Biotechnological, Nutritional, and Therapeutic Applications of Quinoa (Chenopodium quinoa Willd.) and Its By-Products: A Review of the Past Five-Year Findings.

This study aimed to provide an updated critical review of the nutritional, therapeutic, biotechnological, and environmental aspects involved in the exploitation of Chenopodium quinoa Willd and its biowastes. Special attention was devoted to investigations of the therapeutic and nutritional properties of different parts and varieties of quinoa as well as of the use of the biowaste resulting from the processing of grain. Studies published from 2018 onward were prioritized. Extracts and fractions obtained from several Chenopodium quinoa matrices showed antioxidant, antidiabetic, immunoregulatory, neuroprotective, and antimicrobial effects in in vitro and in vivo models and some clinical studies. The activities were attributed to the presence of phytochemicals such as polyphenols, saponins, peptides, polysaccharides, and dietary fibers. Quinoa wastes are abundant and low-cost sources of bioactive molecules for the development of new drugs, natural antioxidants, preservatives, dyes, emulsifiers, and carriers for food and cosmetics applications. Among the demands to be fulfilled in the coming years are the following: (1) isolation of new bioactive phytochemicals from quinoa varieties that are still underexploited; (2) optimization of green approaches to the sustainable recovery of compounds of industrial interest from quinoa by-products; and (3) well-conducted clinical trials to attest safety and efficacy of extracts and compounds.

Discovery of Lead 2-Thiazolylhydrazones with Broad-Spectrum and Potent Antifungal Activity.

Opportunistic fungal infections represent a global health problem, mainly for immunocompromised individuals. New therapeutical options are needed since several fungal strains show resistance to clinically available antifungal agents. 2-Thiazolylhydrazones are well-known as potent compounds against Candida and Cryptococcus species. A scaffold-focused drug design using machine-learning models was established to optimize the 2-thiazolylhydrazone skeleton and obtain novel compounds with higher potency, better solubility in water, and enhanced absorption. Twenty-nine novel compounds were obtained and most showed low micromolar MIC values against different species of Candida and Cryptococcus spp., including Candida auris, an emerging multidrug-resistant yeast. Among the synthesized compounds, 2-thiazolylhydrazone 28 (MIC value ranging from 0.8 to 52.17 µM) was selected for further studies: cytotoxicity evaluation, permeability study in Caco-2 cell model, and in vivo efficacy against Cryptococcus neoformans in an invertebrate infection model. All results obtained indicate the great potential of 28 as a novel antifungal agent.

Cellular Antioxidant, Anti-Inflammatory, and Antiproliferative Activities from the Flowers, Leaves and Fruits of Gallesia integrifolia Spreng Harms.

Gallesia integrifolia, a notable species in the Atlantic Forest, has been traditionally employed in folk medicine for treating rheumatism, asthma, and worms. This study investigated the cellular antioxidant, antiproliferative, and anti-inflammatory activities of the essential oils (EOs) and crude extracts (CEs) from G. integrifolia flowers, fruits, and leaves. The chemical identification of EOs was performed by GC-MS and CEs by UHPLC-MS. Cellular antioxidant and anti-inflammatory activities were assessed through mouse macrophage cell culture. In addition, the antiproliferative potential was evaluated in gastric, colorectal, breast, and lung tumor cell lines and non-tumor VERO cells. EOs predominantly contained organosulfur compounds in flowers (96.29%), fruits (94.94%), and leaves (90.72%). We found the main compound is 2,2'-Disulfanediyldiethanethiol in the EOs of flowers (47.00%), leaves (41.82%), and fruits (44.39%). Phenolic compounds were identified in CEs. The EOs and CEs demonstrated potential against the tumor cell lines tested (GI50 between 51 and 230 µg/mL). The selectivity index values were greater than 1.0 (1.01 to 3.37), suggesting a relative safety profile. Moreover, the anti-inflammatory activity IC50 ranged from 36.00 to 268 µg/mL, and the cellular oxidation inhibition ranged from 69% to 82%. The results suggest that oils and extracts derived from G. integrifolia have potential for use in various industrial sectors.

