Green Chromatographic Methods and in Vitro Pharmacological Analysis of Varronia curassavica Leaf Derivatives.

Varronia curassavica displays anti-inflammatory, antiulcerogenic, and antioxidant activities. Herein, we employed new UHPLC -UV green chromatographic methods for the analysis of in vitro antioxidant and anti-inflammatory activities of V. curassavica and its embryotoxicity in Zebrafish. Cordialin A, brickellin, and artemetin were purified from the ethanol (EtOH) extract of V. Curassavica leaves and identified using spectrometric techniques. In line with Green Analytical Chemistry principles, the proposed UHPLC methods involve the use of ethanol as organic modifier with low mobile phase consumption, and without sample pretreatment (OLE-UHPLC-UV). The application of the Agree and HPLC-EAT tools for greenness assessment yielded this pattern: HPLC-UV (reference)

Casearia Essential Oil: An Updated Review on the Chemistry and Pharmacological Activities.

Casearia species are found in the America, Africa, Asia, and Australia and present pharmacological activities, besides their traditional uses. Here, we reviewed the chemical composition, content, pharmacological activities, and toxicity of the essential oils (EOs) from Casearia species. The EO physical parameters and leaf botanical characteristics were also described. The bioactivities of the EOs from the leaves and their components include cytotoxicity, anti-inflammatory, antiulcer, antimicrobial, antidiabetic, antioxidant, antifungal, and antiviral activities. The main components associated with these activities are the α-zingiberene, (E)-caryophyllene, germacrene D, bicyclogermacrene, spathulenol, α-humulene, ß-acoradiene, and δ-cadinene. Data on the toxicity of these EOs are scarce in the literature. Casearia sylvestris Sw. is the most studied species, presenting more significant pharmacological potential. The chemical variability of EOs components was also investigated for this species. Caseria EOs have relevant pharmacological potential and must be further investigated and exploited.

Identification of azaphilone derivatives of Monascus colorants from Talaromyces amestolkiae and their halochromic properties.

Currently, the ability to produce several kinds of water-soluble red natural colorants makes the genus Talaromyces particularly important to the dye industry, which can be an alternative to the use of harmful synthetic colorants. In this study, colored compounds produced by Talaromyces amestolkiae were extracted, characterized chemically and the color stability of the fermented broth without any extraction procedure was further evaluated over pH variation. Five azaphilones compounds were detected by Ultrahigh Performance Liquid Chromatography-Mass Spectrometry system, all being complexes of the fatty acid amino-hexanedioic acid and azaphilone Monascus colorants. The color of the fermented broth was stable at a wide range of pH (3-9). Furthermore, T. amestolkiae colorants precipitated through hydrolysis of key chemical groups at extremely acidic (pH 1) and lose red color in extremely basic (pH 13) medium, showing negative halochromism. Nevertheless, these findings enhance the industrial relevance of azaphilone colorants produced by biotechnological process.

Growth-inhibitory effects of tris-(1,10-phenanthroline) iron (II) against Mycobacterium tuberculosis in vitro and in vivo.

Mycobacterium tuberculosis is the major etiological agent for tuberculosis (TB), which is the leading cause of single pathogen infection-related deaths worldwide. The End TB Strategy of the World Health Organization aimed to decrease the incidence of TB by 20% between 2015 and 2020, which was not achieved. Here, the growth-inhibitory effects of tris-(1,10-phenanthroline) iron (II) complex ([Fe(phen)3]2+), a known commercially available cheap chemical substance, were examined. The best in vitro results showed great activity with MIC ranging from 0.77 to 3.06 µM against clinical strains and at low pH (mimicking the granuloma) with MIC of 0.21 µM. Preliminary safety analysis revealed that the complex did not exhibit cytotoxic activity against different cell lines or mutagenic activity in vitro. The complex was orally bioavailable after 2 h of administration in vivo. Additionally, the results of the acute toxicity test revealed that the complex did not exert toxic effects in female BALB/c mice. The mechanism of action was performed using D29 mycobacteriophages where the treatment with different concentrations of the complex inhibited viral protein synthesis, which indicated that the anti-TB mechanisms of the complex involve protein synthesis inhibition. These findings suggested that [Fe(phen)3]2+ is a potential novel therapeutic for TB.

Improved in vitro and in vivo Anti-Candida albicans Activity of Cymbopogon nardus Essential Oil by Its Incorporation into a Microemulsion System.

PURPOSE: Vulvovaginal candidiasis (VVC) is an opportunistic fungal infection that adversely affects a woman's health, due to unpleasant symptoms, therapeutic challenges, and the emergence of resistant strains. The association of natural products and nanotechnology is important to improve the antifungal potential of medicinal plants. We aimed to evaluate the in vitro and in vivo anti-Candida albicans activity of unloaded (EO) and loaded (ME+EO) essential oil of Cymbopogon nardus in the microemulsion (ME). METHODS: The chemical analysis of the EO was performed by gas chromatography-mass spectrometry. The ME and ME+EO were characterized by scattering, zeta potential, polarized light microscopy, rheological assays, mucoadhesiveness and transmission electronic microscopy. The in vitro antifungal activity of the EO and ME+EO were evaluated by microdilution technique. The toxicity of EO and ME+EO was analyzed on human cell line HaCat and using alternative model assay with Artemia salina. The experimental in vivo VVC was performed in female mice (C57BL/6). RESULTS: The main compounds of the EO were found to be citronellal, geranial, geraniol, citronellol, and neral. The formulations exhibited suitable size, homogeneity, negative charge, isotropic behavior, highly organized structure, and pseudoplastic behavior, for vaginal application. TEM photomicrographs showed possible EO droplets inside the spherical structures. The EO, when loaded into the ME, exhibited an improvement in its antifungal action against C. albicans. The EO was not toxic against brine shrimp nauplii. An in vivo VVC assay showed that the use of the ME significantly improved the action of the EO, since only the ME+EO promoted the eradication of the fungal vaginal infection on the third day of treatment. CONCLUSION: The EO and ME+EO are promising alternatives for the control of fungal infections caused by C. albicans, once the use of nanotechnology significantly improved the antifungal action of the EO, especially in an in vivo model of VVC.