AbMole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

Honokiol（和厚朴酚）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]；Honokiol（CAS 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SKOV3与Caov-3卵巢癌细胞中的半抑制浓度（IC₅₀）分别为48.71±11.31 μM与46.42±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PCNA、MMP-2、β-catenin及c-Myc表达，抑制Wnt/β-catenin通路[4]。Honokiol（和厚朴酚）在U87 MG与U-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，Honokiol在SD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。。