Loliolide is a monoterpene lactone with diverse biological activities. Loliolide is widely found in marine algae, terrestrial organisms, fungi, and certain animal organisms, and has a wide range of biological activities, including anti-inflammatory, antioxidant, anticancer, neuroprotective, antidiabetic, antidepressant, immunosuppressive, antiviral, and allelopathic effects[1].
In vitro, Loliolide did not induce cytotoxicity in HaCaT keratinocytes at concentrations of 0-62.5µg/mL, and in IFN-γ/TNF-α-stimulated HaCaT cells, it dose-dependently restored cell viability, reduced intracellular ROS, downregulated cytokines and chemokines, and inhibited NF-κB signaling by suppressing p-IκBα/p65 expression and p65 nuclear translocation[2]. Loliolide showed no cytotoxicity in SH-SY5Y cells at 1–100µM and exerted neuroprotective effects against 100µM 6-OHDA-induced toxicity, increasing cell viability by 23.70±7.77% and 41.06±6.31% at 50 and 100µM, respectively[3].
In vivo, Loliolide at 6.25, 12.5, and 25µg/mL for 1h dose-dependently inhibited UVB-induced ROS, NO production, lipid peroxidation, and cell death in zebrafish[4].
References:
[1] Farzeen I, Zafar S, Zafar N, Fatima S, Nazir MM, Ashraf A. Loliolide: green monoterpenoid lactone with therapeutic and ecological significance-a comprehensive review with computational validation. Mol Divers.
[2] Han EJ, Fernando IPS, Kim HS, et al. (-)-Loliolide Isolated from Sargassum horneri Suppressed Oxidative Stress and Inflammation by Activating Nrf2/HO-1 Signaling in IFN-γ/TNF-α-Stimulated HaCaT Keratinocytes. Antioxidants (Basel). 2021;10(6):856.
[3] Silva J, Alves C, Martins A, et al. Loliolide, a New Therapeutic Option for Neurological Diseases? In Vitro Neuroprotective and Anti-Inflammatory Activities of a Monoterpenoid Lactone Isolated from Codium tomentosum. Int J Mol Sci. 2021;22(4):1888.
[4] Wang L, Kim HS, Je JG, et al. In Vitro and In Vivo Photoprotective Effects of (-)-Loliode Isolated from the Brown Seaweed, Sargassum horneri. Molecules. 2021;26(22):6898.
Loliolide是一种具有多种生物活性的单萜内酯。Loliolide广泛存在于海洋藻类、陆生生物、真菌和某些动物中，并具有广泛的生物活性，包括抗炎、抗氧化、抗癌、神经保护、抗糖尿病、抗抑郁、免疫抑制、抗病毒和化感作用[1]。
体外实验中，在0-62.5µg/mL浓度范围内，Loliolide对HaCaT角质形成细胞无细胞毒性；在IFN-γ/TNF-α刺激的HaCaT细胞中，其可剂量依赖性恢复细胞活力、降低细胞内ROS水平、下调细胞因子和趋化因子表达，并通过抑制p-IκBα/p65表达及p65的核转位而抑制NF-κB信号通路[2]。Loliolide在1-100µM范围内对SH-SY5Y细胞无细胞毒性，并对100µM 6-OHDA诱导的毒性具有神经保护作用，在50µM和100µM时分别使细胞活力提高23.70±7.77%和41.06±6.31%[3]。
体内实验中，Loliolide在6.25、12.5和25µg/mL浓度下处理1小时，可剂量依赖性抑制UVB诱导的斑马鱼体内ROS和NO的产生，以及脂质过氧化和细胞死亡[4]。