Krongrawa Wantanwa, Limmatvapirat Sontaya, Pongnimitprasert Nushjira, Meetam Paranee, Limmatvapirat Chutima
Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.
Asian J Pharm Sci. 2018 Sep;13(5):415-424. doi: 10.1016/j.ajps.2018.01.005. Epub 2018 Jan 31.
The biological activity of coconut ( L.) extracts from its kernels and various parts was reported by many previous studies, it is therefore believable that the extracts of its kernels might show some activities in topical formulations. Among several kernel extracts, the TC06 extract prepared by soaking the steamed coconut kernels in hot water showed the highest total phenolic content (6.98 ± 0.30 mg GAE/g extract) and the strongest antioxidant activity as determined using FRAP and DPPH methods with a reducing power value of 4.12 ± 0.16 mg AAE/g of extract and an SC value of 2.38 ± 0.14 mg/ml, respectively. In addition, this extract did not display any cytotoxic effects in the concentration range of 50-3200 µg/ml. Meanwhile, it revealed cytoprotective effects against -BHP-induced cytotoxicity in HaCaT cells at concentrations higher than 400 µg/ml. The results of phytochemical investigations including a chemical color test, TLC, H NMR and FTIR suggested that the TC06 extract was mainly composed of flavonoids and terpenoids. Furthermore, the concentrations of heavy metals including As, Cd, Hg, and Pb in the TC06 extract were below permissible limits. According to the solubility, the TC06 extract was incorporated into gels using Carbopol Ultrez 21 as a gelling agent. The formulated gel containing 3% (w/w) TC06 extract was stable at 4 °C and 25 °C with 75% RH throughout the storage period. It was found that the Carbopol Ultrez 21-based hydroalcoholic gel containing an aqueous extract of coconut kernels exhibited antioxidant activities in the two assays and showed a sufficient consistency, a pleasing color, and a non-oily perception during the period of observation.
许多先前的研究报道了椰子（L.）果仁及其各个部位提取物的生物活性，因此可以相信其果仁提取物在局部制剂中可能会表现出一些活性。在几种果仁提取物中，通过将蒸过的椰子果仁浸泡在热水中制备的TC06提取物显示出最高的总酚含量（6.98±0.30毫克没食子酸当量/克提取物），并且使用FRAP和DPPH方法测定时具有最强的抗氧化活性，还原力值分别为4.12±0.16毫克抗坏血酸当量/克提取物和SC值为2.38±0.14毫克/毫升。此外，该提取物在50-3200微克/毫升的浓度范围内未显示出任何细胞毒性作用。同时，在高于400微克/毫升的浓度下，它对HaCaT细胞中由叔丁基过氧化氢（t-BHP）诱导的细胞毒性具有细胞保护作用。包括化学颜色试验、薄层色谱（TLC）、氢核磁共振（¹H NMR）和傅里叶变换红外光谱（FTIR）在内的植物化学研究结果表明，TC06提取物主要由黄酮类化合物和萜类化合物组成。此外，TC06提取物中包括砷（As）、镉（Cd）、汞（Hg）和铅（Pb）在内的重金属浓度低于允许限值。根据溶解性，使用卡波姆Ultrez 21作为胶凝剂将TC06提取物掺入凝胶中。含有3%（w/w）TC06提取物的制剂凝胶在整个储存期内在4℃和25℃、相对湿度75%的条件下是稳定的。结果发现，含有椰子果仁水提取物的基于卡波姆Ultrez 21的水醇凝胶在两种测定中均表现出抗氧化活性，并且在观察期间显示出足够的稠度、宜人的颜色和无油腻感。
