Effectiveness of an encecalin standardized extract of Ageratina pichinchensis on the treatment of onychomycosis in patients with diabetes mellitus.

Ageratina pichinchensis is utilized in traditional medicine for the treatment of dermatomycosis and inflammation. The aim of this study was to evaluate the clinical and mycological effectiveness of the topical administration of an enecalin standardized extract of A. pichinchensis for treating onychomycosis in patients with type 2 diabetes mellitus (DM2). A double blind, randomized, and controlled clinical trial was carried out that included patients with DM2 and who had mild or moderate onychomycosis. Participants were administered topically, for 6 months, a lacquer containing the encecalin standardized extract of A. pichinchensis (experimental group) or 8% ciclopirox (control group). In a large percentage of both, the control group (77.2%) and the experimental group (78.5%), clinical efficacy was detected as a decrease in the number of affected nails and a reduction in the severity of nail involvement. Without exhibiting statistically significant differences between groups, the encecalin standardized extract of A. pichinchensis was clinically and mycologically effective in the treatment of mild and moderate onychomycosis in patients with DM2. The treatment of onychomycosis in patients with DM2 implies a greater challenge, while control of blood glucose levels in these patients, played a very important role in the response of patients to treatment.

Aislamiento e identificación de compuestos con actividad antiobesidad y antiadipogénica de Thevetia peruviana / Isolation and identification of anti-obesity and anti-adipogenic compounds from Thevetia peruviana

Thevetia peruviana ha sido utilizada en la medicina tradicional mexicana por sus efectos adelgazantes. Para la identificación de las fracciones y los compuestos activos de T. peruviana se utilizó cromatografía en columna abierta y las fracciones obtenidas se evaluaron en ratones con obesidad inducida con glutamato monosódico. Como control positivo se utilizó Orlistat y los tratamientos se administraron oralmente una vez al día durante 8 semanas. La fracción con mayor actividad fue sub-fraccionada y, con la intención de evitar el uso de más ratones, los productos fueron seleccionados por su capacidad para inhibir la adipogénesis en la línea celular 3T3-L1. Los animales tratados con la fracción F-B mostraron un aumento de peso significativamente menor y mantuvieron la sensibilidad a la insulina, así como, niveles significativamente más bajos de colesterol y triglicéridos. El análisis de GC-MS indicó que esta fracción activa está compuesta principalmente por los ácidos palmítico (1), oleico (2) y octadacanoico (3), 2-palmitoil glicerol (4), 2-oleoil glicerol (5) así como la estigmastenona (6).

Thevetia peruviana has been used in Mexican traditional medicine for its slimming effects. Active fractions and compounds from T. peruviana were isolated and identified by means of gravitational open-column chromatography, and the fractions were evaluated on mice with MonoSodium Glutamate-induced obesity. Orlistat was used as positive control, and treatments were administered, orally, once a day for 8 weeks. The fraction with higher activity was sub-fractioned and, with the intention of avoiding using more mice, the fractions were analyzed by evaluating their capability to inhibit adipogenesis in the 3T3-L1 cell line. Animals treated with the F-B fraction revealed a significantly smaller weight increase and maintained adequate insulin sensitivity, and significantly lower blood levels of cholesterol and triglycerides. The active compounds that demonstrated greatest adipogenesis inhibition were palmitic acid (1), oleic acid (2), octadecanoic acid (3), 2-palmitoyl glycerol (4), 2-oleoyl glycerol (5) and stigmastenone (6).

A Malva parviflora´s fraction prevents the deleterious effects resulting from neuroinflammation.

Neuroinflammation, a centralized immune response, is a physiological process by which the organism attempts to remove an injurious stimulus in the central nervous system. Nonetheless, it is known that chronic inflammatory processes play an important role in the onset and progression of neurodegenerative disorders, such as Alzheimer´s disease (AD). Based on this, new strategies to treat AD have been proposed. Among them, the use of non-steroidal anti-inflammatory drugs (NSAIDs) decreases the incidence of this disease. Unfortunately, the prolonged use of NSAIDs results in adverse secondary effects. In this context, plants secondary metabolites have become of great interest. Particularly, our group has demonstrated that the hydroalcoholic extract of Malva parviflora (MpHA) has anti-inflammatory effect and is capable of improving the cognitive deficit present in an AD model. To further characterize the Malva parviflora compounds with anti-inflammatory properties, here we generated a fraction from a dichloromethane extract, which constitutes a less complex mix of compounds than the MpHA. This approach allowed us to isolate a fraction (MpF10) with anti-inflammatory activity, able to ameliorate the spatial learning and memory impairment, and to reduce both astrogliosis as well as IL-1ß and TNF production in a murine model of LPS-mediated neuroinflammation. Among the identified compounds in the MpF10, we found daucosterol (MpDau), which prevented LPS-induced neuroinflammation. Interestingly, MpF10 and MpDau inhibit NFκB activity in macrophages exposed to LPS. Therefore, we propose that the compounds present in the MpF10 represent an alternative to treat neuroinflammation, an important process developed during neurodegenerative diseases such as AD.

