RESUMEN
Bacterial resistance to the antibiotics develops rapidly and is increasingly serious health concern in the world. It is an insoluble topic due to the multiple resistant mechanisms. The overexpression of relative activities of the efflux pump has proven to be a frequent and important source of bacterial resistance. Efflux transporters in the membrane from the resistant bacteria could play a key role to inhibit the intracellular drug intake and impede the drug activities. However, nanoparticles (NPs), one of the most frequently used encapsulation materials, could increase the intracellular accumulation of the drug and inhibit the transporter activity effectively. The rational and successful application of nanotechnology is a key factor in overcoming bacterial resistance. Furthermore, nanoparticles such as metallic, carbon nanotubes and so on, may prevent the development of drug resistance and be associated with antibiotic agents, inhibiting biofilm formation or increasing the access into the target cell and exterminating the bacteria eventually. In the current study, the mechanisms of bacterial resistance are discussed and summarized. Additionally, the opportunities and challenges in the use of nanoparticles against bacterial resistance are also illuminated. At the same time, the use of nanoparticles to combat multidrug-resistant bacteria is also investigated by coupling natural antimicrobials or other alternatives. In short, we have provided a new perspective for the application of nanoparticles against multidrug-resistant bacteria.
Asunto(s)
Infecciones Bacterianas , Nanotubos de Carbono , Animales , Antibacterianos/farmacología , Antibacterianos/uso terapéutico , Infecciones Bacterianas/tratamiento farmacológico , Infecciones Bacterianas/veterinaria , Farmacorresistencia Bacteriana Múltiple , NanotecnologíaRESUMEN
The purpose of the research was to examine the protective effect of essential oil from Thymus serrulatus Hochst. ex Benth. (TSA oil) against cadmium (Cd)-induced renal toxicity. The experimental protocol was designed using 30 healthy adult Wistar albino rats allocated into five groups containing six animals in each group. Group 1 was treated as normal control and groups 2, 3, 4, and 5 were treated with cadmium chloride (CdCl2, 3 mg/kg, IP) for 7 days. Group 3 was also treated with silymarin (100 mg/kg, PO) as a standard group, while groups 4 and 5 were administered with TSA oil at doses of 100 and 200 mg/kg PO, respectively. The nephrotoxicity was measured with various parameters such as kidney function markers, oxidative stress markers (glutathione (GSH) and malondialdehyde (MDA)), and messenger ribonucleic acid (mRNA) expression levels of inflammatory factors. The histological studies were also evaluated in the experimental protocol. The CdCl2-treated groups showed a significant increase in the levels of serum kidney function markers along with MDA levels in kidney homogenate. However, renal GSH level was found to be reduced significantly. It was found that CdCl2 significantly upregulated the nuclear factor levels of kappaB (NF-κB p65), inducible nitric oxide synthase (iNOS), and small mothers against decapentaplegic (Smad2) as compared to the normal control group. On the other hand, TSA oil significantly improved the increased levels of serum kidney function markers, non-enzymatic antioxidants, and lipid peroxidation. In addition, TSA oil significantly downregulated the increased expression of NF-κB p65, iNOS, and Smad2 in Cd-intoxicated rats. Moreover, the histological changes in the tissue samples of the kidney of Cd-treated groups were significantly ameliorated in the silymarin- and TSA-oil-treated groups. The present study reveals that TSA oil ameliorates Cd-induced renal injury, and it is also proposed that the observed nephroprotective effect could be due to the antioxidant potential of TSA oil and healing due to its anti-inflammatory action.
