenine是一种从黄连中分离的异喹啉类生物碱。
Cas No.:38763-29-0
Sample solution is provided at 25 µL, 10mM.
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Worenine is an isoquinoline alkaloid isolated from Coptis chinensis[1-2]. Worenine acts as a JNK2 kinase inhibitor to suppress related signaling pathway activation, while also reducing oxidative stress and inflammatory responses by activating the Nrf2 pathway. Worenine can be used in research related to psoriasis and cancer[3-4].
In vitro, Worenine (0-128μM) was used to treat MDA-MB-231 and MDA-MB-468 breast cancer cell lines for 48 hours. Worenine significantly inhibited the expression of the RNF130 protein and induced apoptosis[5]. Worenine (5–20μM) was used to treat HCT116 and SW620 colorectal cancer cell lines for 24–72 hours. Worenine significantly inhibited cancer cell viability and colony formation, induced cell cycle arrest, downregulated the expression of key glycolytic enzymes, and inhibited glucose uptake, consumption, and lactate production[6].
In vivo, a Balb/c mouse model was topically pretreated with Worenine cream (2mM) 3 hours before the back was irradiated with SUV (100KJ/m²) for 2 hours. Worenine significantly inhibited skin epidermal thickening, edema, and immune cell infiltration, while also reducing IL-6 secretion and JNK phosphorylation levels in the skin[7]. ICR mice were intraperitoneally administered Worenine (5mg/kg/day) for 15 consecutive days. Worenine showed significant accumulation in the liver and induced hepatotoxicity, leading to histopathological changes in the liver including fat vacuole infiltration, inflammation, and deep staining of some hepatocytes[8].
References:
[1] Wang Y, Hu Y, Wu T, et al. Recognition of DNA abasic site nanocavity by fluorophore-switched probe: Suitable for all sequence environments. Spectrochim Acta A Mol Biomol Spectrosc. 2016 Jan 15;153:645-50.
[2] Ishaq AR, Younis T, Lin S, et al. Phosphofructokinase-1 in Cancer: A Promising Target for Diagnosis and Therapy. Recent Pat Anticancer Drug Discov. 2025;20(5):667-680.
[3] Lu H, Huang Y, Ni X, et al. TOPK promotes the development of psoriasis and worenine alleviates psoriasiform dermatitis by inhibiting TOPK activity. J Eur Acad Dermatol Venereol. 2024 May;38(5):851-863.
[4] Yang G, Xu M, Wu M, et al. Worenine enhances the sensitivity of non-small cell lung cancer A549/DDP cells to cisplatin via HIF-1α/BNIP3-mediated mitophagy. Gen Physiol Biophys. 2025 Jul;44(4):317-326.
[5] Hu M, Huang L, Deng H, et al. Single-cell transcriptomics uncover RNF130-mediated TNF-α pathway activation and worenine synergy with paclitaxel in breast cancer. Clin Epigenetics. 2026 Jan 24;18(1):32.
[6] Ji L, Shen W, Zhang F, et al. Worenine reverses the Warburg effect and inhibits colon cancer cell growth by negatively regulating HIF-1α. Cell Mol Biol Lett. 2021 May 18;26(1):19.
[7] Xiao J, Lu H, Ma T, et al. Worenine Prevents Solar Ultraviolet-Induced Sunburn by Inhibiting JNK2. Front Pharmacol. 2022 Jul 22;13:881042.
[8] Zhang H, Luo J, Yi Y, et al. Organic cation transporter 1 and cytochrome P450s play crucial roles in coptisine- and worenine-induced hepatotoxicity. Drug Metab Dispos. 2025 Sep;53(9):100134.
Worenine是一种从黄连中分离的异喹啉类生物碱[1-2]。Worenine可作为JNK2激酶抑制剂来抑制相关信号通路活化，同时通过激活Nrf2通路以减少氧化应激和炎症反应。Worenine可用于银屑病和癌症的相关研究[3-4]。
在体外，Worenine（0-128μM）处理MDA-MB-231及 MDA-MB-468乳腺癌细胞系48小时。Worenine显著抑制RNF130蛋白的表达，同时诱导细胞凋亡[5]。Worenine（5–20μM）处理HCT116和SW620结直肠癌细胞系24–72小时。Worenine显著抑制癌细胞活力与集落形成，引起细胞周期阻滞，同时下调糖酵解关键酶表达并抑制葡萄糖摄取、消耗和乳酸生成[6]。
在体内，Worenine（2mM；乳膏局部涂抹）于SUV照射前3小时预处理Balb/c小鼠，随后以100KJ/m² SUV照射背部2小时。Worenine显著抑制了皮肤表皮增厚、水肿及免疫细胞浸润，同时降低了皮肤中IL-6的分泌和JNK的磷酸化水平[7]。Worenine（5mg/kg/day；腹腔注射）连续处理15天，用于ICR小鼠。Worenine在肝脏中表现出显著的蓄积，诱导了肝毒性，导致肝脏出现脂肪空泡浸润、炎症和部分肝细胞深染等组织病理学改变[8]。
| Cell experiment [1]: | |
Cell lines | HCT116 and SW620 human colorectal cancer cell lines, and FHC normal human colon cell line |
Preparation Method | HCT116 and SW620 cells were maintained in RPMI 1640 medium supplemented with 10% fetal bovine serum (FBS). FHC cells were maintained in DMEM/F12 medium supplemented with 10% FBS. All cells were incubated at 37°C with 5% CO₂. Cells were treated with Worenine (5–20μM) for 24 to 72 hours. |
Reaction Conditions | 5–20μM; 24–72h. |
Applications | Worenine significantly inhibited the viability and colony formation of HCT116 and SW620 cells, and induced G2/M phase cell cycle arrest. Worenine also suppressed the Warburg effect, as evidenced by significantly reduced glucose uptake, glucose consumption, and lactate production. Worenine downregulated the expression of key glycolytic enzymes (GLUT3, HK2, PFK-L, PKM2, LDHA) and promoted HIF-1α protein degradation. No significant cytotoxic effect was observed on normal FHC cells. |
| Animal experiment [2]: | |
Animal models | ICR mice |
Preparation Method | Mice were intraperitoneally administered Worenine (5mg/kg/day) for 15 consecutive days. Blood and liver samples were collected for analysis. |
Dosage form | 5mg/kg/day; i.p.; for 15 days. |
Applications | Worenine administration induced significant hepatotoxicity, evidenced by increased plasma alanine aminotransferase (ALT) and carboxylesterase 1 (CE1) activities. Histopathological evaluation revealed liver abnormalities including fat vacuole infiltration, inflammation, and deep staining of some hepatocytes. Worenine showed significant accumulation in the liver. |
References: | |
| Cas No. | 38763-29-0 | SDF | |
| 别名 | 甲基黄连碱 | ||
| Canonical SMILES | CC1=C2C(C=C3OCOC3=C2)=C[N+]4=C1C(C(CC4)=C5)=CC6=C5OCO6 | ||
| 分子式 | C20H16NO4 | 分子量 | 334.34 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C,protect from light |
| 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 | 2.991 mL | 14.9548 mL | 29.9097 mL |
| 5 mM | 598.2 μL | 2.991 mL | 5.9819 mL |
| 10 mM | 299.1 μL | 1.4955 mL | 2.991 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 | ||||||||||
| 计算重置 | ||||||||||
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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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