Activity of essential oils from leaves, flower buds and stems of Tetradenia riparia on Rhipicephalus (Boophilus) microplus larvae.

Around the world, the main problems of livestock are caused by ectoparasites, however, commercial acaracide are toxic to the environment and detrimental to One Health. Therefore, research has increasingly focused on development of natural products as alternatives for tick control. The purpose of this study was to evaluate the larvicidal effect on Rhipicephalus (Boophilus) microplus, through use of essential oils (EOs) extracted from the leaves, flower buds and stems of Tetradenia riparia. The chemical composition of these EOs was determined through gas chromatography coupled to mass spectrometry (GC-MS). They were tested on larvae at concentrations of 100.000 to 40 µg/mL, using the larval packet test and under semi-natural conditions. The main class of compounds in the chemical composition was sesquiterpenes (both oxygenates and hydrocarbons), whereas the predominant compounds in the leaves, flower buds and stems were 14-hydroxy-9-epi-caryophyllene, T-cadinol and 6-7-dehydroroyleanone, respectively. The leaves proved to be the most effective, with highest larvicidal activity (LC99.9 = 83.53 µg/mL). When tested under semi-natural conditions, the oils obtained efficiency above 98% in all compound tests. The results indicated that these EOs were effective against R. (B.) microplus larvae in vitro and ex-situ, proving that this plant has bioactive molecules with significant larvicidal activity.

Effects of dredging activities and seasonal variation on coastal plankton assemblages: results from 10 years of environmental monitoring.

Coastal zones support the most productive marine ecosystems, yet they are increasingly threatened by anthropogenic stressors such as dredging. In this study, we investigated how seasonal variation and dredging activities conducted during the construction of a harbor and submarine base (Sepetiba Bay, RJ, Brazil) affected the phytoplankton and zooplankton assemblages. The observed temporal variability at five different sites over 10 years revealed that dredging exceeds the expected influence of dry and rainy seasons on plankton abundance and diversity. In general, the abundance of both groups increased during dredging due to the resuspension of nutrients and benthic organisms. This increase was particularly evident in the dinoflagellate Scrippsiellaa cuminata, the diatoms Thalassiosira rotula and Nitzschia longissima, and the herbivorous zooplankton Acartia clausii and Pseudevadne tergestina. Moreover, season and dredging activities synergistically influenced plankton assemblages, resulting in larger seasonal variations during dredging activities. After the end of the harbor construction, plankton abundance decreased and remained low until the end of the monitoring, which may indicate persistent changes in the biodiversity and ecosystem functioning of impacted areas.

Evaluation of Probiotic Properties of Novel Brazilian Lactiplantibacillus plantarum Strains.

Beneficial effects of Lactiplantibacillus plantarum strains have been widely reported. Knowing that the effects of probiotic bacteria are strain-dependent, this study aimed to characterize the probiotic properties and investigate the gastrointestinal protective effects of nine novel L. plantarum strains isolated from Bahia, Brazil. The probiotic functionality was first evaluated in vitro by characterizing bile salt and acidic tolerance, antibacterial activity, and adhesion to Caco-2 cells. Antibiotic resistance profile, mucin degradation, and hemolytic activity assays were also performed to evaluate safety features. In vivo analyses were conducted to investigate the anti-inflammatory effects of the strains on a mouse model of 5-Fluorouracil-induced mucositis. Our results suggest that the used L. plantarum strains have good tolerance to bile salts and low pH and can inhibit commonly gastrointestinal pathogens. Lp2 and Lpl1 strains also exhibited high adhesion rates to Caco-2 cells (13.64 and 9.05%, respectively). Phenotypical resistance to aminoglycosides, vancomycin, and tetracycline was observed for most strains. No strain showed hemolytic or mucolytic activity. Seven strains had a protective effect against histopathological and inflammatory damage induced by 5-FU. Gene expression analysis of inflammatory markers showed that five strains upregulated interleukin 10 (Il10), while four downregulated both interleukin 6 (Il6) and interleukin 1b (Il1b). Additionally, all strains reduced eosinophilic and neutrophilic infiltration; however, they could not prevent weight loss or reduced liquid/ food intake. Altogether, our study suggests these Brazilian L. plantarum strains present good probiotic characteristics and safety levels for future applications and can be therapeutically adjuvant alternatives to prevent/treat intestinal mucositis.