Acute and Chronic Antihypertensive Effect of Fractions, Tiliroside and Scopoletin from Malva parviflora.

Hypertension is a disease of high prevalence and morbidity where vascular inflammation and associated oxidative stress (endothelial dysfunction) is the underlying cause of this pathology. We are reporting the antihypertensive activity of extracts and fractions of Malva parviflora in mice with chronic and acute hypertension. Also, the treatments of this plant were able to counteract the kidney inflammation and associated oxidative stress. The chronic hypertension model consisted of administration of angiotensin II (AGII) during 12 weeks, causing a sustained increase in systolic (SBP) or diastolic (DBP) pressure, with values of pharmacological constants of: ED50 = 0.038 mg/kg y Emax = 135 mmHg for SBP and ED50 = 0.046 mg/kg y Emax = 98 mmHg for DBP. The chronic hypertension caused the inflammation and lipid peroxidation in kidneys, measured by of tissue level of cytokines such as interleukin-1ß (IL-1ß), IL-6, Tumor Necrosis Factor-α (TNF-α), IL-10 and malondialdehyde, and treatments for M. parviflora were able to modulate these parameters. The chemical fractionation allowed to identify three compounds: oleanolic acid, tiliroside and scopoletin, which were tested in a model of acute hypertension. The pharmacodynamic parameters for SBP were ED50 = 0.01 and 0.12 mg/kg while Emax = 33.22 and 37.74 mmHg for scopoletin and tiliroside, respectively; whereas that for DBP data were ED50 = 0.01 and 0.02 mg/kg; with an Emax = 7.00 and 6.24 mmHg, in the same order. M. parviflora, is able to counteract the effect of chronic and acute administration of AGII, on hypertension, but also the inflammatory and oxidative damage in the kidney. The oleanolic acid, scopoletin and tiliroside are the compounds responsible for such activities.

Anti-Inflammatory Activity of a Polymeric Proanthocyanidin from Serjania schiedeana.

The ethyl acetate extract (SsAcOEt) from Serjania schiedeana, select fractions (F-6, F-12, F-13, F-14), and one isolated compound, were evaluated in 12-O-tetradecanoylphorbol 13-acetate (TPA) ear edema and kaolin/carrageenan (KC)-induced monoarthritis assays. SsEtOAc induced edema inhibition of 90% (2.0 mg/ear), fractions showed activity within a range of 67-89%. Due to the fact F-14 showed the highest effect, it was separated, yielding a proanthocyanidin-type called epicatechin-(4ß â†’ 8)-epicatechin-(4ß â†’ 8, 2ß â†’ O → 7) epicatechin (ETP). This compound (2.0 mg/ear) provoked 72% of edema inhibition (ED50 = 0.25 mg/ear, Emax = 52.9%). After 9 days of treatment, joint inflammation was decreasing, and on the last day, SsEtOAc (400 mg/kg), F-14 and ETP (10 mg/kg), SsEtOAc (200 mg/kg), methotrexate (MTX) 1.0 mg/kg and meloxicam (MEL) 1.5 mg/kg, produced an inhibition articulate edema of 94, 62, 36, 21, 80, and 54%, respectively. In the joint, pro-inflammatory molecules were elevated in animals without treatment (vehicle group, VEH). Treatments from S. schiedeana induced a decrease in the concentration of interleukin (IL)-1ß, IL-17, and IL-6, and SsEtOAc at a higher dose diminished tumor necrosis factor (TNF-α). IL-10 and IL-4 were fewer in the VEH group in comparison with healthy mice; the animals with treatments from S. schiedeana induced an increment in the levels of these cytokines in joint and spleen.

Effectiveness of Ageratina pichinchensis Extract in Patients with Vulvovaginal Candidiasis. A Randomized, Double-Blind, and Controlled Pilot Study.

