Therapeutic Potential and Pharmaceutical Development of Thymoquinone: A Multitargeted Molecule of Natural Origin

Abstract

Thymoquinone, a monoterpene molecule is chemically known as 2-methyl-5-isopropyl-1, 4-benzoquinone. It is abundantly present in seeds of Nigella sativa L. that is popularly known as black cumin or black seed and belongs to the family Ranunculaceae. A large number of studies have revealed that thymoquinone is the major active constituent in N. sativa 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.

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“…Medicine from natural sources is one the most important treatments, in addition to its use for medicinal, culinary, dietary, and curative purposes. Traditional and alternative source of medicines from plant sources are relied on for the development of good health and fewer side effects [9]. Camellia sinensis dried plant tea leaves are one of the most famous liquid refreshment drinks worldwide, followed similarly by water, which is the second most consumed [10].…”

Thymoquinone induces cell proliferation inhibition and apoptosis in acute myeloid leukemia cells: role of apoptosis-related WT1 and BCL2 genes

“…Many purified components extracted from medicinal plants have shown beneficial therapeutic potentials in the recent years and widely used as an alternative to chemical drugs. Thymoquinone (TQ), the major bioactive component of the essential oil of black seeds have shown promising inhibitory effects on a large number of solid and leukemia tumors through targeting several pathways such as those involved in cell cycle, apoptosis, ROS generation, metastasis and angiogenesis [21][22][23][24][25][26].…”

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“…TQ administered in the dose of 1 mg/kg body weight /day was mostly well tolerated 57 . There was no sign of toxicity except for the reduction in the amount of plasma glucose concentration in addition to TQ at concentrations up to 0.03% for 3 months in drinking water of rats 58 . The steady delivery of TQ for 30 days using Tri-Calcium Phosphate Lysine with 0.02 grams of TQ for adult male rats, showed very little or no side effect on reproductive organs 59 .…”