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AbMole小讲堂丨Honokiol(和厚朴酚):一种具有多靶点调节活性的天然产物及其科研应用

已有 258 次阅读 2026-3-12 15:08 |系统分类:科研笔记

Honokiol(和厚朴酚,AbMoleM3377)是一种源自木兰属植物树皮的天然双酚类新木脂素化合物,具有多靶点生物活性,例如抑制Akt磷酸化以及促进ERK1/2磷酸化。Honokiol在肾癌细胞中能显著抑制细胞增殖与迁移[1]HonokiolCAS No.35354-74-6)被用于处理异位子宫内膜间质细胞(EESCs),在低剂量时无明显细胞毒性,但可抑制该细胞迁移、侵袭及上皮-间质转化(EMT)等过程[2]Honokiol(和厚朴酚)在SKOV3Caov-3卵巢癌细胞中的半抑制浓度(IC₅₀)分别为48.71±11.31 μM46.42±5.37 μM,能通过激活caspase-3/7/9诱导上述细胞的凋亡[3]

Honokiol(和厚朴酚)在SK-BR-3乳腺癌细胞中,50–60 μmol/L处理后可显著提升其凋亡率,下调PCNAMMP-2β-cateninc-Myc表达,抑制Wnt/β-catenin通路[4]Honokiol(和厚朴酚,AbMoleM3377)在U87 MGU-87 MG-R9胶质瘤细胞中,能促进caspase-9活化、Bax上调及Bcl-2下调,并通过AMPK-mTOR通路诱导该细胞的自噬依赖性凋亡[5]

动物实验方面,Honokiol(和厚朴酚)在SD大鼠子宫内膜异位症模型中,腹腔注射给药后显著改善小鼠的病理形态[2]Honokiol(和厚朴酚)还在C57BL/6小鼠脉络膜新生血管模型中,以20 mg/kg的剂量通过抑制HIF-1α/VEGF轴减轻小鼠病灶面积与渗漏[6];此外,HonokiolSD大鼠非酒精性脂肪性肝炎模型中,通过PPARγ通路促进巨噬细胞M2极化[7]Honokiol还能在氟化钠诱导的C57BL/6小鼠认知障碍模型中,通过激活Sirt3提升SOD2活性、清除线粒体活性氧[8]

参考文献及鸣谢

[1] Hamedani, Y.; Chakraborty, S.; Sabarwal, A.; et al. Novel Honokiol-eluting PLGA-based scaffold effectively restricts the growth of renal cancer cells. PloS one 2020, 15 (12), e0243837.

[2] Kong, X.; Lei, L. Honokiol inhibits cell migration and invasion by blocking EMT via Snail/Slug axis in endometriosis. Naunyn-Schmiedeberg's archives of pharmacology 2026, 399 (3), 4507-4517.

[3] Lee, J. S.; Sul, J. Y.; Park, J. B.; et al. Honokiol induces apoptosis and suppresses migration and invasion of ovarian carcinoma cells via AMPK/mTOR signaling pathway. International journal of molecular medicine 2019, 43 (5), 1969-1978.

[4] Shi, H.; Wang, Y.; Yao, M.; et al. Honokiol inhibits the growth of SKBR3 cells. Translational cancer research 2020, 9 (12), 7596-7604.

[5] Lin, C. J.; Chen, T. L.; Tseng, Y. Y.; et al. Honokiol induces autophagic cell death in malignant glioma through reactive oxygen species-mediated regulation of the p53/PI3K/Akt/mTOR signaling pathway. Toxicology and applied pharmacology 2016, 304, 59-69.

[6] Pan, N.; Shi, J.; Du, S.; et al. Honokiol Attenuates Choroidal Neovascularization by Inhibiting the Hypoxia-Inducible Factor-alpha/Vascular Endothelial Growth Factor Axis via Nuclear Transcription Factor-Kappa B Activation. Current eye research 2024, 49 (1), 88-96.

[7] Zhong, X.; Liu, H. Honokiol attenuates diet-induced non-alcoholic steatohepatitis by regulating macrophage polarization through activating peroxisome proliferator-activated receptor gamma. Journal of gastroenterology and hepatology 2018, 33 (2), 524-532.

[8] Wang, D.; Cao, L.; Zhou, X.; et al. Mitigation of honokiol on fluoride-induced mitochondrial oxidative stress, mitochondrial dysfunction, and cognitive deficits through activating AMPK/PGC-1alpha/Sirt3. Journal of hazardous materials 2022, 437, 129381.

 

细胞实验参考

细胞系:SKOV3, Caov-3 and NIH-3T3 cell

方法:Cells were seeded at 5×103 cells/ml in 96-well microplates and were cultured overnight to allow attachment. Honokiol (1-100 µM), compound C (20 µM), and AICAR (500 µM) were added to the medium.

浓度:1-100 µM

处理时间:24 h

参考文献International Journal of Molecular Medicine, 2019, 43(5): 1969-1978. 

* 上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。

动物实验参考

动物模型Male Institute of Cancer Research (ICR) mice

配制Sterile saline containing 10% dimethyl sulfoxide (DMSO)

剂量10 and 20 mg/kg

给药处理i.p.

参考文献Eur J Pharmacol. 2015 Aug 5;760:88-95.

 

* 上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。  体内实验的工作液,建议现用现配,当天使用;如在配制过程中出现沉淀、析出现象,可以通过超声和(或)加热的方式助溶。  切勿一次性将产品全部溶解。  建议制定动物给药及实验方案时,尽量参考已发表的相关实验文献(溶剂种类及配比众多,简单地溶解目的化合物,并不能解决动物给药依从性、体内生物利用度、组织分布等相关问题,未必能保证目的化合物在动物体内充分发挥生物学效用)。



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