Previous clinical studies have demonstrated the antifungal effectiveness of Ageratina pichinchensis extracts when topically administered to patients with dermatomycosis. The objective of this study was to evaluate the effectiveness and tolerability of a 7% standardized extract of A. pichinchensis (intravaginal) in patients with vulvovaginal candidiasis. The extract was standardized in terms of its encecalin content and administered during 6 days to patients with Candida albicans-associated vulvovaginitis. The positive control group was treated with Clotrimazole (100 mg). On day 7 of the study, a partial evaluation was carried out; it demonstrated that 94.1% of patients treated with Clotrimazole and 100% of those treated with the A. pichinchensis extract referred a decrease or absence of signs and symptoms consistent with vulvovaginal candidiasis. In the final evaluation, 2 weeks after concluding administration, 86.6% of patients in the control group and 81.2% (p = 0.65) of those treated with the A. pichinchensis extract demonstrated therapeutic success. Statistical analysis evidenced no significant differences between the two treatment groups. With the results obtained, it is possible to conclude that the standardized extract from A. pichinchensis, intravaginally administered, showed therapeutic and mycological effectiveness, as well as tolerability, in patients with vulvovaginal candidiasis, without noting statistical differences in patients treated with Clotrimazole. Copyright © 2017 John Wiley & Sons, Ltd.

Chrysoeriol and other polyphenols from Tecoma stans with lipase inhibitory activity.

ETHNOPHARMACOLOGICAL RELEVANCE: Tecoma stans is traditionally used by several ethnical groups in Mexico and Central America to treat diabetes. This species is mentioned in the majority of the ethnopharmacological studies compiled in Mexico focused in medicinal plants used as anti-diabetic treatment. AIM OF THE STUDY: Recently, this plant was found to display a high level of pancreatic lipase inhibitory activity, in addition to the several action mechanisms already described. Here we show the phytochemical and in vitro pharmacological characterization of some of the compounds responsible for the antilipase activity. MATERIALS AND METHODS: Starting with a hydroalcoholic extract, fractions were obtained by liquid-liquid separation and successive processes of column chromatography purifications. Lipase inhibitory activity was measured employing a spectrophotometric analysis. For structural elucidation (1)H and (13)C NMR experiments were used. HPLC was used to quantify and confirm the identity of the bioactive compounds. RESULTS: Bio-guided chemical purification of the hydroalcoholic extract produced an organic fraction (ethyl acetate, TsEA), flavone fractions (TsC1F13), (TsC1F15), (TsC1F16) and isolated compounds (chrysoeriol, apigenin, luteolin, and verbascoside) with the capability to inhibit the activity of pancreatic lipase. The most active fraction (TsC2F6B) was constituted by a mixture of Chrysoeriol (5,7-dihydroxy-2-[4-hydroxy-3-methoxyphenyl]chromen-4-one, 96% ) and Apigenin (4%). This flavone mixture displayed a percentage of inhibition of 85% when it was eavaluated at 0.25mg/mL. Luteolin and chrysoeriol produced a noncompetitive and mixed inhibition with values of IC50=63 and 158µM respectively. The content of chrysoeriol was also quantified in the hydroalcoholic extract (TsHAE) and organic fraction (TsEA) as 1% and 7% respectively. All of this confirms that high proportion of both flavones produce an increase of the biological activity due to they show the highest inhibition of lipase enzyme in a concentration dependant way. CONCLUSIONS: These results evidence that the medicinal use of T. stans could be in part because of its lipase inhibitory activity allowing to adapt the administration of this plant before meals. Also this data could help to develop a novel phytopharmaceutical drug (standardized in luteolin, chrysoeriol, and apigenin) auxiliary for the Type 2 Diabetes mellitus.

Effect of Hautriwaic Acid Isolated from Dodonaea viscosa in a Model of Kaolin/Carrageenan-Induced Monoarthritis.

In the present work, the antiarthritic activity of hautriwaic acid is reported. This ent-clerodane diterpene isolated from Dodonaea viscosa was evaluated in mice using a kaolin/carrageenan-induced monoarthritis model. The inflammation observed in the joint (knee) on days 1-8 ranged from 50-70 %. After 10 days of treatment with different doses of hautriwaic acid (5, 10, 20 mg/kg), a decrease in knee inflammation was detected. This recovery was observed with both reference drugs, methotrexate (1 mg/kg) and diclofenac (0.75 mg/kg). In these groups of mice, the concentration of proinflammatory cytokines interleukin-1 beta, interleukin-6, and tumor necrosis factor alpha in the joint was significantly lower than that of the negative control group (animals with damage without any treatment). The negative control group presented a decrease in the concentration of interleukin-10, while the groups that received hautriwaic acid at different dose exhibited an increase in this interleukin. This anti-inflammatory cytokine was not modified in the joint of mice with diclofenac, but in mice that received methotrexate, a significant decrease was observed. Hautriwaic acid isolated from D. viscosa diminished the joint edema induced by this mixture of polysaccharides (carrageenan), possibly by acting as immunomodulator of the inflammatory response.