The clinical effect of intravenous lipid emulsion on rabbits medicated with diazepam.

Intravenous lipid emulsions (ILE) have been increasingly used to reverse a wide range of lipophilic drug intoxications. However, it is still unknown if these emulsions interfere with other lipophilic drugs routinely used while treating intoxicated patients, such as diazepam, one of the main antiepileptic drugs. Therefore, the objective of the present study was to evaluate whether the administration of a 20% ILE interferes with diazepam's clinical effect. We randomly allocated thirty rabbits to five groups. Three of those groups received diazepam (1.0 mg/kg, IV), one of which did not receive any additional treatment, while the two remaining groups were treated with ILE or lactated ringer solution (1.5 mL/kg followed by 0.25 mL/kg/min for 30 min). The fourth group only received lipid emulsion, and the fifth only lactated ringer. Successive neurological exams at 20 min intervals for a total of 100 min were performed to assess the rabbits' neurological state. We concluded that the ILE did not interfere with diazepam's clinical effect but, although unlikely, the possibility of recurrence of a sedative effect should be considered.

Potential of Tetradenia riparia leaf essential oil and its fractions in controlling Aedes aegypti and Rhipicephalus microplus larvae

Tetradenia riparia (Hochst.) Codd (Lamiaceae) is a shrub, commonly known as ginger bush or false myrrh, and several studies have shown that T. riparia exhibits a variety of biological properties. This study aimed to determine the chemical composition of T. riparia essential oil and its fractions, investigate their anticholinesterase activity, and assess their larvicidal activity against the cattle tick Rhipicephalus microplus and the mosquito Aedes aegypti. Eleven essential oil fractions were obtained by fractionation and analyzed by gas chromatography/mass spectrometry. Larvicidal activity against R. microplus and third-instar A. aegypti was assessed using a larval packet test and a larval immersion test, respectively. Anticholinesterase activity was determined by a bioautographic method. Forty-nine compounds were identified in the essential oil, of which the major classes were oxygenated sesquiterpenes (45.95%) and sesquiterpene hydrocarbons (35.20%) and the major components were isospathulenol (17.40%), ß-caryophyllene (15.61%), 14-hydroxy-9-epi-caryophyllene (10.07%), 14-hydroxy-α-muurolene (8.32%), and 9ß,13ß-epoxy-7-abietene (5.53%). Bioassays showed that T. riparia essential oil (LC50 = 1.56 µg/mL) and FR3 (LC50 = 0.30 µg/mL) were the most active against R. microplus and A. aegypti larvae, respectively. The essential oil and FR1, FR2, and FR3 exhibited acetylcholinesterase inhibitory activity. These results indicate that T. riparia essential oil and its fractions hold promise in the development of novel, environmentally safe agents for the control of R. microplus and A. aegypti larvae.

Bioactive compounds with antifungal activity against pathogens isolated from pregnant woman: Gallesia integrifolia (garlic wood) is a promising treatment for vulvovaginal candidiasis.

