Enzymatic Synthesis of Austroeupatol Esters with Enhanced Antiprotozoal Activity.

Austroeupatol, the principal diterpene isolated from the invasive shrub , holds promise for structural diversification and biological assessment of its derivatives due to its abundant availability and high yield isolation. We propose an efficient enzymatic synthesis of a series of austroeupatol esters derived from aliphatic and heterocyclic carboxylic acids. Systematic optimization of reaction parameters, including enzyme type and quantity, acylating agent amount, solvent, and temperature, was conducted.

Plant Extracts and Phytochemicals from the Asteraceae Family with Antiviral Properties.

Asteraceae (Compositae), commonly known as the sunflower family, is one of the largest plant families in the world and includes several species with pharmacological properties. In the search for new antiviral candidates, an in vitro screening against dengue virus (DENV) was performed on a series of dichloromethane and methanolic extracts prepared from six Asteraceae species, including , , , , , and , along with pure phytochemicals isolated from Asteraceae: mikanolide (), eupatoriopicrin (), eupahakonenin B (), minimolide (), estafietin (), 2-oxo-8-deoxyligustrin (), santhemoidin C (), euparin (), jaceidin (), nepetin (), jaceosidin (), eryodictiol (), eupatorin (), and 5-demethylsinensetin (). Results showed that the dichloromethane extracts of and and the methanolic extracts prepared from and were highly active and selective against DENV-2, affording EC values of 0.

Antiprotozoal compounds from Mikania periplocifolia (Asteraceae).

Chagas disease, African trypanosomiasis and Leishmaniasis are neglected parasitic diseases which affect millions of people worldwide. In a previous work, we report the antiprotozoal activity of the dichloromethane extract of Mikania periplocifolia Hook. & Arn.

toxicologic profile and trypanocidal activity of estafietin, a sesquiterpene lactone isolated from Stevia alpina Griseb.

Chagas disease is an infection caused by the protozoan affecting 6-8 million people worldwide. Only two drugs are available for its treatment, having a limited efficacy and adverse side-effects. Estafietin is a sesquiterpene lactone isolated from with activity against and low cytotoxicity against mammalian cells.

Anti- Properties of Sesquiterpene Lactones Isolated from spp.: In Vitro and In Silico Studies.

species (Asteraceae) have been a rich source of terpenoid compounds, mainly sesquiterpene lactones, several of which show antiprotozoal activity. In the search for new trypanocidal compounds, var. and were studied.

Enzymatic synthesis of amlodipine amides and evaluation of their anti- activity.

Advancing with our project about the development of new antiparasitic agents, we have enzymatically synthesized a series of amides derived from amlodipine, a calcium channel blocker used as an antihypertensive drug. Through lipase-catalyzed acylation with different carboxylic acids, nineteen amlodipine derivatives were obtained, eighteen of which were new compounds. To optimize the reaction conditions, the influence of several reaction parameters was analyzed, finding different requisites for aliphatic carboxylic acids and phenylacetic acids.

Mode of action of the sesquiterpene lactones eupatoriopicrin and estafietin on Trypanosoma cruzi.

Background: The sesquiterpene lactones (STLs) eupatoriopicrin (EP) and estafietin (ES), isolated from Stevia alpina Griseb. (Asteraceae) and Stevia maimarensis (Hieron.) Cabrera (Asteraceae) respectively, have previously showed promising trypanocidal activity, both in vitro and in vivo.

Antiprotozoal Compounds from (Asteraceae).

The dewaxed dichloromethane extract of and the compounds isolated from it were tested for their activity on epimastigotes and promastigotes. The extract of showed activity against both parasites with IC values of 7 g/mL and 31 g/mL, respectively. Fractionation of the dichloromethane extract led to the isolation of euparin, jaceidin, santhemoidin C, and eucannabinolide.

Trypanocidal Activity of Four Sesquiterpene Lactones Isolated from Asteraceae Species.

The sesquiterpene lactones eupatoriopicrin, estafietin, eupahakonenin B and minimolide have been isolated from Argentinean Astearaceae species and have been found to be active against epimastigotes. The aim of this work was to evaluate the activity of these compounds by analyzing their effect against the stages of the parasites that are infective for the human. Even more interesting, we aimed to determine the effect of the most active and selective compound on an model of infection.

Activity of Estafietin and Analogues on and .

Sesquiterpene lactones are naturally occurring compounds mainly found in the Asteraceae family. These types of plant metabolites display a wide range of biological activities, including antiprotozoal activity and are considered interesting structures for drug discovery. Four derivatives were synthesized from estafietin (), isolated from (Asteraceae): 11βH,13-dihydroestafietin (), epoxyestafietin ( and ), 11βH,13-methoxyestafietin, () and 11βH,13-cianoestafietin.