Pilot study that evaluated the clinical effectiveness and safety of a phytopharmaceutical elaborated with an extract of Ageratina pichinchensis in patients with minor recurrent aphthous stomatitis.

ETHNOPHARMACOLOGICAL RELEVANCE: The plant species Ageratina pichinchensis (Schauer) R.M.King & H.Rob. (Asteraceae) in a wild plant native to Mexico that is utilized in traditional medicine for the treatment of skin problems and for mouth ulcers. AIM OF THE STUDY: The objective of the present study was to evaluate the clinical effectiveness and therapeutic safety of a phytopharmaceutical elaborated with a unpigmented hexane-ethyl acetate extract of A. pichinchensis at a concentration of 5% in patients with a clinical condition of Minor Recurrent aphthous stomatitis (MiRAS). MATERIALS AND METHODS: We conducted a double-blind, randomized, and controlled pilot study in which the experimental treatment was a phytopharmaceutical elaborated with a unpigmented hexane-ethyl acetate extract of A. pichinchensis at a 5% concentration and, as control treatment, we utilized Triamcinolone at 0.1%. Study participants were patients with a diagnosis of MiRAS, elderly males and females, with a disease evolution of no. >3 days. Lesion size was measured by means of a tracing sheet and pain, by the Visual analog scale (VAS). Output variables comprised clinical effectiveness, treatment adherence, therapeutic failure, and therapeutic success. RESULTS AND DISCUSSION: Fifty six patients participated in the study and we distributed these into two study groups (28 in each group). The results obtained did not show statistically significant differences between the experimental and the control treatments. Among patients treated with the A. pichinchensis extract, the time required for achieving the absence of pain was 4.0 days, while that of the control treatment was 4.1 days. In patients treated with A. pichinchensis, the time necessary for healing was 4.5 days and for the Triamcinolone 0.1%-treated group, this was 4.7 days. Greater clinical effectiveness was evidenced on days 2, 3, and 4 of treatment. During the first 7 follow-up days, there was clinical effectiveness in 92.8% of experimental-group and in 89.2% of control-group patients. At the end of the study, 100% therapeutic effectiveness was able to be scored.

Effectiveness and tolerability of a standardized extract from Ageratina pichinchensis in patients with diabetic foot ulcer: a randomized, controlled pilot study.

Previous works have shown that extracts obtained from Ageratina pichinchensis are capable of reducing the time needed for wounds to heal. By means of a randomized, double-blind pilot study, the objective of this work was to evaluate the effectiveness and tolerability of a phytopharmaceutical developed with a standardized extract (5 %, cream formulation) of A. pichinchensis, topically administered in patients with diabetic foot ulcer. Micronized silver sulfadiazine (1 %) was employed as a control treatment. Treatments were randomly assigned to each patient, and clinical evolution was evaluated weekly until complete healing of the wound. All patients who concluded the study achieved complete healing of their ulcers. After six weeks of treatment, patients in the experimental group exhibited a wound-healing process of 77.5 %, while that of patients in the control group was 69.8 %. A statistically significant difference was not found between groups. The average time needed for complete wound healing was 65.47 ± 47.08 days for patients treated with the A. pichinchensis extract and 77.46 ± 50.8 days for patients in the control group (p = 0.509). There was no case in either of the groups in which adverse side effects were identified. Thus, it was concluded that the A. pichinchensis extract showed the ability to improve the healing process in patients with diabetic foot ulcer; however, no statistically significant differences were observed when compared with results obtained in patients administered the control treatment (micronized silver sulfadiazine). Some limitations of this study must be addressed, such as small sample size. This work comprises a pilot study that could be useful in a future clinical trial with a greater number of patients.

Pharmacological effect of Ageratina pichinchensis on wound healing in diabetic rats and genotoxicity evaluation.