ETHNOPHARMACOLOGICAL RELEVANCE: The leaves, bark, and roots of Gallesia integrifolia are consumed in folk medicine through infusion, decoction, and topical preparation by crushing because of its pharmacological properties in several peripheral system disorders, including microbial infections. The presence of various molecules in different parts of the plant likely confers this species' fungicidal action, but scientific evidence is lacking. Vulvovaginal candidiasis mainly affects women of reproductive age. When left untreated, it can cause pregnancy complications. Currently available antifungals often cause undesirable side effects. New alternative therapeutic strategies based on medicinal plants have been proposed. AIM: To investigate the antifungal activity of G. integrifolia against vulvovaginal candidiasis secretion in pregnant women. MATERIALS AND METHODS: Antifungal activity was determined by the minimum inhibitory concentration (MIC), determined by broth microdilution method using Candida spp (NEWP1210), C. albicans (CCCD-CC001), C. tropicalis (CCCD-CC002) standard and clinical isolates from pregnant women with vulvovaginal candidiasis. Nystatin and fluconazole were used as positive controls. The chemical composition of essential oils that were extracted from leaves, flowers, and fruits of G. integrifolia was determined by gas chromatography coupled to mass spectrometry. Reverse docking was used to suggest a possible target in Candida. Conventional docking was used to identify the most probable compound that inhibits fungal growth. RESULTS: A total of 24 compounds were identified, accounting for ∼99% of volatile constituents in the essential oils. Leaves of G. integrifolia contained 3,5-dithiahexanol-5,5-dioxide (40.93%), flowers contained methionine ethyl ester (46.78%), and fruits contained 2,8-dithianonane (54.01%) as the most abundant compounds. The MICs of essential oils of leaves, flowers, and fruits of G. integrifolia against standard strains of Candida spp, C. albicans, and C. tropicalis ranged from 13.01 to 625.00 µg/mL. The essential oil of flowers more effectively inhibited Candida spp. Essential oils of leaves and flowers were similar to fluconazole against C. albicans. Essential oils of flowers and fruits were similar to fluconazole against C. tropocalis. In Candida yeast species that were isolated from vaginal secretion samples from pregnant patients, the MICs of leaves and flowers ranged from 52.08 to 5000.00 µg/mL. The essential oil of leaves (277.77 µg/mL) was the most active against C. albicans. No significant differences were found between the essential oils of leaves and flowers against C. glabrata. Docking simulations suggested that phytol in leaves and flowers was responsible for the antimicrobial effect. CONCLUSION: The present results suggest the potential therapeutic use of G. integrifolia, especially its leaves and flowers, against Candida and vulvovaginal candidiasis.

Chemical analysis, antifungal and antimycotoxigenic activity of tetradenia riparia essential oil and crude extract.

Tetradenia riparia is known for its richness in essential oil which has been widely investigated due to its biological activities such as antimicrobial, insecticidal, trypanocidal, antimalarial and antioxidant. The objective of this work was to chemically analyze and evaluate the antifungal and antimycotoxigenic activity of the essential oil and the crude extract of leaves, flower buds and stems of T. riparia from the northwest region of the state of Paraná. The essential oil was obtained by hydrodistillation using a Clevenger-type apparatus. To obtain the crude extract, the leaves, flower buds and stems were pulverized and subjected to a dynamic maceration process using 70% v v-1 ethyl alcohol. Chemical analysis of the essential oil was performed by GC/MS, and chemical identification of the crude extract by UHPLC-ESI/qTOF. Antifungal activity (Rhizopus oryzae, Aspergillus flavus, Aspergillus ochraceus, Penicillium verrucosum and Fusarium graminearum) was performed by broth microdilution and the antimycotoxigenic assay was performed with A. ochraceus and P. verrucosum. Ochratoxin A was extracted by partition with chloroform and quantified by HPLC-FL. The oil yield was 0.29% for leaves, 0.34% for stems and 0.38% for flower buds, and the major compounds were fenchone, ß-caryophyllene, α-cadinol, 14-hydroxy-9- epi-caryophyllene, 9ß,13ß-epoxy-7-abietene, α-cadinol and 6-7-dehydroroyleanone. The main chemical compounds identified in the crude extract were terpenes, anthocyanins, flavonoids, tannins and phenolic acids. The minimum inhibitory concentration (MIC) of oils from leaves, flower buds and stems for the strains tested ranged from 0.87 mg mL-1 to 33.3 mg mL-1, while the minimum fungicidal concentration (MFC) ranged from 6.94 mg mL-1 and 33.3 mg mL-1. The MIC and MFC for ketoconazole, tebuconazole, sorbate and nitrite ranged from 0.05 to 33.3 mg mL-1. The oil and crude extract of leaves, stems and flower buds showed an inhibition of ochratoxin A production for P. verrucosum of approximately 100%.

