The Evaluation of Phenolic Acids and Flavonoids Content and Antiprotozoal Activity of Eryngium Species Biomass Produced by Biotechnological Methods

Three species from the Eryngium L. genus—E. campestre, E. maritimum, and E. planum, plants with a rich chemical composition, were selected for phytochemical and biological studies. The applied biotechnological methods allowed to obtain the biomass of these rare or protected species in the form of multiplied shoots (stationary system) and roots cultured in a liquid medium (agitated system). In the extracts from the raw material obtained under in vitro conditions, the content of selected phenolic acids and flavonoids (HPLC-DAD method) as well as the total of polyphenols (Folin–Ciocalteu assay) were quantified. The highest amount of all phenolic compounds was found in extracts from E. planum roots (950.90 ± 33.52 mg/100 g d.w.), and the lowest from E. campestre roots (285.00 ± 10.07 mg/100 g d.w.). The quantitatively dominant compound proved to be rosmarinic acid. The highest amounts were confirmed for E. planum root extract (694.58 mg/100 g d.w.), followed by E. planum (388.95 mg/100 g d.w.) and E. campestre (325.85 mg/100 g d.w.) shoot extracts. The total content of polyphenols was always increased in the biomass from in vitro cultures in comparison to the analogous organs of intact plants of each species. The obtained extracts were assessed for antiprotozoal activity against Acanthamoeba sp. The strength of biological activity of the extracts correlated with the content of phenolic compounds. To our knowledge, this is the first report on the amoebicidal activity of E. campestre, E. maritimum, and E. planum extracts from biomass produced by biotechnological methods.

An overview of the synthetic route to the marketed formulations of pyrimidine: A Review

: Pyrimidine and its derivatives are a very important class of heterocyclic compounds that show interesting applications in the field of medicinal chemistry. Pyrimidine not only plays an important role as an organic reaction intermediate but also has a wide range of interesting biological activities viz. antibacterial, antifungal, anticancer, anti-inflammatory, antiviral, and antiprotozoal activity, etc. Numerous methods are available for the formation of pyrimidine derivatives have been reported in the literature. The advantage of pyrimidine as a starting material for different therapeutically potent derivatives has given momentum to this research. This review aims to report the new work on the synthesis of marketed drugs which consist of pyrimidine moiety.

Synthesis and antiprotozoal activity of 2-phenoxy derivatives of pyridine

The aim of the present work is to synthesize phenoxypyridine derivatives and to screen substances with a high level of biological activity within the series of synthesized compounds, which is essential for solving the problem of overcoming the growing drug resistance of bacteria and protozoa. The interaction of 2-chloro-5-nitro- and 2-chloro-3-nitro-pyridine with aromatic aldehydes containing phenolic hydroxyl gave 15 pyridine series aryl ethers in high yields when reacted in dimethylformamide (DMFA) or dimethyl sulfoxide (DMSO) in the presence of bases. In the reaction we used phenolic derivative of kojic acid (compound 1 of Table 1), a number of benzene series aldehydes with different substituents: 3-methoxy-4-hydroxybenzaldehyde (compound 2 of Table 1), 4-hydroxybenzaldehyde (compound 3 of Table 1), 2,4-dihydroxybenzaldehyde (compound 5 of Table 1), 3-methoxy-4-hydroxybenzaldehyde (compound 7 of Table 1 ), salicylic aldehyde (compound 11 of Table 1), 3,4-dihydroxybenzaldehyde (compound 12 of Table 1), vanillin (compound 13 of Table 1), and compound 15 (Table 1) of the benzene series with two hydroxyl and aldehyde groups. As well as benzene-type aldehydes, the methyl ester of salicylic acid (compound 4 of Table 1), 4-hydroxymethylphenol (compound 6 of Table 1), 4-acetylphenol (compound 8 of Table 1), and 3-hydroxy benzoic acid (compound 14 of Table 1) were used. In the reaction, in addition to the above compounds, 7-hydroxycoumarin (compound 9 of Table 1) and semicarbazide-4-hydroxybenzaldehyde (compound 10 of Table 1) were also used. Their purification was performed by recrystallization from organic solvents (ethyl acetate, benzene, ethanol, and isopropanol). The obtained compounds were studied as part of the institute's search for compounds to expand the range of active substances with protistoсid and antibacterial activity with low toxicity. Synthesized compounds have pronounced antiprotozoal activity against Colpoda steinii. the most active compound contains a nitro group in the 3rd position of the pyridine ring as well as an aldehyde and hydroxyl group in the benzene ring. The minimum protistocidal concentration of this compound is 0.9 µg/ml, which is 60 fold more active than toltrazuril and 8 fold more active than chloroquine. This compound is recommended for extended toxicological and pharmacological studies.

