Macelignan ((+)-Anwulignan) is a bioactive lignan isolated from nutmeg seeds. It has antibacterial and anti-caries effects on Streptococci such as Streptococcus mutans[1]. Macelignan has multiple pharmacological activities, including anti-inflammatory, anti-cancer, anti-diabetic and neuroprotective activities[2]. Macelignan can inhibit M2 macrophage polarization[3].
In vitro, treatment of HaCaT cells with Macelignan (0.1-1µM) for 24h can reverse the decrease in cell viability caused by UVB treatment, restore cell viability to nearly 100%, and reduce UVB-induced activation of mitogen-activated protein kinase (MAPK), phosphatidylinositol 3-kinase/Akt (PI3K/Akt) and their downstream transcription factors[4]. Treatment of HT22 neuronal cells with Macelignan (1-10μM) for 24h reversed the decrease in cell viability induced by glutamate in a dose-dependent manner and significantly reduced the production of intracellular reactive oxygen species (ROS)[5]. Macelignan (2.5-10μM) treated BV2 microglia for 24 h, inhibited the production of intracellular inflammatory cytokines and nitric oxide (NO) in a dose-dependent manner, and inhibited the expression of inducible nitric oxide synthase (iNOS) protein[6].
In vivo, oral treatment of type 2 diabetes model mice with Macelignan (15mg/kg) for 3 weeks significantly reduced the postprandial blood glucose level of mice[7]. Macelignan (40, 80, 160mg/kg) was used to treat renal ischemia-reperfusion injury (IRI) mice by intraperitoneal injection, and dose-dependently reduced the levels of serum creatinine, blood urea nitrogen, interleukin 6 (IL-6), tumor necrosis factor α (TNF-α) and gamma interferon (IFN-γ) in the blood, and inhibited IRI-induced renal tubular epithelial cell apoptosis[8].
References:
[1] Chung J Y, Choo J H, Lee M H, et al. Anticariogenic activity of macelignan isolated from Myristica fragrans (nutmeg) against Streptococcus mutans[J]. Phytomedicine, 2006, 13(4): 261-266.
[2] Paul S, Hwang J K, Kim H Y, et al. Multiple biological properties of macelignan and its pharmacological implications[J]. Archives of pharmacal research, 2013, 36: 264-272.
[3] Che N, Li M, Liu X, et al. Macelignan prevents colorectal cancer metastasis by inhibiting M2 macrophage polarization[J]. Phytomedicine, 2024, 122: 155144.
[4] Hwang J K. Effects of macelignan isolated from Myristica fragrans Houtt. on UVB-induced matrix metalloproteinase-9 and cyclooxygenase-2 in HaCaT cells[J]. Journal of dermatological science, 2010, 57(2): 114-122.
[5] Jin D Q, Lim C S, Hwang J K, et al. Anti-oxidant and anti-inflammatory activities of macelignan in murine hippocampal cell line and primary culture of rat microglial cells[J]. Biochemical and biophysical research communications, 2005, 331(4): 1264-1269.
[6] Zong K, Liu X, Sun Z, et al. Macelignan inhibits the inflammatory response of microglia and regulates neuronal survival[J]. Journal of Neuroimmunology, 2020, 339: 577123.
[7] Yeo J, Kang Y M, Cho S I, et al. Effects of a multi-herbal extract on type 2 diabetes[J]. Chinese Medicine, 2011, 6: 1-10.
[8] Long J, Qian K, Tan S, et al. Macelignan protects against renal ischemia-reperfusion injury via inhibition of inflammation and apoptosis of renal epithelial cells[J]. Cellular and Molecular Biology, 2020, 66(1): 55-59.
Macelignan ((+)-Anwulignan)是从肉豆蔻种子中分离出来的一种生物活性木脂素，对变形链球菌等链球菌具有抗菌和防龋作用[1]。Macelignan具有多种药理活性，包括抗炎、抗癌、抗糖尿病和神经保护活性[2]。Macelignan 能够抑制M2巨噬细胞极化[3]。
在体外，Macelignan（0.1-1µM）处理HaCaT细胞24h，可逆转经UVB处理导致的细胞活力下降，恢复细胞活力接近100%，减少了UVB诱导的丝裂原活化蛋白激酶（MAPK）、磷脂酰肌醇3-激酶/Akt（PI3K/Akt）及其下游转录因子的活化[4]。Macelignan（1-10μM）处理HT22神经元细胞24h，以剂量依赖性方式逆转了谷氨酸诱导的细胞活力下降，显著减少了细胞内活性氧（ROS）的产生[5]。Macelignan（2.5-10μM）处理BV2小胶质细胞24h，以剂量依赖性方式抑制了细胞内炎症细胞因子和一氧化氮（NO）的产生，抑制了诱导型一氧化氮合酶（iNOS）蛋白的表达[6]。
在体内，Macelignan（15mg/kg）通过口服治疗2型糖尿病模型小鼠3周，显著降低了小鼠的餐后血糖水平[7]。Macelignan（40、80、160mg/kg）通过腹腔注射治疗肾缺血再灌注损伤（IRI）小鼠，剂量依赖性降低了血液中血清肌酐、血尿素氮、白细胞介素6（IL-6）、肿瘤坏死因子α（TNF-α）和γ干扰素（IFN-γ）的水平，抑制了IRI诱导的肾小管上皮细胞凋亡[8]。