Biopharmaceutical evaluation of kavain in Piper methysticum G. Forst dried extract: Equilibrium solubility and intestinal permeability in Caco-2 cell model.

ETHNOPHARMACOLOGICAL RELEVANCE: Piper methysticum G. Forst, popularly known as kava, is a traditional medicinal plant native from South Pacific islands and widely used to treat anxiety, depression and stress. The psychoactive properties are related to the kavalactones, mainly kavain. AIM OF THE STUDY: To evaluate the biopharmaceutical properties of synthetic kavain and when present in kava dried extracts by means of equilibrium solubility and intestinal permeability studies in the Caco-2 cell model. MATERIALS AND METHODS: The equilibrium solubility of kavain was performed using a shake flask incubator at 37 °C in different media at physiological pH range (1.2-6.8). The intestinal permeability of kavain evaluated in Caco-2 cells in the presence and absence of the P-glycoprotein inhibitor verapamil. Kavain concentrations were determined by reversed phase high performance liquid chromatography (HPLC). RESULTS: HPLC methods were developed and fully validated for kavain quantitation. Kavain demonstrated low solubility and the pH of the aqueous media did not affect its solubility. Kavain was found to be highly permeable and efflux of kavain mediated by P-glycoprotein was not significant during intestinal permeation. CONCLUSION: The results of biopharmaceutical studies provided useful information for predicting availability of kavain from the gastrointestinal tract and this compound was ranked as BCS Class II, exhibiting dissolution rate-limited absorption.

Influence of different preparation techniques on the composition and antioxidant action of curcumin and curcuminoids / Influencia de diferentes técnicas de preparación en la composición y acción antioxidante de la curcumina y los curcuminoides

Epidemiological evidence indicates that plant antioxidants activity can treat or help to prevent the development of various diseases. One species with great potential as an antioxidant is Curcuma longa. However, different extraction techniquescan influence isolated chemical compounds. This study investigated chemical composition and antioxidant activity of two rhizome extracts of C. longa: hydroethanolic, obtained by exhaustion (HECLex); and dried by a spray dryer (HECLsd). The phytochemical composition was evaluated by GC/MS. Antioxidant activity was evaluated using DPPH and FRAP assays. Total phenolic compounds and soil analyses were performed. The main components of HECLex were ar-turmerone, γ-curcumene, α-turmerone, and ß-sesquiphellandrene. The main components of HECLsd were 9,12,15-octadecatrienoic acid, 2, 3-bis([trimethylsilyl]oxy) propyl ester, verrucarol, and 1-monolinoleoylglycerol trimethylsilyl ether. HECLsd had significantly higher levels of phenolic compounds and higher antioxidant capacity compared with HECLex. In conclusion, processes of the preparation of C. longarhizomes alter the chemical components and consequently their biological activity.