Natural and synthetic naphthoquinones as potential anti-infective agents

Background: Naphthoquinones are a class of aromatic compounds relevant for their chemical characteristics, structural properties, and biological activity. These compounds are found in nature with a wide range of effects, highlighting their antibacterial, antifungal, and antiprotozoal properties. Additionally, naphthoquinones are used as a scaffold to obtain new derivatives with pharmacological potential, mainly compounds against parasitic diseases. Objective: The purpose of this work was to carry out a comprehensive review of naphthoquinones and their derivatives obtained from both natural and synthetic sources, also, to well as analyze their biological activity against Leishmania spp (Leishmaniasis), Trypanosoma cruzi (Chagas disease), Plasmodium falciparum (Malaria), Toxoplasma gondii (Toxoplasmosis), and Toxocara canis (Toxocariasis). All of these agents are responsible for relevant diseases worldwide. Results : Natural naphthoquinones, such as plumbagin, diospyrin, burmanin, lapachol, lawsone and psychorubrin, show an antiprotozoal activity similar or enhanced antiprotozoal activity to reference drugs. Some naphthoquinones obtained by synthesis or semi-synthesis shown better biological activity or less toxic effects than natural compounds. Conclusion: In this review, natural and synthetic naphthoquinone showed antiparasitic activity, in the most cases with improved results than current drugs currently used in clinical trials. A modification of their structure with different functional groups can enhance their biological effects, improve solubility, and reduce undesirable side effects. Therefore, naphthoquinones are important molecules in the development of new chemotherapeutic agents against parasitic diseases.

Antiparasitic Effects of Potentially Toxic Beetles (Tenebrionidae and Meloidae) from Steppe Zones

Arthropods and specifically beetles can synthesize and/or sequester metabolites from dietary sources. In beetle families such as Tenebrionidae and Meloidae, a few studies have reported species with toxic defensive substances and antiparasitic properties that are consumed by birds. Here we have studied the antiparasitic activity of extracts from beetle species present in the habitat of the Great Bustard (Otis tarda) against four pathogen models (Aspergillus niger, Meloidogyne javanica, Hyalomma lusitanicum, and Trichomonas gallinae). The insect species extracted were Tentyria peiroleri, Scaurus uncinus, Blaps lethifera (Tenebrionidae), and Mylabris quadripunctata (Meloidae). M. quadripunctata exhibited potent activity against M. javanica and T. gallinae, while T. peiroleri exhibited moderate antiprotozoal activity. The chemical composition of the insect extracts was studied by gas chromatography coupled with mass spectrometry (GC-MS) analysis. The most abundant compounds in the four beetle extracts were hydrocarbons and fatty acids such as palmitic acid, myristic acid and methyl linoleate, which are characteristic of insect cuticles. The presence of cantharidin (CTD) in the M. quadripunctata meloid and ethyl oleate (EO) in T. peiroleri accounted for the bioactivity of their extracts.

Furanocoumarins from Ruta chalepensis with Amebicide Activity

Entamoeba histolytica (protozoan; family Endomoebidae) is the cause of amoebiasis, a disease related to high morbidity and mortality. Nowadays, this illness is considered a significant public health issue in developing countries. In addition, parasite resistance to conventional medicinal treatment has increased in recent years. Traditional medicine around the world represents a valuable source of alternative treatment for many parasite diseases. In a previous paper, we communicated about the antiprotozoal activity in vitro of the methanolic (MeOH) extract of Ruta chalepensis (Rutaceae) against E. histolytica. The plant is extensively employed in Mexican traditional medicine. The following workup of the MeOH extract of R. chalepensis afforded the furocoumarins rutamarin (1) and chalepin (2), which showed high antiprotozoal activity on Entamoeba histolytica trophozoites employing in vitro tests (IC50 values of 6.52 and 28.95 µg/mL, respectively). Therefore, we offer a full scientific report about the bioguided isolation and the amebicide activity of chalepin and rutamarin.