Asunto(s)
Enfermedades Renales/tratamiento farmacológico , Aceites Volátiles/química , Estrés Oxidativo/efectos de los fármacos , Thymus (Planta)/química , Animales , Antioxidantes/química , Antioxidantes/farmacología , Cadmio/toxicidad , Regulación de la Expresión Génica/efectos de los fármacos , Humanos , Riñón/efectos de los fármacos , Riñón/patología , Enfermedades Renales/inducido químicamente , FN-kappa B/genética , Óxido Nítrico Sintasa de Tipo II/genética , Aceites Volátiles/farmacología , Ratas , Proteína Smad2/genéticaRESUMEN
Otostegia fruticosa, a plant belonging to the family Lamiaceae, is endemic to Ethiopia. In Ethiopian traditional medicine, O. fruticosa has been used for the treatment of several respiratory-related disorders. The present study was designed to evaluate the bronchodilatory and antimicrobial activities of O. fruticosa leaves crude extract (Of.Cr). Ex-vivo experiments were conducted on guinea-pig trachea provided with physiological oxygenated buffer solution using emkaBath setup. The crude extract was analyzed by gas chromatography-mass spectrometry. Of.Cr, showed the presence of terpenes, fragrance components, saponins, and higher fatty acids. Of.Cr when tested on contracted tracheal chains with carbamylcholine (CCh, 1 µM) and high K+ (80 mM) produced relaxation by showing higher potency against CCh with incomplete inhibition of high K+. Dicyclomine, used as a positive control, also showed selectively higher potency to inhibit CCh when compared with its effect against K+. In the anticholinergic curves, Of.Cr at 1 mg/mL deflected CCh-induced concentration-response curves (CRCs) competitively to the right like dicyclomine (0.03 µM) and atropine whereas a higher dose of Of.Cr (3 mg/mL) produced a non-parallel shift in the CCh curves like a higher dose of dicyclomine (0.1 µM). In the calcium channel inhibitory assay, Of.Cr at 3 & 5 mg/mL, deflected CRCs of Ca++ to the right like verapamil, used as positive control. Of.Cr, at concentrations (1-3 mg/mL) increases cAMP levels in isolated tracheal homogenates, similar to positive control phosphodiesterase inhibitor (papaverine). When tested for antibacterial activity against standard and clinical strains, Of.Cr was found more active (MIC 475 µg/ml) against S. aureus (NCTC 6571), while the maximum inhibition (MIC 625 µg/ml) was observed by the extract when tested against MRSA. These results determine the mechanistic pathways of the observed bronchodilatory effect of Otostegia fruticosa with a combination of anticholinergic and dual inhibition of phosphodiesterase and voltage-gated Ca++ channels.
RESUMEN
The study was aimed to evaluate in vitro antioxidant, α-amylase inhibitory and in vivo antidiabetic activities of Myrica salicifolia root extracts. The powdered roots of M. salicifolia were extracted with 80% methanol and then dried. The dried extract was further fractionated into chloroform, ethyl acetate, butanol and aqueous fractions. The phytochemical screening of the crude extract was performed using standard chemical identification tests. The antioxidant activity of the extracts was determined by in vitro method using 2,2-diphenyl-1-picrylhydrazyl (DPPH) as radical scavenging reagent. The in vitro α-amylase inhibitory activity was performed using the chromogenic3,5-dinitrosalicylic (DNSA) method. The antidiabetic activity of M. salicifolia root crude extract (200, 400 and 600 mg/kg) and fractions (400 mg/kg) were evaluated in normal, glucose loaded hyperglycemic and streptozotocin (STZ)-induced diabetic mice. The crude root extract of M. salicifolia showed strong DPPH radical scavenging activity (IC50 = 4.54µg/ml) which was comparable with the standard antioxidant, ascorbic acid. In α-amylase inhibitory activity, the crude extract and butanol fraction showed highest enzyme inhibition. In the antidiabetic activity, daily administration of the crude extract, aqueous and butanol fractions for fifteen days showed highest significant reduction in fasting blood glucose level (BGL) compared to diabetic control in STZ-induced diabetic mice model. The root extract and fractions of M. salicifolia exhibited significant antihyperglycemic, α-amylase inhibitory and antioxidant activity with no sign of toxicity. The antidiabetic effect of the plant could be due to the synergistic effect of various classes of constituents present in the root part of the plant.
