Macelignan ((+)-Anwulignan)
(Synonyms: 安五脂素; (+)-Anwulignan; Anwuligan) 目录号 : GC30878Macelignan ((+)-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。
Cas No.:107534-93-0
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1]: | |
Cell lines | HaCaT cells |
Preparation Method | HaCaT cells were treated with 0.1, 0.5, 1µM Macelignan for 24h and then exposed to UVB (30mJ/cm2) radiation. After UVB exposure, fresh media plus samples were added. At 72h after UVB irradiation, percent cell viability was assessed by the MTT assay. |
Reaction Conditions | 0.1, 0.5, 1µM; 24h |
Applications | Macelignan at a concentration of 0.1-1µM restores the viability of UVB-treated HaCaT cells, with the greatest cell viability approaching closely 100%. |
Animal experiment [2]: | |
Animal models | C57BL/KsJ-db/db mice |
Preparation Method | The body weight and fasting blood glucose levels of 10-week-old mice were measured. Then, the mice were equally divided into four groups: (1)diabetic control group, (2)Rosiglitazone group, (3)Macelignan group, and (4) treatment group (with extract). All groups were fed with a standard AIN-76 semi-synthetic diet, and the three experimental groups (Rosiglitazone, Macelignan, and treatment groups) were orally administered with rosiglitazone (10mg/kg), Macelignan (15mg/kg), or multi-herbal extract (150mg/kg) for 3 weeks. After starvation for 12h, the mice were anesthetized with ether and blood samples were taken from the inferior vena cava for follow-up analysis. |
Dosage form | 15mg/kg/day for 3 weeks; p.o. |
Applications | Macelignan treatment significantly reduced the blood glucose levels in db/db mice. |
References: [1]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. [2]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. |
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]。
Cas No. | 107534-93-0 | SDF | |
别名 | 安五脂素; (+)-Anwulignan; Anwuligan | ||
Canonical SMILES | OC1=CC=C(C[C@H](C)[C@H](C)CC2=CC=C(OCO3)C3=C2)C=C1OC | ||
分子式 | C20H24O4 | 分子量 | 328.4 |
溶解度 | DMSO : ≥ 30 mg/mL (91.35 mM) | 储存条件 | Store at -20°C,protect from light |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
||
Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.0451 mL | 15.2253 mL | 30.4507 mL |
5 mM | 0.609 mL | 3.0451 mL | 6.0901 mL |
10 mM | 0.3045 mL | 1.5225 mL | 3.0451 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。