Evaluation of selected natural sesquiterpenes as sensitizing agents of ß-lactam-resistant bacterial strains.

AIMS: To evaluate the capacity of fourteen sesquiterpenes to enhance the action of known antibiotics against two ß-lactam resistant strains, and to determine a possible mechanism of antibiotic sensitization by assessing their ability to inhibit a ß-lactamase enzyme. METHODS AND RESULTS: The broth microdilution method was used to determine the minimum inhibitory concentration (MIC) of ß-lactams cefuroxime (CEFM) and cefepime (CPM) against Staphylococcus aureus 23MR and Escherichia coli 82MR strains in the absence and presence of subinhibitory concentrations of fourteen natural sesquiterpenes. (1R,4R)-4H-1,2,3,4-tetrahydro-1-hydroxycadalen-15-oic acid (5), xerantolide (8), estafiatin (11), and ambrosin (12) exhibited the best sensitizing effects in both strains. These compounds were able to reduce the MIC of CEFM by 2-fold (from 15.0 to 7.5 µg/mL) and CPM by 15-fold (from 0.9 to 0.06 µg/mL) in S. aureus 23MR. For E. coli 82MR, the MIC of CEFM was reduced up to 8-fold (from 120.0 to 15.0 µg/mL). In this strain, the activity of 8 and 11 surpassed that of clavulanic acid (positive reference), which reduced the MIC of CEFM from 120.0 to 60.0 µg/mL. To elucidate a possible mechanism of antibiotic sensitization, molecular docking studies were conducted with ß-lactamases. These studies revealed an affinity with the enzymes (energies > -4.93 kcal/mol) by the formation of hydrogen bonds with certain conserved amino acid residues within the active sites. However, the in vitro results indicated only marginal inhibition, with percentages <50%. CONCLUSIONS: The bioevaluations indicate that nine of fourteen sesquiterpenes enhance the action of CEFM and CPM against the ß-lactam resistant strains, and these compounds displayed moderate activity as inhibitors of ß-lactamase.

Antimicrobial activity of some macroalgae of the Veracruzano Reef System (SAV), Mexico.

The study of macroalgae antimicrobial agents is limited to Mexico and scarce in the Veracruzano Reef System (SAV). It is necessary to devote efforts towards this field of applied phycology. The aim was to evaluate the antimicrobial activity of some phyla of Rhodophyta, Chlorophyta and Ochrophyta from SAV. Methanolic extracts from 23 marine macroalgae species (7 Chlorophyta, 4 Phaeophyta and 12 Rhodophyta) from the Veracruzano Reef System (SAV) (Mexico) were evaluated for antimicrobial activity. Antibacterial and antifungal activity were assessed by agar diffusion and agar dilution methods. The differences between mean values obtained for experimental groups was done by analysis of variance (ANOVA multifactorial model), p-values of 0.001 or less were considered statistically significant. Two new records are recognized for SAV (Laurencia gracilis and Sebdenia flabellata) and Compsothamnion thuioides for the Gulf of Mexico coasts. 16 species showed antibacterial activity, of which Caulerpa sertularioides, Ulva lactuca and Laurencia obtuse had significant activity on Gram-positive bacteria. 43.7% belong to the phyla Chlorophyta (7 species), 50% Rhodophyta (8 species) and 6.25% Ochrophyta (1 species). This indicates that the extracts of the algae of the Rhodophyta and Chlorophyta are the ones that showed the greatest activity. Regarding the yeasts, 16.6% of the total algae collected were active in the different yeast strains. 43.7% belongs to Chlorophyta species and for Rhodophyta were 60%. The macroalgae with the highest antifungal activity were: Cymopolia barbata, Ulva lactuca and Laurencia gracilis. The macroalgae of the Veracruzano Reef System present antimicrobial activity. This study is the first investigation of macroalgae's bioactive components from SAV, where they could be sources for future medical applications.