ETHNOPHARMACOLOGICAL RELEVANCE: Among the main causes affecting the wound healing process, we find diabetes mellitus, which is due to the occurrence of a prolonged inflammation phase, defects in angiogenesis, and a diminution in fibroblast proliferation. The species Ageratina pichinchensis has been utilized in Mexican traditional medicine for the treatment of skin wounds. Pharmacological models have demonstrated that an extract obtained from this species improves wound healing and, through a clinical study, it was evidenced that the extract (in a pharmaceutical form) is effective in the treatment of patients with chronic venous ulcers. The 7-O-(ß-D-glucopyranosyl)-galactin compound was recently identified as responsible for the pharmacological activity. The objective of the present study was to evaluate the wound healing activity of an aqueous extract and another hexane-ethyl acetate extract from Ageratina pichinchensis (both standardized in the active compound) in a diabetic foot ulcer rat model, as well as evaluating the possible genotoxic effects produced by the same species. MATERIALS AND METHODS: Rats with streptozotocin-induced diabetes were submitted (under anesthesia with pentobarbital) to a circular lesion on the skin (excisional) on the rear of the paw. All animals were topically treated daily until healing. 5-methyl-1 phenyl-2-(1H) Pyridone was used as a positive control treatment. Once the wound was healed, a skin sample was obtained and utilized for histopathological analysis. The possible genotoxic effects produced by the extract, in a model of spermatozoid viability and morphology, were evaluated. RESULTS: The results showed that 100% of animals treated with Ageratina pichinchensis extracts presented wound healing between days 4 and 11 of treatment, while in the positive control group (treated with 5-methyl-1 phenyl-2-(1H) pyridone) and in the negative control group (vehicle), only 70% and 40%, respectively, exhibited wound healing at day 11. Histological analysis demonstrated evidences of an active regenerative process in animals that received the extracts, in addition to that in the study, the effects of the plant extracts that could be compatible with genotoxicity were not observed. CONCLUSIONS: Aqueous and hexane-ethyl acetate extracts of the aerial parts of Ageratina pichinchensis (standardized in its content of 7-O-(ß-D-glucopyranosyl)-galactin), consistently improve wound healing induced on the skin of rats with streptozotocin-induced diabetes. The capacity was evidenced of the extracts to promote histological tissue regeneration, without exhibiting genotoxicity.

Toxicology, genotoxicity, and cytotoxicity of three extracts of Solanum chrysotrichum.

ETHNOPHARMACOLOGICAL RELEVANCE: Infusions of Solanum chrysotrichum (Schldl.) or "sosa" are employed in Traditional Mexican Medicine for the local and systemic treatment of skin and mucosal infections. Different studies have verified its antifungal effectiveness and therapeutic safety in superficial mycosis caused by dermatophytes or yeasts, and have identified a group of spirostanic saponins, denominated SC-2-SC-6, as responsible for the antifungal activity. Of these, SC-2 is the most active molecule. Electron microscopy studies showed that SC-2 disintegrates cell wall and internal membranes of the fungi studied. In order to continue the systematic study of Solanum chrysotrichum, the goal of the present study was to evaluate the toxicity, genotoxicity, and cytotoxicity of the three different extracts of Solanum chrysotrichum. MATERIALS AND METHODS: From the dried leaves of Solanum chrysotrichum, we obtained the aqueous, hydroalcoholic, and ethanolic extracts. Saponins (SC-2-SC-6) were quantified by High-performance liquid chromatography (HPLC). For the toxicology study, we formed four groups: three experimental groups, treated with each of the extracts at 1-g/kg doses per os (po) during 4 weeks, and a negative control group treated with the vehicle. For the genotoxicity study, we added another group, which was treated with cyclophosphamide for 1 week. The cytotoxicity study was carried out with international methods and employing the nasopharyngeal cancer (KB) and breast cancer (MDA) cell lines. RESULTS: The three evaluated extracts did not modify either of the behavioral parameters, and on the hepatic-function biochemical tests (alanine aminotransferase [ALT] and aspartate aminotransferase [AST]), did not showed significant increase on comparing to placebo. The genotoxicity parameters did not exhibit differences between the experimental groups and the placebo (control) group. Histologic analysis showed that the three extracts caused amyloidosis and moderate necrosis in liver, and focal tumefaction in kidney, as well as significant, but clinically irrelevant, elevations of creatinine with the aqueous and hydroalcoholic, but not with the ethanolic, extracts. In addition, the aqueous and ethanolic extracts exhibited interesting cytotoxic activity against the KB cell line. CONCLUSIONS: At the doses administered, the ethanolic extract of Solanum chrysotrichum showed a slightly toxic effect on liver and kidney, without biochemical or genotoxic repercussions and with cytotoxic activity against the KB cell line.

Pharmacological and chemical study to identify wound-healing active compounds in Ageratina pichinchensis.

The aerial parts of Ageratina pichinchensis are used in Mexican traditional medicine for the treatment of skin wounds. Recently, it was demonstrated that the aqueous extract of this plant reduced the time required to cicatrize a wound induced in the rat. The same extract showed a capability to induce overgrowth in normal fetal lung cells (MRC-5). The objective of the present study was isolating and identifying the active compounds in A. pichinchensis that are capable of inducing cellular overgrowth, as well as performing a preliminary evaluation of their anti-inflammatory and toxic effects. By means of bioguided chemical separation of an aqueous extract of A. pichinchensis, the most active compound capable of inducing cellular overgrowth was identified as 7-O-(ß-D-glucopyranosyl)-galactin. In vivo inflammation induced with carrageenan in mice was significantly reduced by the aqueous extract of A. pichinchensis, reaching a decrease of up to 60.6 %. Acute (2 g/kg) and subchronic (1 g/kg for 28 days) oral administration of the aqueous extract of this plant did not affect hepatic function (through alanine aminotransferase and aspartate aminotransferase activity evaluation), while no alterations of the histologic samples of liver and kidney were evidenced.

