Antitussive and Anti-inflammatory Dual-active Agents Developed from Natural Product Lead Compound 1-Methylhydantoin

Abstract

Natural products play an important role in drug discovery. This work employed a natural product 1-methylhydantoin as the lead compound to develop novel dual-active drugs. 1-Methylhydantoin was isolated from Oviductus Ranae, which is a traditional Chinese medicine that has been used for tussive and inflammation treatment for a long time. An in silico study screened the more active 1-methylhydantoin derivatives. Antitussive assessment indicated that the newly synthesized agent had similar bioactivity with the natural product. An anti-inflammatory model used xylene induced ear edema model. At the same dosage (100 mg/Kg), the newly prepared agent had an inhibition rate 53.18% which was much higher than that of the lead compound (22.69%). The results might be ascribed to the cyclooxygenases-1 (COX-1) and cyclooxygenases-2 (COX-2) selectivity, and the fitness of the compound, and the binding pocket. The anti-particulate matter (PM 2.5) acute pneumonia was evaluated through an in vivo model constructed by nasal instillation with PM 2.5 suspension. The results of the above models suggested that this novel agent had remarkable antitussive, anti-inflammatory, and anti-PM 2.5 acute pneumonia activities.

Antitussive, Antioxidant, and Anti-Inflammatory Effects of a Walnut (Juglans regia L.) Septum Extract Rich in Bioactive Compounds

“…Natural products such as endogenous or exogenous metabolites of animals and plants, played a significant role in the discovery of medicines as more than half of the medicines in use were developed from natural products [ 1 ]. Famous examples are aspirin, a product derived from salicylic acid, present in the bark of several species of genus Salix [ 2 ], codeine, a naturally occurring alkaloid found in plants of Papaver spp.…”

Antioxidant Activity Evaluation of Oviductus Ranae Protein Hydrolyzed by Different Proteases

“…As the representative component of Oviductus Ranae , the protein content is much higher than most typical high-protein foods (for example, in typical high-protein foods, the protein content of poultry meat, fish and eggs is approximately 25%, 20%, 15%, respectively), so it is considered an ideal source for the production of antioxidant peptides. Anti-aging is one of the important traditional efficacies of Oviductus Ranae [ 27 , 28 ], and the aging process is mostly closely related to the production of excess ROS. Antioxidants can inhibit the production of ROS and remove excessive ROS, keeping the content of ROS at normal levels.…”

Rana chensinensis Ovum Oil Based on CO2 Supercritical Fluid Extraction: Response Surface Methodology Optimization and Unsaturated Fatty Acid Ingredient Analysis

“…In the Rana chensinensis industry, Rana chensinensis ovum (RCO) is the residual by-product in the production process of Oviductus Ranae ( Figure 1 ) [ 1 , 2 , 3 , 4 , 5 , 6 ]. Due to the relatively small amount of research on the by-products, RCO is usually treated as waste, causing serious wastage of Rana chensinensis resources.…”