Género Bursera: Una revisión de sus aspectos etnobotánicos, farmacológicos y fitoquímicos / Género Bursera: Uma revisão dos seus aspectosetnobotânicos, farmacológicos e fitoquímicos / Genus Bursera: A review of its ethnobotanical, pharmacological and phytochemical aspects

El género Bursera pertenece a la familia de las Burseráceas y ha sido usado en la medicina tradicional del continente americano para tratar diversos padecimientos. Las actividades farmacológicas más importantes reportadas para el género han sido la actividad citotóxica, antiinflamatoria, antimicrobiana y antioxidante, entre otras. Dentro de los compuestos fitoquímicos aislados, se destacan los terpenos, lignanos y flavonoides los cuales son responsables de sus diferentes propiedades medicinales. Los resultados de estas investigaciones validan el uso de las especies del género Bursera en la medicina tradicional y su potencial uso en la industria farmacéutica. (AU)

O género Bursera pertence à família Burseraceae e tem sido utilizado na medicina popular americana para o tratamento de diversas doenças. As atividades farmacológicas mais importantes relatadas para o género são as atividades citotóxica, antiinflamatória, antimicrobiana, antioxidante. Entre os compostos fitoquímicos isolados, predominam os terpenos, lenhanos e flavonóides, os quais são responsáveis pelas suas diferentes propriedades medicinais. Os resultados desta pesquisa validam o uso de espécies de Bursera na medicina tradicional e o seu potencial uso na indústria farmacêutica. (AU)

The Bursera genus belongs to the family Burseraceae and has been used in the american folk medicine to treat various diseases. The most important pharmacological activities reported for the genus have been cytotoxic, anti-inflammatory, antimicrobial and antioxidant activity among others. Among the isolated phytochemical compounds, terpenes, lignans and flavonoids are predominant which are responsible for their different medicinal properties. The results of this research validate the use of Bursera species in traditional medicine aand their potential use in the pharmaceutical industry. (AU)

3ß-Palmitoyloxy-olean-12-ene analogs from Sapium lateriflorum (Euphorbiaceae): Their cytotoxic and anti-inflammatory properties and docking studies.

Ten compounds, including a new anti-inflammatory acyl triterpene, 3ß-palmitoyloxy-1ß,11α-dihydroxy-olean-12-ene, were isolated from the bioactive organic extract prepared from the leaves of Sapium lateriflorum (syn: S. nitidum). The isolated compounds were screened for their cytotoxic activity against selected human cancer cell lines and did not display significant activity. They were also evaluated as anti-inflammatory agents in mouse models (TPA-induced edema in the ear and in a carrageenan-induced paw edema model). The results indicated that the new compound, 3ß-palmitoyloxy-1ß,11α-dihydroxy-olean-12-ene, was the compound with major anti-inflammatory activity similar to that of indomethacin, being the hydroxyl at C-11 important for the observed activity. The results of docking studies of the 3ß-palmitoyloxy esters of olean-12-ene with NF-κB and with COX-2 receptors were consistent with possible molecular mechanisms of the anti-inflammatory activity.

Evaluation of the Antimicrobial Activity of Some Components of the Essential Oils of Plants Used in the Traditional Medicine of the Tehuacán-Cuicatlán Valley, Puebla, México.

In Tehuacán-Cuicatlán valley (Mexico), studies have been carried out on the essential oils of medicinal plants with antimicrobial activity and it was found that they present compounds in common such as: α-pinene, ß-pinene, carvacrol, eugenol, limonene, myrcene, ocimene, cineole, methyl salicylate, farnesene, and thymol. The goal of this study was to assess the antimicrobial activity of essential oils' compounds. The qualitative evaluation was carried out by the Kirby Baüer agar diffusion technique in Gram-positive bacteria (11 strains), Gram-negative bacteria (18 strains), and yeasts (8 strains). For the determination of the minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), the agar dilution method was used. All the evaluated compounds presented antimicrobial activity. The compounds eugenol and carvacrol showed the largest inhibition zones. Regarding yeasts, the compounds ocimene, cineole, and farnesene did not show any activity. The compounds eugenol, carvacrol, and thymol presented the lowest MIC; bactericidal effect was observed at MIC level for S. aureus 75MR, E. coli 128 MR, and C albicans CUSI, for different compounds, eugenol, carvacrol, and thymol. Finally, this study shows that the essential oils of plants used by the population of Tehuacán-Cuicatlán valley share compounds and some of them have antibacterial and fungicidal activity.