Influence of two hypoglycemic Cucurbitaceae (Cucurbita ficifolia Bouché and Ibervillea sonorae Greene) on ATP-sensitive potassium channels in rat aortic rings / Influencia de dos Cucurbitaceae (Cucurbita ficifolia Bouché e Ibervillea sonorae Greene) sobre los canales de potasio sensibles a ATP en anillos aórticos de rata

Cucurbita ficifolia Bouché fruit containing D-chiro-inositol and Ibervillea sonorae Greene root containing cucurbitane-type glycosides are used to control diabetes in Mexico. Although the hypoglycemic effect of both plants has been demonstrated and some active compounds proposed, their mechanisms are still unknown. The aim of this study was to determine if the incubation with both aqueous extracts avoids the inhibition of contraction induced by phenylephrine similarly to glibenclamide in rat aortic rings. The hypoglycemic aqueous extracts of C. ficifolia and I. sonorae were characterized for their content of either D-chiro inositol or cucurbitanes respectively, and then we assayed the characterized extracts in vitro on the diazoxide-induced relaxation of rat aortic rings precontracted with phenylephrine, using as positive control glibenclamide. I. sonorae extract blocked the KATP channels in a concentration-dependent manner (p < 0.05), whereas C. ficifolia extract had no effect on these channels. I. sonorae extract produces a hypoglycemic effect through a similar mechanism to sulphonylureas in this experimental model; however, hypoglycemic action of C. ficifolia extract should be explained by an independent KATP channels mechanism.

Los frutos de Cucurbita ficifolia conteniendo D-quiro-inositol y las raíces de Ibervillea sonorae conteniendo glucósidos tipo cucurbitano son empleados en el control de la diabetes en México. Aunque el efecto hipoglucémico de ambas plantas ha sido demostrado y se han propuesto algunos de sus compuestos activos, aún se desconoce su mecanismo de acción. El objetivo de este estudio fue determinar si la incubación con ambos extractos acuosos evita la inhibición de la contracción inducida por fenilefrina de manera similar a la glibenclamida en anillos aórticos de rata. Los extractos acuosos hipoglucémicos de C. ficifolia e I. sonorae fueron caracterizados en su contenido de D-quiro inositol o cucurbitanos, respectivamente y entonces fueron estudiados en un modelo in vitro en la relajación inducida por diazóxido en anillos aórticos previamente contraídos con fenilefrina, usando como control positivo glibenclamida. El extracto de Ibervillea sonorae bloqueó los canales KATP de manera dosis-dependiente (p < 0.05), mientras que Cucurbita ficifolia no tuvo efecto en esos canales. El extracto de I. sonorae produce efecto hipoglucémico a través de un mecanismo similar al de las sulfonilureas en este modelo experimental; por su parte, la acción hipoglucemiante del extracto de C. ficifolia debe ser explicado mediante un mecanismo independiente de los canales KATP.

Inhibition of acetylcholinesterase activity by hidroalcoholic extractand their fractions of Bouvardia ternifolia (Cav. ) Shcltdl (Rubiaceae) / Inhibición de la actividad de acetilcolinesterasa por el extracto hidroalcohólico y sus fracciones de Bouvardia ternifolia (Cav. ) Shcltdl (Rubiaceae)

The hydroalcoholic extract (BtHA) and its fractions of Bouvardia ternifolia were evaluated as inhibitors of the activity of the acetylcholinesterase enzyme utilizing the in vitro method (Ellman). BtHA inhibited the acetylcholinesterase enzyme competitively (IC50 = 0.6 ug/ml); the ethyl acetate fraction (BtF-AcOEt) caused mixed-type inhibition (IC50 = 0.96 ug/ml). A fraction insoluble on methanol (Bt-Faq-1) showed a mixed-type inhibition (CI50 = 0.96 ug/ml). Finally, the methanol-soluble fraction (Bt-Faq-2), presented complex, mixed-type inhibition that corresponds to the C5 system ( alpha= 0.740 and beta = 0.842). Rutin, quercetin, kaempferol and ursolic acid were detected by HPLC and the concentration of these compounds was different in each fraction.

