Dharambir Kashyap, Ajay Sharma, Hardeep S Tuli, Sandeep Punia, Anil K Sharma
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引用次数: 104
Abstract
Background: Plant derived products are not only served as dietary components but also used to treat and prevent the inflammatory associated diseases like cancer. Among the natural products pentacyclic terpenoids including ursolic acid and oleanolic acid are considered as the promising anti-inflammatory therapeutic agents.
Objectives: The current review extensively discusses the anti-inflammatory therapeutic potential of these pentacyclic moieties along with their proposed mechanisms of action. Furthermore, the relevant patents have also been listed to present the health benefits of these promising therapeutic agents to pin down the inflammatory diseases. Expert opinion: Pentacyclic terpenoids are known to negatively down-regulate a variety of extracellular and intracellular molecular targets associated with disease progression. The major anti-inflammatory effects of these molecules have been found to be mediated via inactivation of NFkB, STAT3/6, Akt/mTOR pathways. A number of patents on UA & OA based moieties have been reported between 2010 and 2016. Still there have been only a few compounds which meet the need of sufficient hydro solubility and bioavailability along with higher anti-inflammatory activities. Thus, it is essential to develop novel derivatives of terpenpoids which may not only overcome the solubility issues but also may improve their therapeutic effects. In addition, scientific community may utilize nanotechnology based drug delivery systems so as to increase the bio-availability, selectivity and dosages related problems.
背景：植物提取物不仅可作为膳食成分，还可用于治疗和预防癌症等与炎症相关的疾病。在天然产品中，包括熊果酸和齐墩果酸在内的五环萜类化合物被认为是很有前景的抗炎治疗剂：本综述广泛讨论了这些五环分子的抗炎治疗潜力及其拟议的作用机制。此外，还列出了相关专利，以介绍这些有前景的治疗剂对治疗炎症疾病的健康益处。专家意见：众所周知，五环萜类化合物能够负向下调与疾病进展相关的多种细胞外和细胞内分子靶标。已发现这些分子的主要抗炎作用是通过 NFkB、STAT3/6、Akt/mTOR 通路的失活介导的。2010 年至 2016 年间，基于 UA 和 OA 的分子申请了多项专利。然而，只有少数几种化合物既能满足足够的水溶性和生物利用度要求，又具有较高的抗炎活性。因此，开发新型萜类衍生物至关重要，这不仅能克服溶解性问题，还能提高其治疗效果。此外，科学界还可以利用基于纳米技术的给药系统来提高生物利用率、选择性和剂量相关问题。
期刊介绍：
Recent Patents on Inflammation & Allergy Drug Discovery publishes review articles by experts on recent patents in the field of inflammation and allergy drug discovery e.g. on novel bioactive compounds, analogs and targets. A selection of important and recent patents in the field is also included in the journal. The journal is essential reading for all researchers involved in inflammation and allergy drug design and discovery.
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