Medicinal plants of Oaxaca, Mexico: ethnobotany and antibacterial activity / Plantas medicinales de Oaxaca, México: etnobotánica y actividad antibacteriana

Santiago Quiotepec, one of the oldest communities of the Tehuacán-Cuicatlán Valley (México), has a great tradition using medicinal plants. The aim of this study was to make an inventory of the medicinal species used by the inhabitants of Santiago Quiotepec and evaluate the antibacterial activity. An ethnobotanical study of medicinal plants was carried out, 60 informants mentioned that 66 species of plants are being used in the treatment of different diseases. Fifteen species were selected to evaluate the antibacterial activity in possible bacterial originated diseases treatment. The lowest values were presented in the hexane extract of Plumbago pulchella, with a MIC of 0.25 mg/mL over Staphylococcus aureus and S. epidermidis as well as the hexanic extract of Echinopterys eglandulosa showed a MIC of 0.25 mg/mL over Pseudomona aeruginosa.

Santiago Quiotepec es una de las comunidades más antiguas del valle de Tehuacán-Cuicatlán (México), y tiene una gran tradición en el uso de plantas medicinales. El objetivo de este estudio fue realizar un inventario de las especies medicinales utilizadas por los habitantes de Santiago Quiotepec y evaluar la actividad antibacteriana. Se realizó un estudio etnobotánico de plantas medicinales, 60 informantes mencionaron 66 especies de plantas utilizadas en el tratamiento de diferentes enfermedades. Quince especies utilizadas en la comunidad para tratar enfermedades de posible origen bacteriano fueron seleccionadas para evaluar la actividad antibacteriana. Los valores más bajos se presentaron en el extracto hexánico de Plumbago pulchella, con una CMI de 0.25 mg/ml sobre Staphylococcus aureus y S. epidermidis, así como el extracto hexánico de Echinopterys eglandulosa mostró una CMI de 0.25 mg/mL sobre Pseudomona aeruginosa.

Photoprotection of Buddleja cordata extract against UVB-induced skin damage in SKH-1 hairless mice.

BACKGROUND: In recent years, there has been considerable interest in using botanical agents to prevent skin damage resulting from solar UV-irradiation. Buddleja cordata is a plant that is known as "tepozan". Some people in Mexico use the leaves of this plant to treat tumours, abscesses, sores and burns. The purpose of this study is to investigate the photoprotective properties of Buddleja cordata methanolic extract (BCME) against UVB-induced skin damage in SKH-1 hairless mice at the macroscopic and histological levels. METHODS: BCME was characterised to determine its spectroscopic, chromatographic and antioxidant (DPPH, superoxide and hydroxyl radicals) properties. To conduct the photoprotection studies, BCME was applied topically to the skin of SKH-1 mice before acute exposure to UVB for 10 minutes. The murine skin samples were used for macroscopic and histological studies to assess tissue damage. Penetration of active components of BCME into stratum corneum on the dorsal area of mice was investigated in vivo by the tape stripping method. Moreover, genotoxicity of BCME was evaluated in a Vicia faba cell root micronucleus model. RESULTS: BCME displayed absorbance over the entire UVB spectrum, and its principal components included verbascoside and linarin. BCME exhibited antioxidant activity and significantly scavenged hydroxyl radicals. BCME reduced erythema, sunburn cell production, vessel congestion and epidermal thickening of UVB irradiated mouse skin. BCME penetrate the skin of mice. BCME did not exhibit genotoxic activity in the micronucleus test. CONCLUSION: The topical administration of BCME protected against acute UVB-induced damage in mouse SKH-1 skin, and our results suggest that BCME may potentially prevent photodamage.