Chiu Sharon, Wang Thomas, Belski Martin, Abourashed Ehab A
Nat Prod Commun. 2016 Apr;11(4):483-8.
Many studies on the biological activities of nutmeg continue to appear in the literature. The most common targets include GIT, CNS, oxidative stress and inflammation. However, results obtained from most studies are often inconsistent due to the variability of utilized samples, lack of standardized nutmeg products or insufficient amounts of pure compounds for comprehensive follow-up investigation. To address the consistency and supply issue we utilized available technology to develop a reproducible procedure for preparation of specific extracts and isolation of the major phenolic constituents present in nutmeg kemel. A well-defined and reproducible sequence of extraction, fractionation and chromatographic purification was adopted and was guided by HPLC fingerprinting. Spectroscopic methods, mainly NMR, and mass spectrometry were utilized to identify each compound. Thirteen compounds were isolated in a pure form and identified as: elemicin (1), isoelemicin (2), myristicin (4), surinamensin (5), malabaricone C (6), 2-(3'-allyl-2',6'-dimethoxy-phenyloxy)-l- acetoxy-(3,4-dimethoxyphenyl)-propyl ester (7), methoxylicarin A (8), licarin A (9), malabaricone B (10), licarin C (11), 5'-methoxylicarin B (12), licarin B (13), and 2-(3'-allyl-2',6'-dimethoxy-phenyloxy)-l-methyl-5-methoxy-1,2-dihydrobenzofuran (3, a new compound). With repeated isolation runs, these pure compounds can be prepared in quantities sufficient for biological evaluation as needed. The availability of purified compounds will also allow the development of specific, accurate, and sensitive analytical procedures for pharmacokinetic studies and for quality control of nutmeg products. Both aspects are essential for nutmeg-focused drug discovery. The same approach can also be adapted to other medicinal plants of potential interest.
关于肉豆蔻生物活性的许多研究仍不断出现在文献中。最常见的研究对象包括胃肠道、中枢神经系统、氧化应激和炎症。然而,由于所用样品的变异性、缺乏标准化的肉豆蔻产品或用于全面后续研究的纯化合物数量不足,大多数研究所得结果往往不一致。为了解决一致性和供应问题,我们利用现有技术开发了一种可重复的程序,用于制备特定提取物并分离肉豆蔻仁中存在的主要酚类成分。我们采用了明确且可重复的提取、分馏和色谱纯化顺序,并以高效液相色谱指纹图谱为指导。利用光谱方法(主要是核磁共振)和质谱来鉴定每种化合物。以纯形式分离出13种化合物,分别鉴定为:榄香脂素(1)、异榄香脂素(2)、肉豆蔻醚(4)、苏里南烯(5)、马拉巴酮C(6)、2-(3'-烯丙基-2',6'-二甲氧基苯氧基)-1-乙酰氧基-(3,4-二甲氧基苯基)-丙酯(7)、甲氧基卡林A(8)、利卡灵A(9)、马拉巴酮B(10)、利卡灵C(11)、5'-甲氧基卡林B(12)、利卡灵B(13)以及2-(3'-烯丙基-2',6'-二甲氧基苯氧基)-1-甲基-5-甲氧基-1,2-二氢苯并呋喃(3,一种新化合物)。通过重复分离操作,这些纯化合物可按需制备出足以进行生物学评估的量。纯化化合物的可得性还将有助于开发用于药代动力学研究和肉豆蔻产品质量控制的特定且准确灵敏的分析程序。这两个方面对于以肉豆蔻为重点的药物发现都至关重要。同样的方法也可适用于其他有潜在价值的药用植物。