The outbreak of coronavirus disease-2019, caused by severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) is a worldwide emerging crisis. Polyphenols are a class of herbal metabolites with a broad-spectrum antiviral activity. However, most polyphenols encounter limited efficacy due to their poor solubility and degradation in neutral and basic environments. Thus, the effectiveness of their pharmaceutical application is critically dependent on the delivery systems to overcome the aforementioned drawbacks. Herein, Polyphenols-rich
Cuphea ignea
extract was prepared and its constituents were identified and quantified. Molecular docking was conducted for 15 compounds in the extract against SARS-CoV-2 main protease, among which rutin, myricetin-3-
O
-rhamnoside and rosmarinic acid depicted the most promising antiviral activity. Further, a self-nanoemulsifying formulation, composed of 10% oleic acid, 40% tween 20 and propylene glycol 50%, were prepared to improve the solubility of the extract components and enable its concurrent delivery permitting combined potency. Upon dilution with aqueous phases, the formulation rapidly form nanoemulsion of good stability and excellent dissolution profile in acidic pH when compared to the crude extract. It inhibited SARS-CoV-2 completely
in vitro
at a concentration as low as 5.87 μg/mL presenting a promising antiviral remedy for SARS-CoV-2, which may be attributed to the possible synergism between the extract components.
Cuphea ignea A. DC. is
an ornamental
tropical plant belonging to the family Lythraceae. The aim of this
study is to verify the in vivo antihypertensive potential
of C. ignea A. DC. and to explore its
metabolic profile using a UHPLC-Orbitrap-HRMS technique. The results
revealed that the ethanolic extract of the leaves in two doses (250
and 500 mg/kg b.wt.) significantly normalized the elevated systolic
blood pressure in N(G)-nitro-l-arginine-methyl ester-induced
hypertension in rats. An angiotensin-converting enzyme (ACE) concentration
was significantly decreased by the high dose extract compared to lisinopril.
Nitric oxide (NO) level was significantly restored by both doses.
Concerning the oxidative stress parameters, both doses displayed significant
reduction in malondialdehyde (MDA) level while the high dose restored
elevated glutathione level. These biochemical results were clearly
supported by the histopathological examination of the isolated heart
and aorta. A UHPLC-Orbitrap-HRMS study was represented by a detailed
metabolic profile of leaves and flowers of C. ignea A. DC., where 53 compounds were identified among which flavonoids,
fatty acids, and hydrolysable tannins were the major identified classes.
This study established scientific evidence for the use of C. ignea A. DC., a member of genus Cuphea as a complementary treatment in the management of hypertension.
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