La evidencia epidemiológica indica que la actividad de los antioxidantes de las plantas pueden tratar o ayudar a prevenir el desarrollo de diversas enfermedades. Una especie con gran potencial como antioxidante es Curcuma longa. Sin embargo, diferentes técnicas de extracción pueden influir en los compuestos químicos aislados. Este estudio investigó la composición química y la actividad antioxidante de dos extractos de rizoma de C. longa: hidroetanólico, obtenido por agotamiento (HECLex); y se seca con un secador por pulverización (HECLsd). La composición fitoquímica se evaluó mediante GC/MS. La actividad antioxidante se evaluó mediante ensayos DPPH y FRAP. Se realizaron análisis de suelos y compuestos fenólicos totales. Los componentes principales de HECLex fueron ar-turmerona, γ-curcumene, α-turmerone y ß-sesquiphellandrene. Los componentes principales de HECLsd fueron ácido 9,12,15-octadecatrienoico, éster 2,3-bis ([trimetilsilil] oxi) propílico, verrucarol y éter 1-monolinoleoilglicerol trimetilsilil. HECLsd tenía niveles significativamente más altos de compuestos fenólicos y mayor capacidad antioxidante en comparación con HECLex. En conclusión, los procesos de preparación de los rizomas de C. longa alteran los componentes químicos y consecuentemente su actividad biológica.

Larvicidal activity of Brunfelsia uniflora extracts on Aedes aegypti larvae.

The aim of this study was to evaluate the chemical composition and the larvicidal activity of Brunfelsia uniflora leaf and flower extracts against Aedes aegypti larvae. Twenty-four compounds were found in the leaf extract, and the major compounds were phytol (23.1%), 9,12,15-octadecatrienoic acid, ethyl ester (21.3%), and hexadecanoic acid, ethyl ester (12.8%). In the flower extract, twenty-four compounds were also identified and the major compounds were α-amyrin (35.7%), ß-amyrin (16.4%), and (EE)-geranyl linalool (9.6%) by gas chromatography coupled to mass spectrometry. The larvicidal activity was evaluated by larval immersion test. The lethal concentrations (LC) obtained from leaf extract were LC50 = 4.89 and LC99.9 = 11.14 mg/mL and from flower extract were LC50 = 3.82 and LC99.9 = 11.03 mg/mL, and the positive control presented LC50 = 0.40 and LC99.9 = 1.14 mg/mL. Thus, B. uniflora extracts are promising alternatives to control A. aegypti larvae.

Chemical composition of Tradescantia pallida (Rose) D.R. Hunt var. purpurea Boom (Commelinaceae) essential oil.

Tradescantia pallida is a herbaceous plant with promising compounds in its composition that can be applied in several areas such as agronomic, pharmaceutical and chemical. However, further studies on this plant are needed in order to characterise it phytochemically, pharmacologically and toxicologically. In this sense, the present study aimed to verify the unprecedented identification of its essential oil (EO) components. The EO extraction of T. pallida aerial parts was performed by hydrodistillation in a Clevenger apparatus (5 h), and the chemical analysis by gas chromatography coupled to mass spectrometry. The oxygenated sesquiterpene was the dominant class in EO composition and spathulenol (19.56%) was the principal identified compound, followed by caryophyllene oxide (18.84%), ß-caryophyllene (13.65%) and α-copaene (6.08%). The chemical identification of sesquiterpene compounds (oxygenated and hydrocarbons) in EO contributes to the understanding of the biological activities evidenced by T. pallida reported by literature.

Cytotoxicity and anti-inflammatory activities of Gallesia integrifolia (Phytolaccaceae) fruit essential oil.

The chemical composition of Gallesia integrifolia fruits essential oil was obtained by hydrodistillation using a modified Clevenger apparatus was investigated by gas chromatography coupled to mass spectrometry (GC/MS). In addition, the cytotoxicity activity against human tumor cell lines MCF-7 (breast adenocarcinoma), NCI-H460 (large cell lung carcinoma), HeLa (cervical carcinoma), and HepG2 (hepatocellular carcinoma), and non-tumor PLP2 (porcine liver primary cells) as well as the anti-inflammatory action was proposal. The compounds were predominantly organosulfates (2,8-dithianonane, dimethyl trisulfide, and lenthionine). Anti-inflammatory activity that provides 50% inhibition of nitric oxide production (55 µg/mL) of essential oil of the fruits. It also presents cytotoxic activity against MCF-7 (GI50 = 66 µg/mL), NCI-H-460 (GI50 = 147 µg/mL), HeLa (GI50 = 182 µg/mL) and HepG2 (GI50 = 240 µg/mL). The essential oil is more active in tumor cells than in non-tumor cells and the GI50 values for essential oil reported in our work support future studies.

