Background Understanding the mechanisms, activated and inhibited pathways as well as other molecular targets involved in existing and emerging disease conditions provides useful insights into their proper diagnosis and treatment and aids drug discovery, development and production. G protein-coupled receptors (GPCRs) are one of the most important classes of targets for small-molecule drug discovery. Of all drug targets, GPCRs are the most studied, undoubtedly because of their pharmacological tractability and role in the pathophysiology as well as the pathogenesis of human diseases. Main body of the abstract GPCRs are regarded as the largest target class of the “druggable genome” representing approximately 19% of the currently available drug targets. They have long played a prominent role in drug discovery, such that as of this writing, 481 drugs (about 34% of all FDA-approved drugs) act on GPCRs. More than 320 therapeutic agents are currently under clinical trials, of which a significant percentage targets novel GPCRs. GPCRs are implicated in a wide variety of diseases including CNS disorders, inflammatory diseases such as rheumatoid arthritis and Crohn’s disease, as well as metabolic disease and cancer. The non-olfactory human GPCRs yet to be clinically explored or tried are endowed with perhaps a huge untapped potential drug discovery especially in the field of immunology and genetics. Short conclusion This review discusses the recent advances in the molecular pharmacology and future opportunities for targeting GPCRs with a view to drug development.
Buchholzia coriacea Engl. is a medicinal plant belonging to the family Capparidaceae. It has antimicrobial, anthelmintic, antidiabetic and antihypercholesterol activities. The aim of this study was to employ the quality control parameters in the evaluation of the leaf of B. coriacea. The plant leaves were collected, air dried, pulverized and stored in a clean glass container. Standard procedures were carried out to obtain the microscopic features of the fresh and powdered samples, micromeritic, chemomicroscopy, fluorescence properties, soluble extractive values, moisture contents and ash values. The results of the microscopic study using fresh and powdered leaf samples revealed the presence of anomocytic stomata on the abaxial surface (hypostomatic) with mean length of 31.8 ± 0.6 cm. The cell shape was polygonal and straight anticlinal cell wall pattern. Results of the micromeritic properties of the powdered sample showed bulk volume of 31.00± 0.70cm, tapped volume of 25.1± 0.20 cm, bulk density of 0.32 ± 0.01g/m, tapped density of 0.39± 0.01g/ml, flow rate of 2.2 ± 0.08g/s, angle of repose of 26.1 ± 1.3 degrees, Carr’s index of 18.9± 1.35 %, Hausner’s ratio of 1.23 ± 0.02, pH of 8.0 when cold and 8.2 when hot for the powdered sample liquid extract. The results of the chemomicroscopic study revealed the presence of lignin, mucilage, calcium oxalate crystals, oil, calcium carbonate, but starch was absent. Results for the ethanol-soluble extractive value was 7 ± 0.00% , water-soluble extractive value was 14 ± 0.00% and methanol-soluble extractive value was 3 ± 0.00% for the powdered samples. Results for the moisture content was 10.3 ± 0.00% , total ash values was 6.3± 0.00% , acid-insoluble ash value was 1 ± 0.00% , water-soluble ash value was 3±0.00% and sulfated ash values was 7.5 ± 0.00% . In conclusion, the above evaluation methods and parameters there in could be used to identify and authenticate both the fresh and powdered crude drug product of Buchholzia coriacea.
Jatropha tanjorensis J.L. Ellis & Saroja. (Euphorbiaceae) is a shrub commonly used as an edible vegetable and is also used as a tonic herb. The study was aimed to evaluate pharmacognostic parameters of Jatropha tanjorensis leaves. The plant leaves were collected, air-dried, pulverized and stored in a clean glass container. Standard procedures were employed to obtain the microscopic features of the fresh and powdered samples, micromeritic, chemomicroscopy, fluorescence properties, moisture content, ash values and soluble extractive values were also carried out. The results of the microscopic studies using the fresh and powered leaf samples revealed the presence of anomocytic, anomalous and paracytic stomata on the abaxial surface and anomocytic stomata on the adaxial surface. The plant sample also possessed unicellular trichomes. Results of micromeritic properties of the powdered samples show bulk volume of 38.67±0.7, tapped volume of 30.00±0.4, bulk density of 0.26±0.00, tapped density of 0.33±0.00, angle of repose of 350, Carr’s Index of 22.96±2.15, Hausner’s ratio of 1.27±0.03, pH of 7.51 and 7.52 when hot and cold respectively. Chemomicroscopy studies revealed the presence of lignin, mucilage, calcium oxalate crystals, starch and oil in the powdered leaf. Results for moisture contents was 18.33±0.01% w/w, total ash value was 9.33±0.00%w/w, acid-insoluble ash value was 0.67±0.01%w/w, water-soluble ash value was 4.0±0.00%w/w and sulfated ash value was 14±0.01%w/w. Results for ethanol-soluble extractive value was 15±0.00%w/w, methanol-soluble extractive value was 19±0.00%w/w and water-soluble extractive value was 27±0.01%w/w. In conclusion, the above evaluation and parameters could be used to establish pharmacopoeial standard of both fresh and powdered drug of Jatropha tanjorensis.
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