Allicin is the main biologically active component of the freshly crushed garlic extracts[1]. Allicin has wide-ranging biological effects including antioxidative, anticancer, antimicrobial, and antifungal activities[2-5].
In vitro, treatment of HeLa, SW480, and L-929 cells with Allicin(0-100μM; 24h) inhibited the growth of cancer cells, induced the formation of apoptotic bodies and nuclear condensation, caused a typical DNA ladder, and activated caspases-3, -8, and -9 as well as cleaved poly(ADP-ribose) polymerase[3]. Treatment of lung adenocarcinoma cells with Allicin (0-20µM; 24h) dose-dependently inhibited cell adhesion, invasion, and migration, decreased mRNA and protein levels of MMP-2 and MMP-9, increased TIMP-1 and TIMP-2 levels, and suppressed AKT phosphorylation (P<0.05) without affecting total AKT expression[6].
In vivo, in a murine model of sporotrichosis induced by Sporothrix schenckii, oral administration of Allicin (400mg/kg/day for 15 days) enhanced antifungal activity by reducing fungal load and increased nitric oxide production, modulated immune responses by influencing cytokine release from peritoneal macrophages[5]. In a murine model of imiquimod-induced psoriasis-like dermatitis, topical application of Allicin (1.7, 3.4, and 5.0mg/g) twice daily for 6 consecutive days significantly improved the epidermal structure by inhibiting keratinocyte proliferation and reducing apoptosis, while decreasing the secretion of inflammatory cytokines (IL-17A/F, IL-22, IL-12, IL-20), chemokines (CXCL2, CXCL5, CCL20), and anti-bacterial peptides (S100a8/9) by directly inhibiting the IL-17-induced TRAF6/MAPK/NF-κB and STAT3/NF-κB signaling cascades[7].
References:
[1] Ankri S, Mirelman D. Antimicrobial properties of allicin from garlic. Microbes Infect. 1999;1(2):125-129.
[2] Chan JY, Yuen AC, Chan RY, Chan SW. A review of the cardiovascular benefits and antioxidant properties of allicin. Phytother Res. 2013;27(5):637-646.
[3] Oommen S, Anto RJ, Srinivas G, Karunagaran D. Allicin (from garlic) induces caspase-mediated apoptosis in cancer cells. Eur J Pharmacol. 2004;485(1-3):97-103.
[4] Müller A, Eller J, Albrecht F, et al. Allicin Induces Thiol Stress in Bacteria through S-Allylmercapto Modification of Protein Cysteines. J Biol Chem. 2016;291(22):11477-11490.
[5] Burian JP, Sacramento LVS, Carlos IZ. Fungal infection control by garlic extracts (Allium sativum L.) and modulation of peritoneal macrophages activity in murine model of sporotrichosis. Braz J Biol. 2017;77(4):848-855.
[6] Huang L, Song Y, Lian J, Wang Z. Allicin inhibits the invasion of lung adenocarcinoma cells by altering tissue inhibitor of metalloproteinase/matrix metalloproteinase balance via reducing the activity of phosphoinositide 3-kinase/AKT signaling. Oncol Lett. 2017;14(1):468-474.
[7] Zhang L, Ma X, Shi R, et al. Allicin ameliorates imiquimod-induced psoriasis-like skin inflammation via disturbing the interaction of keratinocytes with IL-17A. Br J Pharmacol. 2023;180(5):628-646.
Allicin是新鲜压碎的大蒜提取物中的主要生物活性成分[1]。Allicin具有广泛的生物效应，包括抗氧化、抗癌、抗菌和抗真菌活性[2-5]。
在体外实验中，用Allicin（0-100µM；24小时）处理HeLa、SW480和L-929细胞，能够抑制癌细胞生长，诱导凋亡小体的形成和核浓缩，导致典型的DNA梯状条带出现，并激活了半胱天冬酶-3、-8 和 -9 以及裂解的聚腺苷二磷酸核糖聚合酶[3]。在肺腺癌细胞中，Allicin（0-20µM；24小时）剂量依赖性地抑制了细胞的黏附、侵袭和迁移能力，降低了基质金属蛋白酶（MMP-2和-9的mRNA和蛋白水平，增加了组织金属蛋白酶抑制因子（TIMP-1和-2的水平，并抑制了AKT的磷酸化（P<0.05），但不影响AKT的总蛋白表达[6]。
在体内实验中，在由申克孢子菌（Sporothrix schenckii）诱导的小鼠孢子丝菌病模型中，口服给予Allicin（400mg/kg/天；连续15天），通过减少真菌负荷和增加一氧化氮的产生增强了抗真菌活性，并通过影响腹膜巨噬细胞释放的细胞因子调节免疫反应[5]。在由咪喹莫特诱导的小鼠银屑病样皮炎模型中，局部应用Allicin（1.7、3.4和5.0mg/g），每天两次，连续6天，通过抑制角质形成细胞的增殖和减少凋亡显著改善了表皮结构，同时通过直接抑制IL-17诱导的TRAF6/MAPK/NF-κB和STAT3/NF-κB信号级联，减少了炎症细胞因子（IL-17A/F、IL-22、IL-12、IL-20）、趋化因子（CXCL2、CXCL5、CCL20）和抗菌肽（S100a8/9）的分泌[7]。