Antimicrobial and antioxidant activities of secondary metabolites from endophytic fungus Botryosphaeria fabicerciana (MGN23-3) associated to Morus nigra L.

This study was to evaluate the biological activity of the extract of Botryosphaeria fabicerciana isolated from leaves of Morus nigra. The volatile compounds from the crude extract were analysed by GC-MS which demonstrate that mellein and ß-orcinaldehyde were are the major compounds. The best minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the extract was observed against Gram-positive bacteria, with a MIC of 15.6 µg/mL towards B. cereus and MIC of 62.5 µg/mL towards S. aureus and B. subtilis. MBC values of 31.25 µg/mL, 62.5 µg/mL, and 250 µg/mL were observed towards B. cereus, B. subtilis, and S. aureus, respectively. The cytotoxicity analyses showed CC50 of 115 µg/mL. The crude extract showed antioxidant activity by the DPPH, ABTS, and FRAP assays. Therefore, the extract of the endophytic fungus presented biotechnological potential as an antibacterial and antioxidant agent.

Recent Advances in the Prediction of Pharmacokinetics Properties in Drug Design Studies: A Review.

This review presents the main aspects related to pharmacokinetic properties, which are essential for the efficacy and safety of drugs. This topic is very important because the analysis of pharmacokinetic aspects in the initial design stages of drug candidates can increase the chances of success for the entire process. In this scenario, experimental and in silico techniques have been widely used. Due to the difficulties encountered with the use of some experimental tests to determine pharmacokinetic properties, several in silico tools have been developed and have shown promising results. Therefore, in this review, we address the main free tools/servers that have been used in this area, as well as some cases of application. Finally, we present some studies that employ a multidisciplinary approach with synergy between in silico, in vitro, and in vivo techniques to assess ADME properties of bioactive substances, achieving successful results in drug discovery and design.

Tetradenia riparia leaves, flower buds, and stem essential oils to control of Aedes aegypti larvae

Abstract Tetradenia riparia (Hochst.) Codd (Lamiaceae) is a species native to the African continent and used as an insect repellent. The objective of the study was to evaluate the larvicidal potential of essential oils (EOs) from the leaves, flower buds, and stem of T. riparia, collected in winter against Aedes aegypti larvae. The EOs were extracted by hydrodistillation (3 h) and identified by GC/MS. The EOs were tested against larvae of A. aegypti at concentrations ranging from 12500 to 1.5 µg/mL for 24 h. The insecticide activity was evaluated by probit analysis, and the anticholinesterase activity was determined by bioautographic method. The results of the class projection indicated sesquiterpenes as the majority class, corresponding to 60.66% (leaves), 64.70% (flower buds) and 83.99% (stem), and the bioassays on A. aegypti larvae indicated LC50 of 1590, 675 and 665 µg/mL, respectively. The anticholinesterase activity indicated that the EO of the leaves inhibited the enzyme at a concentration of 780 µg/mL, and those from the flower buds and stem inhibited up to 1560 µg/mL. The results indicated weak activity of essential oils against A. aegypti larvae.

