Goyal Sameer N, Prajapati Chaitali P, Gore Prashant R, Patil Chandragouda R, Mahajan Umesh B, Sharma Charu, Talla Sandhya P, Ojha Shreesh K
Department of Pharmacology, R. C. Patel Institute of Pharmaceutical Education and Research, North Maharashtra UniversityShirpur, India.
SVKM Institute of PharmacyDhule, India.
Front Pharmacol. 2017 Sep 21;8:656. doi: 10.3389/fphar.2017.00656. eCollection 2017.
Thymoquinone, a monoterpene molecule is chemically known as 2-methyl-5-isopropyl-1, 4-benzoquinone. It is abundantly present in seeds of L. that is popularly known as black cumin or black seed and belongs to the family . A large number of studies have revealed that thymoquinone is the major active constituent in oil this constituent is responsible for the majority of the pharmacological properties. The beneficial organoprotective activities of thymoquinone in experimental animal models of different human diseases are attributed to the potent anti-oxidant and anti-inflammatory properties. Thymoquinone has also been shown to alter numerous molecular and signaling pathways in many inflammatory and degenerative diseases including cancer. Thymoquinone has been reported to possess potent lipophilicity and limited bioavailability and exhibits light and heat sensitivity. Altogether, these physiochemical properties encumber the successful formulation for the delivery of drug in oral dosages form and restrict the pharmaceutical development. In recent past, many efforts were undertaken to improve the bioavailability for clinical usage by manipulating the physiochemical parameters. The present review aimed to provide insights regarding the physicochemical characteristics, pharmacokinetics and the methods to promote pharmaceutical development and endorse the clinical usage of TQ in future by overcoming the associated physiochemical obstacles. It also enumerates briefly the pharmacological and molecular targets of thymoquinone as well as the pharmacological properties in various diseases and the underlying molecular mechanism. Though, a convincing number of experimental studies are available but human studies are not available with thymoquinone despite of the long history of use of black cumin in different diseases. Thus, the clinical studies including pharmacokinetic studies and regulatory toxicity studies are required to encourage the clinical development of thymoquinone.
百里醌是一种单萜分子，化学名称为2-甲基-5-异丙基-1,4-苯醌。它大量存在于黑种草的种子中，黑种草俗称黑孜然或黑籽，属于黑种草属。大量研究表明，百里醌是黑种草油中的主要活性成分，该成分具有大部分药理特性。百里醌在不同人类疾病的实验动物模型中的有益器官保护活性归因于其强大的抗氧化和抗炎特性。百里醌还被证明可改变包括癌症在内的许多炎症和退行性疾病中的众多分子和信号通路。据报道，百里醌具有很强的亲脂性和有限的生物利用度，并且对光和热敏感。总之，这些物理化学性质阻碍了口服剂型药物递送的成功制剂，并限制了药物开发。最近，人们通过操纵物理化学参数进行了许多努力来提高临床应用的生物利用度。本综述旨在提供有关物理化学特征、药代动力学以及促进药物开发的方法的见解，并通过克服相关的物理化学障碍来支持未来百里醌的临床应用。它还简要列举了百里醌的药理和分子靶点以及在各种疾病中的药理特性和潜在分子机制。尽管有大量令人信服的实验研究，但尽管黑孜然在不同疾病中的使用历史悠久，但关于百里醌的人体研究却没有。因此，需要进行包括药代动力学研究和监管毒性研究在内的临床研究，以促进百里醌的临床开发。
