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.
Highlights
Natural products (NPs) and drugs have been linked to each other for thousands of years [1,2,3].natural product product (NP) are referred to the constituents or metabolites of animals, plants, insects, marine organisms and microorganisms, as well as many endogenous chemical components in animals, which are characterized by structural diversity and easy to bind to biological macromolecules [4,5,6,7]
NPs are referred to the constituents or metabolites of animals, plants, insects, marine organisms and microorganisms, as well as many endogenous chemical components in animals, which are characterized by structural diversity and easy to bind to biological macromolecules [4,5,6,7]
The antitussive drug codeine was prepared using morphine, a natural product isolated from Papaver somniferum, as the lead compound [12]
Summary
Natural products (NPs) and drugs have been linked to each other for thousands of years [1,2,3]. Pacific yew in 1971 and used for the treatment of lung cancer, breast cancer, ovarian cancer, cervical cancer, and pancreatic cancer [13,14,15]. Theisolation anti-malarial drug quinine wascompounds first isolatedfrom fromnatural the bark of a cinchona tree [16].a. Currently, the isolation of biologically active compounds from natural products has become a popular interest in the development of new drugs. Using the active ingredients from natural molecules, medicines medicines as development the lead compounds can greatly improve the hit rateisolated of newly designed as the lead greatly improve the hit rate of newly designed molecules, contract the contract thecompounds developing can cycle, and avoid the high development cost of chemical synthetic drugs [17–.
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