Chemical composition and insecticidal activity of Garcinia gardneriana (Planchon & Triana) Zappi (Clusiaceae) essential oil / Composición química y actividad insecticida del aceite esencial de Garcinia gardneriana (Planchon & Triana) Zappi (Clusiaceae)

The present study aimed to analyze the chemical composition of the essential oil from Garcinia gardneriana (Planchon & Triana) Zappi leaves and fruits, and to determine its acaricidal activity on Rhipicephalus microplusy larval packet test and larvicidal action on Aedes aegyptiby larval immersion test. The chemical analysis of the essential oil by gas chromatography-mass spectrometry identified sesquiterpene hydrocarbons and oxygenated sesquiterpenes in bacupari leaves and fruits, and α-cedrene, α-chamigrene, α-trans-bergamotene, and ß-curcumene as major compounds. Essential oil from leaves of G. gardneriana presented acaricidal activity on R. microplus (LC50= 4.8 mg/mL; LC99= 10.8 mg/mL) and larvicidal effect on A. aegypti (LC50= 5.4 mg/mL; LC99 = 11.6 mg/mL), where as essential oil from the fruits of G. gardneriana showed LC50= 4.6 mg/mL and LC99= 8.9 mg/mL against R. microplus and LC50= 6.4 mg/mL and LC99= 13.9 mg/mL against A. aegypti. These results thus demonstrate the potential acaricidal and larvicidal activity of essential oil of G. gardneriana, offering new perspectives for the realization of bioassays from this essential oil.

El presente estudio tuvo como objetivo analizar la composición química del aceite esencial de las hojas y frutos de Garcinia gardneriana (Planchon & Triana) Zappi, y determinar su actividad acaricida en Rhipicephalus microplus y larvicida en Aedes aegypti empleando la prueba de inmersión de larvas. El análisis químico del aceite esencial por cromatografía de gases-espectrometría de masas identificó hidrocarburos sesquiterpénicos y sesquiterpenos oxigenados en hojas y frutos de bacupari, y α-cedreno, α-chamigreno, α-trans-bergamoteno y ß-curcumeno como compuestos principales. El aceite esencial obtenido de las hojas de G. gardneriana presentó actividad acaricida en la garrapata del ganado (LC50= 4,8 mg/mL; LC99= 10,8 mg/mL) y actividad larvicida en A. aegypti (LC50= 5,4 mg/mL; LC99= 11,6 mg/mL), así como, el aceite esencial obtenido de los frutos de G. gardneriana mostró LC50= 4,6 mg/mL y LC99= 8,9 mg/mL contra las larvas de garrapatas de ganado y LC50= 6,4 mg/mL y LC99= 13,9 mg/mL en las larvas de A. aegypti. Por lo tanto, estos resultados demuestran la actividad acaricida y larvicida del aceite essencial de G. gardneriana, ofreciendo nuevas perspectivas para la realización de bioensayos a partir de este aceite esencial.

Campomanesia xanthocarpa (Mart.) O. Berg essential oil induces antileishmanial activity and remodeling of the cytoplasm organelles.

Leishmaniasis is a neglected disease that affects millions of people worldwide. This study aimed to analyze antileishmanial activity of Campomanesia xanthocarpa leaf essential oil (EO) on promastigote and amastigote forms of Leishmania amazonensis, cytotoxicity in murine macrophages and sheep erythrocytes. The essential oil (EO) was analyzed by gas chromatography/mass spectrophotometry. The main and most abundant compounds were sesquiterpene hydrocarbons (71.22%) such as trans-caryophyllene (7.87%), bicyclogermacrene (11.28%), and δ-cadinene (8.34%). The IC50 for promastigote and amastigote forms of L. amazonensis was 70 µg mL-1 and 6 µg mL-1, respectively. C. xanthocarpa EO was not cytotoxic for murine macrophages (CC50 1860 µg mL-1) and sheep erythrocytes (1.5%), presenting high selectivity index for protozoan (310). C. xanthocarpa EO induced effects on the morphology and ultrastructure of this parasite. The high activity for intracellular amastigote forms, low toxicity to murine macrophages, and erythrocytes, suggest that C. xanthocarpa EO is promising for the treatment of leishmaniasis.