El extracto hidroalcohólico (BtHA) y fracciones provenientes de Bouvardia ternifolia fueron evaluadas como inhibidores de la enzima acetilcolinesterasa utilizando el método enzimático propuesto por Ellman. BtHA inhibe a la enzima de manera competitiva (IC50 = 0.6 ug/ml); la fracción de acetato de etilo (BtF-AcOEt) provoca una inhibición mixta (IC50 = 0.96 ug/ml). La fracción insoluble en metanol (Bt-Faq-1) mostró una inhibición tipo mixta (CI50 = 0.96 ug/ml). Finalmente la fracción soluble en metanol, Bt-Faq-2, inhibe a la enzima presentando una inhibición mixta que corresponde a un sistema C5 ( alfa= 0.740 and beta= 0.842). Mediante HPLC se detectó rutina, quercetina, canferol y ácido ursólico la concentración de estos compuestos fue diferente en cada fracción.

Therapeutic effectiveness of Ageratina pichinchensis on the treatment of chronic interdigital tinea pedis: a randomized, double-blind clinical trial.

OBJECTIVES: Interdigital tinea pedis is the most frequent presentation, as well as the most severe clinical form of tinea pedis, constituting a therapeutic challenge. The aim of the study was to evaluate the effectiveness and tolerability of two concentrations of Ageratina pichinchensis extract (encecalin content, 0.76 and 1.52%, respectively) on patients with clinical and mycological diagnosis of chronic interdigital tinea pedis. DESIGN: By means of a randomized, double-blind clinical trial, three groups of patients were treated topically for 4 weeks with a cream containing the following: Group I-the lower concentration of A. pichinchensis extract, group II-the higher concentration, group III-2% ketoconazole. SUBJECTS: One hundred and sixty (160) ambulatory patients of either sex between the ages of 18 and 65 years were enrolled. OUTCOME MEASURES: The primary outcome variables were: clinical effectiveness, mycological effectiveness, therapeutic cure, tolerability, and treatment compliance. The secondary outcome variable was therapeutic success. RESULTS: At the end of treatment, therapeutic cure was achieved by 34.1, 41.8, and 39.53% of Groups I, II, and III, respectively. No statistical difference between the groups was observed. CONCLUSIONS: Both treatments were effective for the treatment of interdigital-type tinea pedis, while better results were observed on patients that received the higher concentration of the extract.

Efecto de Bursera grandiflora sobre el peso corporal y lipemia en ratones obesos / Effect of Bursera grandiflora on body weight and lipemia in obese mice

Obesity and overweight are clearly related to the caloric intake that leads to a chronic systemic inflammation of low degree. Pharmacological therapy is highly recommended for this disease. Within the Burseraceae family there are species used empirically for the treatment of obesity; one of them, Bursera grandiflora, is also reported for exhibiting anti-inflammatory properties. Evaluate the effect produced by B. grandiflora on a mice model of obesity, its toxicity potential, and chemical identification of the major chemical compound. Mice of the C57B1/6 strain were used. All animals were fed for 8 weeks with a hypercaloric diet. Afterwards, during 7 weeks, animals were daily administered with the hidro-alcoholic extract from B. grandiflora or water (control). At the end of the administration period, plasma cholesterol and triglycerides levels were measured. Moreover, toxicity tests were carried out in mice after acute and chronic administering the B. grandiflora extract. Finally, the main compound in the active extract was identified. Animals treated with the B. grandiflora extract showed a greater food consumption and, paradoxically, without increasing the body weight. Moreover, a decrease of the plasma-triglycerides was observed. Toxicological evaluation showed that the extract administration did not produce any death of the experimental animals or modifications on the organs or behavior. The major compound identified in the extract was scopoletin.

El sobrepeso y la obesidad están claramente vinculados con la ingesta calórica que lleva a la instalación crónica de inflamación sistémica de bajo grado. La terapia farmacológica es altamente recomendable para este padecimiento. Dentro de la familia Burseraceae existen especies utilizadas para el tratamiento de la obesidad, de las cuales, Bursera grandiflora es referida también por su efecto anti-inflamatorio. Evaluar el efecto de B. grandiflora en un modelo de obesidad, su potencial toxicológico, e identificación del compuesto mayoritario. Se utilizaron ratones C57Bl/6 alimentados durante 8 semanas con dieta hipercalórica. Posteriormente, durante 7 semanas se administró diariamente un extracto hidroalcohólico de B. grandiflora o agua (control). Al final se cuantificaron colesterol y triglicéridos. Además, se realizaron pruebas de toxicidad en ratones administrando el extracto de B. grandiflora en forma aguda y subcrónica. Finalmente, se identificó el compuesto mayoritario. Los animales tratados con B. grandiflora registraron el mayor consumo de alimento y, paradójicamente, sin mostrar un crecimiento ponderal y con una disminución de los triglicéridos. Las evaluaciones de toxicología revelaron que la administración del extracto no produjo muertes en los animales de experimentación, ni cambios orgánicos o de comportamiento. El compuesto mayoritario identificado en el extracto activo fue escopoletina.

