Abstract
This study aimed to study the in vitro antioxidant activity and cytotoxicity on tumor cells lines of six synthetic substances derived from riparins. All the substances showed antioxidant activity and riparins C, D, E, F presented cell growth inhibition rates greater than 70%, suggesting that these molecules have antitumor properties. These substances also caused greater than 80% releases of cytoplasmic lactate dehydrogenase enzyme (LDH). Although the antioxidant and antitumor properties presented herein require further assessment, the outcomes indicate that these novel riparins are promising biologically active compounds.
Highlights
The synthesis of new substances with pharmacological activity a great challenge frequently approached by the conversion of medicinal plant products into medicines
The riparins Rip A-F were identified and their structures elucidated by information acquired by 1H-NMR and 13C-NMR, respectively, (Tables 1 and 2)
Zucc., Cenostigma macrophyllum Tul. var. acuminata Teles Freire, Qualea grandiflora Mart.), did not show differences in their potential to scavenge free radicals [18], while the riparins, besides their low availability, have demonstrated promising bioactivities in in vitro antioxidant tests and to bioprospect pharmacological products that promote protection against cell disorders caused by oxidative stress
Summary
The synthesis of new substances with pharmacological activity a great challenge frequently approached by the conversion of medicinal plant products into medicines. The synthesis of these substances and their derivatives frequently allows the pharmacophore to be established and modulation of biological profiles, representing an excellent opportunity to explore the biological actions of these synthetic and semi-synthetic organic compounds [4] The response to this increasing demand for structurally innovative substances for pharmacological evaluation has established a new paradigm in the search for prototype compounds and in the optimization/development of pre-existing ones, recognizing sustainable use of the Brazilian biodiversity and development of a national industry and ensuring access and appropriate usage of medicinal plants, phytotherapics and their analogues by the population [5]. Using the Schotten Bauman reaction, some riparin derivatives were prepared and named riparins A and B, and by the condensation of the corresponding metallated esters with substituted phenethylamines, riparins C, D, E and F were obtained (Scheme 1) These analogues were obtained using a simple and reliable method that makes feasible the commercial exploitation of these molecules by the pharmaceutical industry in face of the low availability of the selected substance in natural sources [9]. The cytotoxic effects of the riparins on the viability of three tumor cells lines were evaluated by MTT colorimetric assays and cytoplasmic enzyme lactate dehydrogenase (LDH) level measurements in order to screening their antitumor potential
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