Asunto(s)
Diabetes Mellitus Experimental/inducido químicamente , Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/farmacología , Myrica/química , Extractos Vegetales/farmacología , Estreptozocina/farmacología , alfa-Amilasas/antagonistas & inhibidores , Animales , Antioxidantes/farmacología , Compuestos de Bifenilo/farmacología , Glucemia/efectos de los fármacos , Femenino , Masculino , Ratones , Fitoquímicos/farmacologíaRESUMEN
Background: Various indigenous medicinal systems including Ethiopians used Cyphostemma adenocaule for managing tumors, helminthiasis, snake envenomation, rabis virus, splenomegaly, and other immunological disorders. However, no scientific study was conducted to validate these traditional medicinal claims of the plant. Therefore, this study aimed to evaluate the in-vivo immunomodulatory activity of the crude root extract and its solvent fractions. Methods: Carbon clearance rate and humoral antibody titer were determined for 100, 200, and 400 mg/kg of crude extract and solvent fractions among Swiss albino mice. Carbon ink and sheep red blood cells were used as antigens for carbon clearance assay and humoral antibody titer respectively. Results: Among all groups, an increase in both carbon clearance rate and the humoral antibody titer was observed with an increase in the dose of both crude extract and solvent fractions. Compared to the solvent fractions of comparable doses, the crude extract showed better activity. The crude extract at a dose of 400 mg/kg revealed the highest and statistically significant augmentation of carbon clearance rate (0.1100 ± 0.0124) and humoral antibody titer (96.00 ± 14.31) compared to the vehicle control group. Conclusion: From our study, it is concluded that crude extract and n-butanol fraction showed promising immunostimulant activity by enhancing carbon clearance rate and humoral antibody titer.
RESUMEN
INTRODUCTION: Cyphostemma adenocaule (Steud. ex A. Rich) Descoings ex wild & Drummond (Vitaceae) has been used in traditional medicine for the management of various immunological and hematological disorders in different areas of Ethiopia and the rest of the world. In Ethiopia, the plant is used for the management of enlarged spleen, rabies virus, helminthic infection, snake bite, and various types of tumors. OBJECTIVE: To evaluate the effect of hydroethanolic root extract and solvent fractions of Cyphostemma adenocaule on cell-mediated immunity (delayed-type hypersensitivity), organ index (spleen and liver), and blood cell count in Swiss albino mice. MATERIALS AND METHODS: Acute oral toxicity test was conducted using nulliparous and nonpregnant Swiss albino mice following OECD 425 limit test method. Delayed-type hypersensitivity model was used to evaluate the effect on cell-mediated immunity. The experimental animals were divided into twelve groups which were sensitized and challenged with sheep red blood cells on day 0 and day 7, respectively. Levamisole 50 mg/kg was used as stimulant control, whereas cyclophosphamide 30 mg/kg was used as suppressant control. Hydroethanolic root extract (100 mg/kg, 200 mg/kg, and 400 mg/kg), aqueous fraction (100 mg/kg, 200 mg/kg, and 400 mg/kg), and n-butanol fraction (100 mg/kg, 200 mg/kg, and 400 mg/kg) were administered for seven days. The paw volume was measured using a digital plethysmometer before challenge and 24 hours after challenge. Blood was collected, and organs (spleen and liver) were isolated from each challenged mouse to determine blood cell count and organ index, respectively. RESULTS: No mortality and noticeable behavioral changes were observed among all mice receiving hydroethanolic root extract and solvent fractions at a dose of 2000 mg/kg. Hydroethanolic root extract and solvent fractions of Cyphostemma adenocaule showed enhancement of delayed-type hypersensitivity, organ index, and blood cell count. Hydroethanolic root extract at a dose of 400 mg/kg showed the highest and statistically significant stimulation of delayed-type hypersensitivity (0.123 ± 0.010) and blood cell count compared to the vehicle. CONCLUSION: Hydroethanolic root extract and solvent fractions of Cyphostemma adenocaule showed a stimulatory effect on cell-mediated immunity and hematopoiesis.
