Camalexin

Camalexin is an alkaloid phytoalexin derived from tryptophan in Arabidopsis thaliana with antimicrobial activity^[1]. Camalexin is produced in Arabidopsis thaliana upon microbial infection or abiotic induction, acting as both a component of plant immune responses and a hallmark representative of the indole phytoalexin family^[2]. Camalexin is commonly utilized in plant immunity research and the development of sustainable crop protection strategies against fungi, bacteria, viruses, and insects^[3].

In vitro, Camalexin (25-200μM) treatment of human breast cancer T47D cells for 72h significantly inhibited cell proliferation in a dose-dependent manner, with an IC₅₀ value of 133.8μM^[4]. Camalexin treatment of various human cancer cell lines for 72h significantly inhibited the proliferation of Jurkat (IC₅₀=46.2μM), HeLa (IC₅₀=50.0μM), MDA-MB-231 (IC₅₀=77.7μM), and CEM (IC₅₀=67.6μM) cells, while showing no significant toxicity against A-549 and MCF-7 cell lines even at 100μM concentration^[5]. Camalexin (25μM) treatment of human prostate cancer C4-2 cells for 24h induced the translocation of cathepsin D (CD) from lysosomes to the cytoplasm, an effect that could be partially reversed by 10mM of the antioxidant N-acetylcysteine (NAC)^[6].

In vivo, Camalexin (2.5, 5, 10mg/kg; every three days) via intraperitoneal injection in BALB/c mice bearing NB4 or HL-60 tumor xenografts for 27 days dose-dependently inhibited tumor volume and weight growth, with no significant effect on mouse body weight^[7]. Camalexin (100, 200mg/kg) administered orally to Benomyl-induced Parkinson’s disease mice for 14 days significantly improved motor coordination in the Rota-Rod test^[8].

References:
[1] ZOOK M, HAMMERSCHMIDT R. Origin of the thiazole ring of camalexin, a phytoalexin from Arabidopsis thaliana[J]. Plant physiology, 1997, 113(2): 463-468.
[2] NGUYEN N H, TROTEL-AZIZ P, CLÉMENT C, et al. Camalexin accumulation as a component of plant immunity during interactions with pathogens and beneficial microbes[J]. Planta, 2022, 255(6): 116.
[3] LOPA F R, SNIGDHA F N, LUMACTUD R A, et al. Harnessing Camalexin as a Sustainable and Ecofriendly Strategy to Control Harmful Phytopathogens[J]. Plant Pathology, 2025.
[4] YAMASHITA N, TAGA C, OZAWA M, et al. Camalexin, an indole phytoalexin, inhibits cell proliferation, migration, and mammosphere formation in breast cancer cells via the aryl hydrocarbon receptor[J]. Journal of natural medicines, 2022, 76(1): 110-118.
[5] PILATOVA M, IVANOVA L, KUTSCHY P, et al. In vitro toxicity of camalexin derivatives in human cancer and non-cancer cells[J]. Toxicology in Vitro, 2013, 27(2): 939-944.
[6] SMITH B, RANDLE D, MEZENCEV R, et al. Camalexin-induced apoptosis in prostate cancer cells involves alterations of expression and activity of lysosomal protease cathepsin D[J]. Molecules, 2014, 19(4): 3988-4005.
[7] YANG Y, WANG G, WU W, et al. Camalexin induces apoptosis via the ROS-ER stress-mitochondrial apoptosis pathway in AML cells[J]. Oxidative medicine and cellular longevity, 2018, 2018(1): 7426950.
[8] MANASA K, TAMILANBAN T, SANDHANAM K, et al. Exploring the Therapeutic Potential of Camalexin in Benomyl-induced Parkinson’ s Disease in Mice: In vitro, In vivo and Aldehyde Dehydrogenase Insights[J]. 2024.

Camalexin是拟南芥中一种源自色氨酸且具有抗菌活性的生物碱类植物抗毒素^[1]。Camalexin在拟南芥受到微生物感染或非生物诱导后产生，是植物免疫反应的组成部分，也是吲哚植物抗毒素家族的标志性代表^[2]。Camalexin常用于植物免疫力的研究及针对真菌、细菌、病毒和昆虫等可持续的作物保护策略开发^[3]。

在体外，Camalexin（25-200μM）处理人乳腺癌T47D细胞72h，以剂量依赖性方式显著抑制了细胞的增殖，IC₅₀值为133.8μM^[4]。Camalexin处理多种人类癌细胞系72h，可显著抑制Jurkat（IC₅₀=46.2μM）、HeLa（IC₅₀=50.0μM）、MDA-MB-231（IC₅₀=77.7μM）和CEM（IC₅₀=67.6μM）细胞的增殖，但对A-549和MCF-7细胞系即使在100μM浓度下也未见明显毒性作用^[5]。Camalexin（25μM）处理人前列腺癌C4-2细胞24h，诱导cathepsin D（CD）从溶酶体向胞质中转移，但可被10mM抗氧化剂N-acetylcysteine（NAC）部分逆转^[6]。

在体内，Camalexin（2.5, 5, 10mg/kg; every three days）通过腹腔注射治疗携带NB4或HL-60的肿瘤异种移植BALB/c小鼠27天，能剂量依赖性地抑制肿瘤体积和重量的增长，且对小鼠体重无显著影响^[7]。Camalexin（100, 200mg/kg）通过口服治疗Benomyl诱导的帕金森病小鼠14天，显著改善了小鼠在Rota-Rod测试中的运动协调能力^[8]。