Hinokitiol是一种在Formosan cypress中天然存在的tropolone类化合物，具有抗菌和抗癌特性。
Cas No.:499-44-5
Sample solution is provided at 25 µL, 10mM.
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Hinokitiol is a naturally occurring tropolone compound from the Formosan cypress with antibacterial and anticancer properties [1]. Hinokitiol induces oxidative stress, cytotoxicity, and autophagy through modulation of PI3K/Akt/mTOR, p38/ERK/MAPK, nuclear factor kappa B, and c-Jun N-terminal kinase signaling pathways [2]. Hinokitiol has been widely used to inhibit the metabolic processes of bacterial cell membranes, regulate respiration and membrane permeability, thereby effectively killing various bacteria[3].
In vitro, Hinokitiol treatment for 48 hours significantly reduced the cell viability of Ishikawa cells, HEC-1A cells, and KLE cells, with IC50 values of 13.33μM, 49.51μM, and 4.69μM, respectively[4]. Treatment with 30μg/ml Hinokitiol for 24 hours led to the loss of cell membrane integrity and cell cycle arrest in KB-1 cells[5]. Treatment with 40µM Hinokitiol for 24 hours blocked the process of HeLa cells transitioning from the G2/M phase to the G1 phase, increased the expression levels of p21 and p53, promoted cytoplasmic expansion and enhanced SA-β-gal activity, and induced cell senescence[6].
In vivo, Hinokitiol treatment via oral administration at a dose of 100mg/kg every other day for 3 weeks significantly reduced tumor volume and tumor weight in the HCT-116 xenograft mouse model[7]. A single intravenous injection of 1.7mg/kg dose of Hinokitiol can alleviate liver injury induced by hemorrhagic shock/resuscitation in mice within 24 hours[8].
References:
[1] El Hachlafi N, Lakhdar F, Khouchlaa A, et al. Health benefits and pharmacological properties of hinokitiol[J]. Processes, 2021, 9(9): 1680.
[2] Bhuia M S, Chowdhury R, Afroz M, et al. Therapeutic efficacy studies on the Monoterpenoid Hinokitiol in the treatment of different types of cancer[J]. Chemistry & biodiversity, 2025, 22(5): e202401904.
[3] Morita Y, Sakagami Y, Okabe T, et al. The mechanism of the bactericidal activity of hinokitiol[J]. Biocontrol Science, 2007, 12(3): 101-110.
[4] Chen H Y, Cheng W P, Chiang Y F, et al. Hinokitiol exhibits antitumor properties through induction of ROS-mediated apoptosis and p53-driven cell-cycle arrest in endometrial cancer cell lines (Ishikawa, HEC-1A, KLE)[J]. International journal of molecular sciences, 2021, 22(15): 8268.
[5] Roy A, Cheriyan B V, Perumal E, et al. Effect of hinokitiol in ameliorating oral cancer: in vitro and in silico evidences[J]. Odontology, 2025, 113(2): 750-763.
[6] Wang C C, Chen B K, Chen P H, et al. Hinokitiol induces cell death and inhibits epidermal growth factor-induced cell migration and signaling pathways in human cervical adenocarcinoma[J]. Taiwanese Journal of Obstetrics and Gynecology, 2020, 59(5): 698-705.
[7] Lee Y S, Choi K M, Kim W, et al. Hinokitiol inhibits cell growth through induction of S-phase arrest and apoptosis in human colon cancer cells and suppresses tumor growth in a mouse xenograft experiment[J]. Journal of natural products, 2013, 76(12): 2195-2202.
[8] Lu W J, Lin K H, Tseng M F, et al. New therapeutic strategy of hinokitiol in haemorrhagic shock‐induced liver injury[J]. Journal of Cellular and Molecular Medicine, 2019, 23(3): 1723-1734.
Hinokitiol是一种在Formosan cypress中天然存在的tropolone类化合物，具有抗菌和抗癌特性[1]。Hinokitiol通过调控PI3K/Akt/mTOR、p38/ERK/MAPK、核因子κB和c-Jun N-terminal kinase信号通路，诱导氧化应激、细胞毒性和自噬[2]。Hinokitiol已被广泛用于抑制细菌细胞膜的代谢过程，调节呼吸和膜通透性，从而有效杀灭多种细菌[3]。
在体外，Hinokitiol处理Ishikawa细胞、HEC-1A细胞和KLE细胞48小时，显著降低了细胞活力，IC50值分别为13.33μM、49.51μM和4.69μM[4]。30μg/ml的Hinokitiol处理KB-1细胞24小时，导致细胞膜完整性丧失和细胞周期阻滞[5]。40µM的Hinokitiol处理HeLa细胞24小时，阻断了细胞从G2/M期向G1期的转变，增加了p21和p53的表达水平，促进了细胞质扩张并提高了SA-β-gal活性，诱导了细胞衰老[6]。
在体内，每隔一天口服100mg/kg剂量的Hinokitiol，持续3周，显著降低了HCT-116异种移植小鼠模型中的肿瘤体积和肿瘤重量[7]。单次静脉注射1.7mg/kg剂量的Hinokitiol，可在24小时内减轻失血性休克/复苏诱导的小鼠肝损伤[8]。
| Cell experiment [1]: | |
Cell lines | KLE cells |
Preparation Method | KLE cells were seeded in 96-well plates at a density of 3×103 cells in DMEM/Ham’s F-12 with 10% (v/v) fetal bovine serum (FBS), 100U/ml penicillin, and 100µg/ml streptomycin in a humidified atmosphere containing 5% CO2 for 24h. After 48h of treatment with different concentrations of Hinokitiol (1, 5, 10, 25, and 50µM), the cell viability was measured. |
Reaction Conditions | 1, 5, 10, 25, and 50µM; 48h |
Applications | Hinokitiol treatment significantly inhibited the cell viability of KLE cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male BALB/c-nude mice |
Preparation Method | Male BALB/c-nude mice (6 weeks old; 22-25g) were housed in a room with controlled temperature (21-23°C), humidity (55-60%), and lighting (12h light/dark cycle) and were supplied with water. After being acclimated for 1 week, nude mice were randomly distributed in 3 groups: normal (n=10), HCT-116 xenograft (n=10), HCT-116 xenograft-Hinokitiol treatment (n=10). The mice were inoculated with HCT-116 cells by intradermal injection (2×106 tumor cells in 0.2ml of PBS/mouse) with a 26-gauge needle into the flank. After 2 days, mice were orally administered Hinokitiol (100mg/kg; every other day for 3 weeks). Tumor volumes were periodically measured. |
Dosage form | 100mg/kg; every other day for 3 weeks; p.o. |
Applications | Hinokitiol treatment significantly decreased the tumor volumes in mice with HCT-116 xenografts. |
References: | |
| Cas No. | 499-44-5 | SDF | |
| 别名 | 桧木醇; β-Thujaplicin | ||
| 化学名 | 2-hydroxy-4-isopropylcyclohepta-2,4,6-trienone | ||
| Canonical SMILES | OC1=CC(C(C)C)=CC=CC1=O | ||
| 分子式 | C10H12O2 | 分子量 | 164.20 |
| 溶解度 | ≥ 16.4mg/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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 6.0901 mL | 30.4507 mL | 60.9013 mL |
| 5 mM | 1.218 mL | 6.0901 mL | 12.1803 mL |
| 10 mM | 609 μL | 3.0451 mL | 6.0901 mL |
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| 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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2.
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