RESUMEN
BACKGROUND: Diabetes mellitus (DM) is a group of metabolic disorders that are characterized by hyperglycemia which results from defects in insulin release or its efficient use by the human body. Although significant progress has been made to manage DM and related complications, it remains a major global health problem. To this end, the search for new antidiabetic drugs from traditionally claimed medicinal plants is important. Aloe megalacantha Baker is an endemic plant used traditionally to treat diabetes in Ethiopia. This study aimed to investigate antidiabetic activity of isolates from the leaf of A. megalacantha Baker in streptozotocin-induced diabetic mice. METHODS: The exudate of A. megalacantha was collected by cutting the leaves and scraping the yellow sap and then dried at room temperature. The dried exudate was subjected to repeated thin layer chromatographic (TLC) separations using a mixture of solvent system to isolate the major compounds identified on the TLC plate. A single dose of streptozotocin (50 mg/kg) was injected intraperitoneally to overnight fasted mice to induce diabetes. Antidiabetic activity of TLC isolates was assessed by in vivo methods including oral glucose tolerance test, antihyperglycemic and hypoglycemic activity tests. RESULTS: Three major isolates were obtained from the TLC analysis of the exudate of A. megalacantha. Exudate and TLC isolates were found to be non-toxic up to a dose of 2000 mg/kg. The TLC isolates (Ia and Ib) significantly (p<0.05) reduced blood glucose levels and also increased body weight change of the diabetic mice compared with control groups. CONCLUSION: The present study demonstrated the ability of the exudate of A. megalacantha and its TLC isolates to significantly decrease blood glucose levels and increase body weights in mice, thus strengthening the claim of its traditional use in DM-related disorders.
RESUMEN
The genus Thymus is traditionally used for the treatment of hyperactive airways complaints. The purpose of the current study is to investigate the potential tracheal relaxant effect and possible mechanism(s) of the essential oil of Thymus serrulatus (TS Oil) in isolated guinea pig tracheal tissues. The essential oil was obtained from the fresh erial parts of Thymus serrulatus, and its phyto-components were identified by GC-MS analysis. Guinea pig tracheal preparations were used for testing the tracheal relaxant effect of TS Oil with the determination of the mechanism(s) involved in this relaxation. GC-MS findings reveal that terpenes, fragrance constituents, saponins, and higher fatty acids are present in TS Oil. In isolated guinea pig trachea, TS Oil inhibited carbachol (CCh, 1 µM) and K+ (80 mM)-induced contractions in a pattern similar to that of dicyclomine. TS Oil, at 0.3 mg/ml, shifted parallel CCh-curves towards the right, followed by a non-parallel shift at higher concentration (1 mg/ml), thus suppressing maximum response in the same manner as produced by dicyclomine. Pretreatment of tissues with TS Oil (1 and 3 mg/ml) also produced a rightward shift of Ca++ concentration-response curves (CRCs) in the same manner as caused by verapamil. Further, TS Oil at low concentrations (0.3 and 1 mg/ml) shifted isoprenaline-induced inhibitory CRCs towards the left and increased cAMP levels in isolated tracheal homogenates similar to papaverine, a phosphodiesterase (PDE) inhibitor. In the antimicrobial assay performed by the agar well diffusion method, TS Oil was found most active against Candida albicans and Staphylococcus aureus where the zone of inhibition measured was 28 mm. Additionally, there was little difference between standard strains of gram-positive and gram-negative bacteria. However, methicillin-resistant S. aureus (MRSA) showed a small zone of inhibition as compared to standard strains (22 mm). From these results, it can be concluded that the essential oil of T. serrulatus has the potential to produce antimicrobial effects while causing tracheal relaxation mediated possibly by anticholinergic effects, Ca++ channel blockade, and PDE inhibition whereas additional mechanism(s) cannot be ruled out.
RESUMEN
Ulcerative colitis (UC) is an inflammatory bowel disease (IBD) that causes irritation, inflammation, and ulceration in the linings of the colon and rectum. Otostegia fruticosa is traditionally used to treat various disorders in different parts of the Middle East and sub-Saharan Africa. In the present study, we evaluated the ameliorative effects of crude leaves extract of O. fruticosa (OF.Cr) on acetic acid (AA)-induced UC model in Wistar albino rats. Wistar rats were administered orally with either vehicle (10 mL/kg), OF.Cr (200 and 400 mg/kg), or prednisolone (2 mg/kg) once a day for 6 days. On day 6, UC was induced in rats by intrarectal administration of a single dose of 5% AA (1.0 mL). Disease activity index (DAI) was recorded after one day of colitis induction by assessing the symptoms of colitis and then the rats were euthanized by cervical dislocation, and colon tissues were isolated for the histopathological examination and biochemical analysis of oxidative stress parameters and cytokines (Interleukin-6 and Tumor Necrosis Factor-α). OF.Cr pretreatment exhibits significant prevention against UC, as confirmed by a significant decrease of DAI, colonic ulceration, and reduced inflammatory score as compared to the AA-induced colitis rats. Depletion of total glutathione (GSH) levels and catalase (CAT) activities in the colitis group was significantly restored in the OF.Cr treated groups, while increased lipid peroxidation in the colon tissues was significantly reduced. OF.Cr prevented the activation of the IL-6 and TNF-α pathways in the colonic tissues, which were clearly observed by the decreased levels of IL-6 and TNF-α in the OF.Cr treated animals. Hence, OF.Cr could be developed in the future for the treatment of UC.
