Antifungal, antibiofilm, and antiproliferative activities of Guapira graciliflora Mart

Abstract: The aim of this study was to evaluate in vitro the antifungal, antibiofilm and antiproliferative activities of the extract from the leaves of Guapira graciliflora Mart. The phytochemical characterization of the extract was performed using electrospray ionization mass spectrometry (ESI-MS). The antimicrobial activity of the extract and its fractions was evaluated using the broth microdilution method against species of Candida. The inhibition of C. albicans biofilm was evaluated based on the number of colony-forming units (CFU) and metabolic activity (MTT). The antiproliferative activity of the extract and its fraction was evaluated in the presence of human tumor and non-tumor cells, and the cytotoxicity of the extract was determined on the RAW 264.7 macrophage line - both using the sulforhodamine B method. The phytochemical characterization indicated the presence of the flavonoids rutin and kaempferol. The extract and the methanol fraction exhibited moderate antifungal activity against C. albicans, C. krusei, and C. glabrata, and strong activity against C. dubliniensis. In the biofilms at 24 and 48 hours, the concentration of 12500 µg/mL of the extract was the most effective at reducing the number of CFU s/mL (44.4% and 42.9%, respectively) and the metabolic activity of C. albicans cells (34.6% and 52%, respectively). The extract and its fractions had no antiproliferative effect on the tumor lines tested, with mean activity (log GI50) equal to or greater than 1.71 µg/mL. Macrophage cell viability remained higher than 80% for concentrations of the extract of up to 62.5 µg/mL. G. graciliflora has flavonoids in its chemical composition and demonstrates potential antifungal and antibiofilm activity, with no evidence of a significant change in the viability of human tumor and non-tumor cell lines.

Punarnavine, an alkaloid isolated from ethanolic extract of Boerhaavia diffusa Linn. reverses depression-like behaviour in mice subjected to chronic unpredictable mild stress.

Punarnavine (20 and 40 mg/kg) and fluoxetine (20 mg/kg) per se administered orally for 14 successive days significantly decreased immobility periods of both unstressed and stressed mice in forced swim test. These drugs also significantly decreased sucrose preference in both stressed and unstressed mice as compared to their respective controls, indicating significant antidepressant-like activity. The drugs did not show any significant effect on locomotor activity of mice. The alkaloid also significantly decreased monoamine oxidase (MAO-A) activity, malondialdehyde levels in both unstressed and stressed mice; and significantly reversed the stress-induced decrease in reduced glutathione and catalase activity. It also significantly attenuated the stress-induced increase in plasma nitrite and corticosterone levels. Thus, punarnavine showed antidepressant-like activity in unstressed and stressed mice probably through inhibition of brain MAO-A activity, decrease in plasma nitrite levels and due to its antioxidant activity. In addition, punarnavine also showed antidepressant-like activity in stressed mice possibly through decrease in plasma corticosterone levels.

Behavioural and neuroendocrine effects of aqueous extract of Boerhaavia diffusa Linn. in mice using tail suspension and forced swim tests – A preliminary study.

The present study was done to evaluate the effect of aqueous extract of B. diffusa on depression in mice using behavioral models such as tail suspension test (TST) and forced swim test (FST). The extract (50, 100 and 200 mg/kg, po) was administered for 14 successive days to Swiss young albino mice. On 14th day, 60 min after administration, mice were subjected to TST and FST. The administration of aqueous extract of B. diffusa (50, 100 and 200 mg/kg, po) significantly decreased immobility period in both TST and FST, indicating significant antidepressant-like activity. The lowest dose (50 mg/kg) of the extract decreased the immobility period most significantly in FST, showing most potent antidepressant-like action. The efficacy of the extract (50 mg/kg) was comparable to fluoxetine (20 mg/kg). The extract did not show any significant effect on locomotor activity. The extract showed significant monoamine oxidase -A inhibitory activity. There was no significant effect of the extract on plasma corticosterone levels. Prazosin (α1-adrenoceptor antagonist), sulpiride (selective D2-receptor antagonist), baclofen (GABAB agonist), and p-CPA (tryptophan hydroxylase inhibitor) significantly attenuated the extract-induced antidepressant-like effect, when tested in TST. The extract might produce antidepressant-like effect by interaction with α1-adrenoceptors, dopamine-D2 receptors, serotonergic, and GABAB receptors. Thus, aqueous extract of B. diffusa showed significant antidepressant-like activity in mice probably through involvement of monoaminergic and GABAergic systems.

Antioxidant status in polycystic end-staged renal diseased patients and antihemolytic effect of Boerhaavia diffusa.

Chronic renal failure (CRF) induces anaemia by shortening the life-span of erythrocytes, due to an increase in oxidative stress, which is considered to be one of the major risk factors in CRF patients undergoing hemodialysis. In the present study, the antioxidant status of the end-staged renal disease (ESRD) patients was investigated. The antihemolytic activity of Boerhaavia diffusa on the erythrocytes of the patients was also studied. Protein, lipid peroxides (LPO), reduced glutathione (GSH) levels and glutathione peroxidase (GPX) and glutathione-S-transferase (GST) activities were measured in the hemolysate from 55 polycystic ESRD patients (Group II) and compared with normal subjects (Group I). The antioxidant status was found to be significantly reduced in the patients as compared to normal healthy volunteers, due to increased oxidative stress. Also, aqueous extract of B. diffusa showed a significant antihemolytic activity on the erythrocytes of the polycystic ESRD patients.  