Exploratory study on the effectiveness of a standardized extract from Ageratina pichinchensis in patients with chronic venous leg ulcers.

The aerial parts of the species Ageratina pichinchensis, popularly known as "axihuitl", have been empirically used in Mexico for wound-healing purposes. The evaluation of an extract from A. pichinchensis (in an in vivo model) demonstrated its capacity to reduce, in a significant manner, the time required for wound healing in rodent skin. This same extract showed (in vitro) a capacity of encouraging proliferation of normal human fetal lung fibroblasts (MRC-5). This study's objective was to evaluate, in a clinical trial, the effectiveness and tolerability of the topical administration of a product elaborated with the standardized extract from the aerial parts of A. pichinchensis in patients with chronic venous leg ulcers, and to compare the effect with a control group treated with 7 % propylene glycol alginate. In this study, a total of 34 patients were included (50 % in each group). Six patients of the control group withdrew from the treatment, three of these because of lack of recovery. In the experimental group, 2 participants withdrew from the study, but none of these due to treatment or clinical-evolution reasons. The A. pichinchensis extract showed therapeutic effectiveness in one hundred percent of the patients treated with it, while the control treatment achieved this condition in 81.8 % of the control group patients. Ulcer size reduction resulted significantly higher (p < 0.010) in the group of patients administered the experimental treatment, which allows us to assure that the A. pichinchensis standardized extract is effective in the treatment of chronic venous leg ulcers and, compared with the 7 % propylene glycol alginate formula, achieves a significant reduction of the time required for the ulcers to heal.

Effect on the wound healing process and in vitro cell proliferation by the medicinal Mexican plant Ageratina pichinchensis.

The species Ageratina pichinchensis (Asteraceae) has been used for a long time in Mexican traditional medicine for the treatment of different skin conditions and injuries. In this study, the healing capacity of the plant extracts obtained was evaluated and, in order to understand the mechanism of healing, we also analyzed its effect on cell proliferation IN VITRO, cytotoxicity, and skin irritation. Different extracts obtained from the aerial parts of A. pichinchensis, topically administrated, were evaluated in a healing model by scalpel-blade incision on the rat. The extracts, at 10 % concentrations, were administrated daily during an eight-day period. A control group, to which the vehicle was administered, was used; while fibrinolysin (Fibrase SA®) was administered for positive control purposes. Reduction in wound size and the histological characteristics of the skin at the end of the treatment were evaluated. Cytotoxicity was evaluated in cell lines KB (nasopharyngeal carcinoma), UISO (squamous cell carcinoma of the cervix), OVCAR (ovarian carcinoma), and HCT-15 (colon carcinoma). In addition, the effect on cell proliferation of cell line MRC-5 (normal cells from human fetal lung) was measured, and skin irritation was evaluated. The results showed an important healing capacity of A. pichinchensis extract in noninfected wounds; the aqueous extract was found to be the most efficient. The extracts exhibited no cytotoxic effect; however, there was an effect that promoted cell proliferation in cell line MRC-5. The products tested demonstrated no skin irritant effects.

Clinical trial to compare the effectiveness of two concentrations of the Ageratina pichinchensis extract in the topical treatment of onychomycosis.

UNLABELLED: The plant species Ageratina pichinchensis has been used, for many years, in Mexican traditional medicine for the treatment of superficial mycosis. AIM OF THE STUDY: This study compared the therapeutic effectiveness and tolerability of two concentrations of the standardized extract from Ageratina pichinchensis (12.6 and 16.8%) on patients with clinical and mycological diagnosis of mild and moderate onychomycosis. MATERIALS AND METHODS: Two identical phytopharmaceuticals (containing the standardized extract from Ageratina pichinchensis) in nail lacquer solution for topical administration were evaluated in a double-blind clinical trial. Treatments were administered for 6 months to patients distributed in two groups. RESULTS AND DISCUSSION: Of 122 patients who agreed to participate in the study, 103 (84.4%) concluded the treatment. The therapeutic effectiveness exhibited by the 12.6% Ageratina pichinchensis extract was 67.2%, while that of the 16.8% Ageratina pichinchensis extract was 79.1%. Regarding clinical evolution, analysis of results at the end of treatment evidenced that the 16.8% concentration possesses higher therapeutic effectiveness with a significant statistical difference (p=0.010). No treatment produced side effects. CONCLUSION: Both concentrations of phytopharmaceuticals possess high rates of effectiveness on patients with mild and moderate onychomycosis, and the formulation with a 16.8% concentration possesses higher effectiveness.