RESUMEN
Thymus serrulatus, an endemic plant of Ethiopia, is traditionally used to cure various diseases and as a food ingredient. In the Ethiopian folk medicine, the decoction is orally taken as a remedy to treat diabetes and high blood pressure. The purpose of the present study was to evaluate the antioxidant and antihyperglycemic effects of the aqueous extract and of the essential oil of Thymus serrulatus. The chemical composition of the aqueous extract was determined by LC-MS and the essential oil was characterized by GC-MS analysis. Radical scavenging assays, namely scavenging of 2,2-diphenyl-1-picrylhydrazyl (DPPHâ¢), hydroxyl (â¢OH), and nitric oxide (â¢NO), were used as a first approach to screen the potential antioxidant abilities of the samples. Alpha-amylase and α-glucosidase inhibitory studies were also employed to evaluate the in vitro antihyperglycemic potential of the plant. The in vivo blood glucose lowering effect of the extracts was assessed using hypoglycemic activity and the oral glucose tolerance test in normal and in streptozotocin induced diabetic mice. When compared to the aqueous extract, the essential oil showed superior radical scavenging activity, particularly for â¢NO, as well as greater inhibitory potency against α-amylase and α-glucosidase (IC50 = 0.01 mg/ml and 0.11 mg/ml, respectively). Both tested samples showed a statistically significant antihyperglycemic effect. The aqueous extract at 600 mg/kg exerted maximum antihyperglycemic activity (44.14%), followed by the essential oil (30.82%). Body weight and glucose tolerance parameters were also improved by the samples both in normal and diabetic mice. The findings of this study support the hypothesis that aqueous extract and essential oil of T. serrulatus are promising therapeutic agents.
RESUMEN
Barlericin, the new neolignan diglycoside, has been isolated from the n-butanol soluble sub-fraction of Barleria acanthoides along with dehydrodiconiferyl alcohol 12-O-beta-D-glucopyranoside (2), reported for the first time from the genus Barleria. Their structures have been assigned on the basis of spectral studies.
Asunto(s)
Acanthaceae/química , Glicósidos/química , Glicósidos/aislamiento & purificación , Lignanos/aislamiento & purificación , Lignanos/química , Estructura Molecular , Resonancia Magnética Nuclear Biomolecular , Pakistán , EstereoisomerismoRESUMEN
BACKGROUND: Gastrointestinal disorders are often poorly managed, especially in developing countries, where there are limited resources and therapeutic options. Despite the rich diversity of medicinal plants that offer effective treatment options with fewer side effects, studies that provide scientific verification are lacking. Maerua subcordata (Gilg) DeWolf is among the plants claimed to have wide traditional medicine, use, including as a remedy against gastrointestinal problems. Therefore, this work aimed to evaluate the gut-modulatory effects of a crude leaf extract of M. subcordata (MSL.Cr), as well as its possible mechanism of action. METHODS: A castor oil (10 mL/kg)-induced diarrheal mouse model was used to evaluate the antidiarrheal effect of MSL.Cr, and the spasmodic/antispasmodic effect of the extract was assessed using isolated rabbit jejunum with and without addition of standard cholinergic agonists/antagonists to predict the possible mechanism of action. RESULTS: MSL.Cr exhibited 40% and 80% protection against castor oil-induced diarrhea in mice at doses of 500 and 1,000 mg/kg, respectively. In isolated rabbit jejunum, the extract increased spontaneous contractions at low doses (0.01-0.1 mg/mL), and was sensitive to atropine, whereas it showed complete inhibition at higher doses (0.3-1 mg/mL). It was shown that the relaxant effect was possibly mediated by the involvement of phosphodiesterase-enzyme inhibition and K+-channel activation. The extract potentiated the control concentration-response curve of carbachol, shifting it to the left, similarly to the control drug papaverine. The potassium-channel opening-like activity of MSL.Cr was possibly mediated by the involvement of aspecific K+-channels inhibition, since tetraethylammonium, anunselective antagonist of K+ channels, significantly reversed its inhibitory effect. CONCLUSION: This study showed that the M. subcordata leaf extract demonstrated gut-modulatory effects, possibly mediated by a combination of muscarinic-receptor stimulation, phosphodiesterase inhibition, and aspecific K+-channel activation.