Estudio de secado por aspersión hasta escala de banco del extracto acuoso de Boerhaavia erecta L / Study of spray drying of water extract from Boerhaavia erecta L

Introducción: la utilización de los extractos obtenidos a partir de las plantas se difunde cada vez más en la industria farmacéutica para la fabricación de numerosos productos. Para su obtención en forma de polvo, se emplea el secado por aspersión por ser un método de secado que preserva los componentes naturales presentes en estos productos. La presencia de compuestos como los azúcares impide que estos productos puedan ser secados por aspersión sin que se adhieran a las superficies internas del equipo, lo que produce bajo rendimiento en su recuperación. El uso de aditivos inertes como almidón, ciclodextrinas, lactosa y maltodextrina, favorece la recuperación del producto, porque actúan como coadyuvantes del secado. Objetivos: determinar la concentración de aditivo que permite alcanzar el mayor rendimiento en el secado del extracto acuoso de Boerhaavia erecta L. Métodos: se estudió la influencia del uso de diferentes aditivos sobre el rendimiento en el proceso de secado por aspersión. Resultados: se logró obtener a escala de banco un extracto seco que cumple con los requisitos de calidad fisicoquímicos y microbiológicos, con un rendimiento superior a 90 por ciento. Conclusiones: la presencia de aditivos en el proceso de secado del extracto de B. erecta eleva el rendimiento y se obtuvo un producto que cumple con los requisitos de calidad establecidos.

Introduction: the use of plant extracts increasingly extends in the pharmaceutical industry for the manufacture of many products. To obtain them in powder form, the spray drying is employed because it is a method that preserves the natural components of these products. The presence of compounds like sugars makes the spray drying of these products difficult since they adhere to the internal surface of the equipment and this brings about low rate of product recovery. Use of inert additives such as starch, cyclodextrines, lactose and maltodextrine favors recovery of product because they act as drying coadjuvants. Objectives: to determine the additive concentration that allows reaching the highest performance in drying water extract from Boerhaavia erecta L. Methods: the influence of several additives on the performance of the spray drying process was researched. Results: it was possible to obtain at the test bed dry extract that fulfils the physical, chemical and microbiological quality requirements, with over 90 percent performance. Conclusions: the presence of additives in the process of B. erecta extract drying increases the performance and the final product fulfils the set quality requirements.

A dehydrorotenoid produced by callus tissue culture and wild plant roots of Boerhaavia coccinea

Calli cultures were established from leaves and stem of B. coccinea plantlet produced in vitro and analysed for isoflavonoid content. The quantification of 6,9,11-trihydroxy-6a,12a-dehydrorotenoid isolated from the roots of Boerhaavia coccinea P. Miller collected from its natural environment, and the same metabolite produced in callus tissue culture of the same plant are described in this paper. The rotinary quantitative HPLC analysis indicated that callus culture produced the same isoflavonoid compound found in the roots of intact wild growing plant. The amount of the secondary metabolite produced in vitro was 955.35 µg/g of dry cell weight, 2.5 times more than the highest amount concentration produced by the wild growing plant in its natural environment.

Cultura de calos foram estabelecidos de folhas e galhos finos de plântula de B. coccinea produzida in vitro e analisada para isoflavonóide. A quantificação do 6,9,11-triidroxi-6a,12a-desidro-rotenóide isolado das raízes de B. coccinea P Miller, coletada em seu habitat natural, e do mesmo rotenóide produzido na cultura de células estão descritos neste artigo. A análise rotineira em CLAE mostrou que a cultura de calos produziu o mesmo isoflavonóide encontrado nas raízes da planta do campo. A quantidade do metabólito secundário produzido in vitro foi de 955.35 µg/g de massa seca de callus, atingindo uma concentração de 2,5 vezes maior do que a quantidade do metabólito produzido pela planta em seu meio ambiente natural.

Inhibitory effect of the plant Boerhavia diffusa l. against the dermatophytic fungus Microsporum fulvum.

Antifungal activity (reduction in colony diameter) of various extracts (pt. ether, chloroform, ethyl acetate, ethyl alcohol and aqueous) of aerial and root parts of Boerhavia diffusa (Nictaginaceae) was screened against dermatophytic fungi Microsporum fulvum. Statistically significant increase has been recorded in the % inhibition of the target fungal species with increasing test concentrations (1000-5000 ppm) of chloroform, ethyl acetate and ethyl alcohol extracts of the root. The maximum % inhibition observed in various solvent extracts of root was about 26% (chloroform), 46% (ethyl alcohol) and 57% (ethyl acetate) at 5000 ppm concentration with time exposure of 10 days. The colony diameter of the target mycelial colony decreased with increasing supplementation of the phytoextract, showing the presence of significant amount of some antifungal phytochemical moiety.

Antifungal activity of Boerhavia diffusa against some dermatophytic species of Microsporum.

Various extracts petroleum ether, chloroform, ethyl acetate and ethyl alcohol) of aerial and root parts of Boerhavia diffusa was sereened for Antitungal activity (Inhibition in sporulation) against dermatophytic fungi Microsporum gypseum, M. fulvum and M. canis by using broth dilution method. Extracts of aerial part not show any noticeable antifungal activity. Ethyl acetate extract of root part of the plant was found to be most effective of against target fungal species. The maximum inhibition of mycelial growth was observed for M. gypseum (78.83%) followed by M. fulvum (62.33%) and M. canis (42.30%) of ethyl acetate in the test concentration of 1000 microg/ml 24 hours of incubation. The sporulation of target fungal species decreases with increasing supplementation of phytoextract, confirms the presence of some antifungal phytochemical moiety in roots of the plant.