Carbidopa (hydrate)是一种aryl hydrocarbon receptor (AhR)激动剂，可抑制胰腺癌细胞和肿瘤的生长。
Cas No.:38821-49-7
Sample solution is provided at 25 µL, 10mM.
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Carbidopa (hydrate) is an aryl hydrocarbon receptor (AhR) agonist that inhibits pancreatic cancer cell and tumor growth [1]. Carbidopa can block the conversion of levodopa to dopamine in the periphery, enabling greater availability of dopamine to the central nervous system as well as minimizing the peripheral side effects of dopamine [2]. Carbidopa has been widely used to improve neurodegenerative diseases and promote the proteasomal degradation of androgen receptor (AR) protein[3].
In vitro, Carbidopa treatment for 72 hours significantly reduced the viability of NCI-H146, NCI-H209 and NCI-H727 cells, with IC50 values of 12, 22 and 29μM, respectively[4]. Treatment with 1mM Carbidopa for 24 hours significantly reduced the expression of IDO1 mRNA and IDO1 protein in BxPC-3 cells[5]. Treatment with 300μM Carbidopa for 24 hours significantly reduced the mitochondrial membrane potential of MDA-MB-231 cells, leading to mitochondrial dysfunction and cell damage[6].
In vivo, Carbidopa treatment via intraperitoneal injection at a dose of 7.5mg/kg), twice a day for 14 days, significantly inhibited tumor growth in a MCF7 cell-xenograft mouse model, and led to an increase in CYP1A1 protein and a decrease in ERα protein in the tumor tissue[7]. Daily intraperitoneal injection of Carbidopa (25mg/kg) was administered for 11 weeks, which significantly inhibited tumor growth in a xenograft mouse model of LNCaP cells and suppressed the production of serum prostate-specific antigen (PSA)[8].
References:
[1] Safe S. Carbidopa: a selective Ah receptor modulator (SAhRM)[J]. Biochemical Journal, 2017, 474(22): 3763-3765.
[2] Lenka A, Vernino S. Carbidopa: beyond Parkinson’s disease[J]. Clinical Autonomic Research, 2025, 35(3): 347-352.
[3] Chen Z, Cai A, Zheng H, et al. Carbidopa suppresses prostate cancer via aryl hydrocarbon receptor-mediated ubiquitination and degradation of androgen receptor[J]. Oncogenesis, 2020, 9(5): 49.
[4] Gilbert J A, Frederick L M, Pobst L J, et al. Hydrogen peroxide degradation and selective carbidopa-induced cytotoxicity against human tumor lines[J]. Biochemical pharmacology, 2005, 69(8): 1159-1166.
[5] Korac K, Rajasekaran D, Sniegowski T, et al. Carbidopa, an activator of aryl hydrocarbon receptor, suppresses IDO1 expression in pancreatic cancer and decreases tumor growth[J]. Biochemical Journal, 2022, 479(17): 1807-1824.
[6] Actis Dato A B, Naso L G, Martínez V R, et al. Carbidopa and ZnCarbidopa Induce Reductive Stress in MDA‐MB‐231 Cells[J]. ChemPlusChem, 2025, 90(3): e202400596.
[7] Chen Z, Xia X, Chen H, et al. Carbidopa suppresses estrogen receptor-positive breast cancer via AhR-mediated proteasomal degradation of ERα[J]. Investigational New Drugs, 2022, 40(6): 1216-1230.
[8] Wafa L A, Cheng H, Plaa N, et al. Carbidopa abrogates L‐dopa decarboxylase coactivation of the androgen receptor and delays prostate tumor progression[J]. International journal of cancer, 2012, 130(12): 2835-2844.
Carbidopa (hydrate)是一种aryl hydrocarbon receptor (AhR)激动剂，可抑制胰腺癌细胞和肿瘤的生长[1]。Carbidopa能阻断左旋多巴在外周转化为多巴胺，使多巴胺更多地进入中枢神经系统，同时最大限度地减少多巴胺的外周副作用[2]。Carbidopa已被广泛用于改善神经退行性疾病，并促进雄激素受体蛋白的蛋白酶体降解[3]。
在体外，Carbidopa处理72小时显著降低了NCI-H146、NCI-H209和NCI-H727细胞的活力，IC50值分别为12、22和29μM[4]。使用1mM的Carbidopa处理BxPC-3细胞24小时，显著降低了IDO1 mRNA和IDO1蛋白的表达[5]。使用300μM的Carbidopa处理MDA-MB-231细胞24小时，显著降低了细胞的线粒体膜电位，导致线粒体功能障碍和细胞损伤[6]。
在体内，每日两次腹腔注射7.5mg/kg剂量的Carbidopa，持续14天，显著抑制了MCF7细胞异种移植小鼠模型中的肿瘤生长，并导致肿瘤组织中CYP1A1蛋白增加和ERα蛋白减少[7]。每日腹腔注射25mg/kg的Carbidopa，持续11周，显著抑制了LNCaP细胞异种移植小鼠模型中的肿瘤生长，并抑制了血清前列腺特异性抗原（PSA）的产生[8]。
| Cell experiment [1]: | |
Cell lines | NCI-H146 cells |
Preparation Method | NCI-H146 cells (50,000) were seeded in 60mm plates in 3ml growth medium supplemented with 10% qualified, heat-inactivated FBS and 50units/ml of penicillin and streptomycin. Following incubation overnight, different concentrations of Carbidopa (0, 0.1, 1, 10, and 100μM) were added to the plate of a suspension cell line or to 3ml of fresh media for a monolayer cell for 72h and cell viability was measured. |
Reaction Conditions | 0, 0.1, 1, 10, and 100μM; 72h |
Applications | Carbidopa treatment significantly inhibited the cell viability of NCI-H146 cells in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | BALB/c nude mice |
Preparation Method | BALB/c nude mice were housed in temperature (23±2°C) and light-controlled (12:12-hour light-dark cycle) animal care facility with food and tap water ad libitum. The rats were provided with standard rat chow and water. MCF7 cells were subcutaneously injected into the right flank of each mouse (0.1ml; 1×106 cells per mouse). When tumors reached a volume of 100mm3, mice were randomized into control and treatment groups (6 mice per group); no specific criteria or method was used for randomization. The treatment group received intraperitoneal (i.p.) injection of Carbidopa (7.5mg/kg) and the control group the same amount of vehicle twice a day, every 12h. The treatment continued for 14 days continuously. The body weight and tumor volume were recorded every two days throughout the procedure. |
Dosage form | 7.5mg/kg; twice a day for 14 days; i.p. |
Applications | Carbidopa treatment inhibited tumor growth in a MCF7 cell-xenograft mouse model without affecting body weight. |
References: | |
| Cas No. | 38821-49-7 | SDF | |
| 别名 | 卡比多巴单水合物,(S)-(-)-Carbidopa monohydrate | ||
| Canonical SMILES | OC1=C(O)C=CC(C[C@](C)(NN)C(O)=O)=C1.O | ||
| 分子式 | C10H14N2O4.H2O | 分子量 | 244.2 |
| 溶解度 | DMSO: Slightly Soluble,Methanol: Slightly Soluble | 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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.095 mL | 20.475 mL | 40.95 mL |
| 5 mM | 819 μL | 4.095 mL | 8.19 mL |
| 10 mM | 409.5 μL | 2.0475 mL | 4.095 mL |
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