RESUMEN
Otostegia fruticosa is traditionally used to treat tonsillitis, stomach ache, asthma, arthritis, and febrile illness in different parts of Ethiopia and other countries. In this experiment 70% ethanolic crude extract and fractions of the leaf of Otostegia fruticosa (Forssk.) Schweinf. ex Penzig were evaluated for their in-vivo anti-inflammatory and analgesic activities and in-vitro hyaluronidase inhibition properties at different concentrations. Tail immersion, acetic acid induced writhing and carrageenan-induced paw edema model were used to assess the in-vivo analgesic and anti-inflammatory activities, respectively. Swiss albino mice of either sex were randomly divided into five groups of six mice per group and for evaluation of the fractions randomly divided into six groups of six mice per group. The test groups were treated with hydroalcoholic extract of Otostegia fruticosa (O. fruticosa) at doses of 100, 200, and 400 mg/kg. The positive control groups received either pethidine 5 mg/kg or aspirin at 100 mg/kg or 150 mg/kg. The negative control groups were orally given sunflower oil. All the fractions were administered at the dose of 400 mg/kg. In all models, the higher dose (400 mg/kg) of the crude extract and chloroform fraction showed a significant central and peripheral analgesic and anti-inflammatory activities with comparable effects to standards used. The hyaluronidase inhibition assay result showed that the test samples displayed concentration-dependent inhibitory activities. These findings indicate that 70% ethanol extract and organic solvent fractions of O. fruticosa leaves have potential analgesic, anti-inflammatory, and enzyme inhibitory activities.
RESUMEN
OBJECTIVE: To evaluate the antimalarial effect of aqueous methanolic extract and solvent fractions of Meriandra dianthera leaves against Plasmodium berghei in mice model. METHOD: M. dianthera leaves were extracted with 80% methanol and dried. The dried crude extract was then defatted and further fractionated with chloroform, ethyl acetate, and butanol. Acute oral toxicity test was performed as per the Organization for Economic Cooperation and Development guideline 425. Peter's 4-day suppressive test was used to determine the in vivo antimalarial activity of the extract and fractions. RESULT: The crude leaf extract of Meriandra dianthera leaves against P < 0.001) chemosuppression compared to the negative control. Both the extract and fractions were able to prevent P. berghei induced body weight loss and body temperature reduction and also increased the survival time of the mice as compared to the negative control. The aqueous methanolic leaf extract of M. dianthera leaves were extracted with 80% methanol and dried. The dried crude extract was then defatted and further fractionated with chloroform, ethyl acetate, and butanol. Acute oral toxicity test was performed as per the Organization for Economic Cooperation and Development guideline 425. Peter's 4-day suppressive test was used to determine the. CONCLUSION: The extracts of M. dianthera leaves showed promising antimalarial activity, with no sign of toxicity and therefore may support its traditional use for the treatment of malaria.M. dianthera leaves were extracted with 80% methanol and dried. The dried crude extract was then defatted and further fractionated with chloroform, ethyl acetate, and butanol. Acute oral toxicity test was performed as per the Organization for Economic Cooperation and Development guideline 425. Peter's 4-day suppressive test was used to determine the.
RESUMEN
Barlerisides A (1) and B (2), new phenolic glycosides, have been isolated from the n-butanol soluble sub-fraction of Barleria acanthoides along with two known compounds acteoside (3) and p-hydroxycinnamic acid (4). Their structures have been assigned on the basis of spectral studies. Both 1 and 2 showed significant activity in the superoxide scavenging assay while weak inhibitory activity was observed against the enzyme xanthine oxidase.
