Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, Thailand.
Cluster of Excellence on Biodiversity based Economics and Society (B.BES-CMU), Chiang Mai University, Chiang Mai 50200, Thailand.
Nutrients. 2018 Apr 4;10(4):444. doi: 10.3390/nu10040444.
Colorectal cancer occurs due to various factors. The important risks are dietary lifestyle and inflammatory bowel diseases, such as Crohn’s disease and ulcerative colitis. It has been found that the inhibitory enzyme cyclooxygenase-2 (COX-2) in the colorectal region can potentially reduce the risk of colorectal cancer. The present study investigated rice bran oil from natural purple rice bran, which exhibits antioxidant and anti-inflammatory activity. This study aimed to evaluate the bioactive compound content of natural purple rice bran oil (NPRBO) derived from native Thai purple rice and the anti-inflammatory activity of NPRBO in colorectal cancer cells, and to develop a colorectal delivery platform in the form of film-coated tablets. NPRBO from the rice bran of five different Thai purple rice cultivars, namely Khao’ Gam Leum-Phua (KGLP), Khao’ Gam Boung (KGB), Khao’ Gam Thor (KGT), Khao’ Gam Pah E-Kaw (KGPEK), and Khao’ Niaw Dam (KND), were extracted using the supercritical carbon dioxide extraction technique. The amount of γ-oryzanol (ORY), tocotrienols, and tocopherols present in NPRBOs and the in vitro anti-inflammatory activity of NPRBO were investigated. The highest anti-inflammatory NPRBO was transformed into a dry and free-flowing powder by liquisolid techniques. Then, it was compressed into core tablets and coated with EudragitL100 and Eudragit NE30D. The in vitro release study of the film-coated NPRBO tablets was performed in three-phase simulated gastrointestinal media. The cultivar KGLP was superior to the other samples in terms of the ORY, tocotrienol and tocopherol contents and anti-inflammatory activity. Aerosil was the most suitable absorbent for transforming NPRBO into a free-flowing powder and was used to prepare the NPRBO core tablets. The in vitro KGLP-NPRBO film-coated tablet release profile showed that no ORY was released at gastric pH while 85% of ORY was released at pH 7.4 after 6 h; this would be expected to occur in the colorectal area. Therefore, this study demonstrates the potential of KGLP-NPRBO to prevent colorectal cancer via a specific colorectal dietary supplement delivery system.
结直肠癌的发生涉及多种因素。重要的风险因素包括饮食生活方式和炎症性肠病，如克罗恩病和溃疡性结肠炎。已经发现，结直肠区域的抑制酶环氧化酶-2（COX-2）可能降低结直肠癌的风险。本研究调查了天然紫米米糠油，其具有抗氧化和抗炎活性。本研究旨在评估源自泰国本土紫米的天然紫米糠油（NPRBO）的生物活性化合物含量及其在结直肠癌细胞中的抗炎活性，并以薄膜包衣片剂的形式开发一种结直肠给药平台。使用超临界二氧化碳萃取技术从五个不同的泰国紫米品种（Khao’ Gam Leum-Phua（KGLP）、Khao’ Gam Boung（KGB）、Khao’ Gam Thor（KGT）、Khao’ Gam Pah E-Kaw（KGPEK）和 Khao’ Niaw Dam（KND）的米糠中提取 NPRBO。研究了 NPRBO 中γ-谷维素（ORY）、生育三烯酚和生育酚的含量以及 NPRBO 的体外抗炎活性。具有最高抗炎活性的 NPRBO 通过液质转化技术转化为干燥且自由流动的粉末。然后，将其压缩成核心片剂，并包衣以 EudragitL100 和 Eudragit NE30D。在三相模拟胃肠道介质中进行了 NPRBO 薄膜包衣片剂的体外释放研究。KGLP 在 ORY、生育三烯酚和生育酚含量和抗炎活性方面优于其他样品。Aerosil 是将 NPRBO 转化为自由流动粉末的最合适吸收剂，并用于制备 NPRBO 核心片剂。体外 KGLP-NPRBO 薄膜包衣片剂的释放曲线表明，在胃 pH 值下没有 ORY 释放，而在 pH7.4 下 6 小时后有 85%的 ORY 释放；这预计会在结直肠区域发生。因此，本研究表明，通过特定的结直肠饮食补充剂递送系统，KGLP-NPRBO 有可能预防结直肠癌。
