Anti-aging potential and anti-tyrosinase activity of three Hypericum species with focus on phytochemical composition by LC–MS/MS

In a search for new potential multitarget anti-HIV compounds from natural products, we have identified in Hypericum scruglii, an endemic and exclusive species of Sardinia (Italy), a potent plant lead. The phytochemical study of the hydroalcoholic extract obtained from its leaves led to the isolation of its most abundant secondary metabolites, belonging to different chemical classes. In particular, three phloroglucinols derivatives were identified, confirming their significance as chemotaxonomic markers of the Hypericum genus. Among them, the 3-(13-hydroxygeranyl)-1-(2'-methylbutanoyl)phloroglucinol was reported here for the first time. All six isolated compounds have been evaluated firstly for the inhibition of both Human Immunodeficiency Virus type 1 (HIV-1) Reverse Transcriptase (RT)-associated DNA Polymerase (RDDP) and Ribonuclease H (RNase H) activities, for the inhibition of HIV-1 integrase (IN) in biochemical assays, and also for their effect on viral replication. Among the isolated metabolites, three phloroglucinol derivatives and quercitrin were effective on both RT-associated RDDP and RNase H activities in biochemical assays. The same active compounds affected also HIV-1 IN strand transfer function, suggesting the involvement of the RNase H active site. Furthermore, phloroglucinols compounds, included the newly identified compound, were able to inhibit the HIV-1 replication in cell based assays.

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Prenylated phloroglucinols from Hypericum scruglii, an endemic species of Sardinia (Italy), as new dual HIV-1 inhibitors effective on HIV-1 replication.

Phenolic profile and biological activity of Hypericum perforatum L.: Can roots be considered as a new source of natural compounds?

Evaluation of in vitro biological activities of three Hypericum species (H. calycinum, H. confertum, and H. perforatum) from Turkey

Calendula officinalis L., (marigold), well known for its medicinal properties, has been extensively studied for its therapeutic properties. Nonetheless, as far as the literature could establish, no study has attempted to comparatively assess the biological (antioxidant and enzyme inhibitory potential) of the flowers, leaves, and roots of C. officinalis extracted using conventional (maceration and Soxhlet extraction (SE)) and non-conventional extraction (homogenizer (HAE) and ultrasound (UAE) assisted extraction) techniques. The detailed phytochemical profile of each extract along with the concentration of specific bioactive compounds has also been established. Total phenolic content was highest for the flower extracts while flavonoid content was highest in the leaf extracts. Phytochemical profiling showed that the extraction method influenced the phytochemical composition of the extract. Nicotiflorin was identified in the flower extracts only while amentoflavone occurred only in the roots, inferring that the occurrence of bioactive compounds varies within a plant. The flower extracts showed highest antioxidant potential while the roots extracts were potent inhibitors of cholinesterase and tyrosinase. This study provides valuable data on the influence of extraction techniques on the recovery of bioactive compounds from plants. In an endeavor to scale-up extraction from plant considering the more efficient extraction method is of paramount importance. Moreover, the study highlighted the necessity to thoroughly examine the biological activities of various parts of a plant obtained via different extraction protocols.

T. Yilmaz Ozden

Papers

Evaluation of chemical composition, antioxidant and anti-acetylcholinesterase activities of Hypericum neurocalycinum and Hypericum malatyanum