Asunto(s)
Acanthaceae/química , Flavonas/aislamiento & purificación , Depuradores de Radicales Libres/aislamiento & purificación , Glucósidos/aislamiento & purificación , Glicósidos/aislamiento & purificación , Fenoles/química , Superóxidos/metabolismo , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Antiinflamatorios/farmacología , Flavonas/química , Flavonas/farmacología , Depuradores de Radicales Libres/química , Depuradores de Radicales Libres/farmacología , Glucósidos/química , Glucósidos/farmacología , Glicósidos/química , Glicósidos/farmacología , Fenoles/aislamiento & purificación , Fenoles/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Solventes/química , Xantina Oxidasa/antagonistas & inhibidores , Xantina Oxidasa/metabolismoRESUMEN
Malaria is a devastating parasitic disease which caused around 216 million cases and 445,000 deaths worldwide in 2016. This might be attributed to a wide spread of drug resistant parasites. The plant Aloe megalacantha is indigenous to Ethiopia where the sap of the leaves is traditionally used for the treatment of malaria. This study was aimed at evaluating the antimalarial effect of leaf latex and isolates obtained from Aloe megalacantha against chloroquine sensitive Plasmodium berghei ANKA strain in Swiss albino mice. Peters' 4-day suppressive test method was used to test the antimalarial activity of both leaves latex and isolates. Three isolates were obtained using thin layer chromatography and were coded as AM1, AM2, and AM3 in ascending order of their retention factor. After treatment of Plasmodium berghei infected mice with leaf latex of Aloe megalacantha for four days at 100, 200, and 400 mg/kg, it shows 30.3%, 43.4%, and 56.4% suppression of the parasite growth, respectively. 32.3%, 51.3%, and 67.4% chemosuppression after treatment with AM1, 39.8%, 50.6%, and 64.2% chemosuppression after treatment with AM2, and 52.6%, 69.4%, and 79.6% chemosuppression after treatment with AM3 were observed at doses of 100, 200, and 400 mg/kg/day, respectively. The observed parasite suppression of leaves latex and isolates was statistically significant (P<0.05) as compared to negative control. Moreover, both the leaves latex and isolates were also observed to prevent Plasmodium berghei induced body weight loss and hypothermia and increased the survival time of Plasmodium berghei infected mice as compared to the negative control. Hence, the present study supports the traditional claim of the plant for the treatment of malaria.
RESUMEN
The seed of Nigella sativa (N. sativa) has been used in different civilization around the world for centuries to treat various animal and human ailments. So far, numerous studies demonstrated the seed of Nigella sativa and its main active constituent, thymoquinone, to be medicinally very effective against various illnesses including different chronic illness: neurological and mental illness, cardiovascular disorders, cancer, diabetes, inflammatory conditions, and infertility as well as various infectious diseases due to bacterial, fungal, parasitic, and viral infections. In spite of limited studies conducted so far, the promising efficacy of N. sativa against HIV/AIDS can be explored as an alternative option for the treatment of this pandemic disease after substantiating its full therapeutic efficacy. Moreover, the strong antioxidant property of this valued seed has recently gained increasing attention with regard to its potential role as dietary supplement with minimal side effects. Besides, when combined with different conventional chemotherapeutic agents, it synergizes their effects resulting in reducing the dosage of concomitantly used drugs with optimized efficacy and least and/or no toxicity. A number of pharmaceutical and biological properties have been ascribed to seeds of N. sativa. The present review focuses on the profile of high-value components along with traditional medicinal and biological principles of N. sativa seed and its oil so as to explore functional food and nutraceutical potential of this valued herb.
RESUMEN
A new pregnane derivative, 2,6beta,7beta-trihydroxy-4-methyl-19-norpregna-1,3,5(10)-trien-17-one, has been isolated from the ethyl acetate soluble fraction of Potentilla evestita along with a pregnane derivative, 11alpha,17alpha,21-trihydroxypregna-4,16(22)-diene-3,20-dione, that is reported for the first time as a natural product. Their structures were elucidated with the aid of 1H and 13C NMR spectra and by COSY, HMQC, HMBC and NOESY experiments.