Antidiabetic and Toxicological Effects of the Tea Infusion of Summer Collection from Annona cherimola Miller Leaves.

Annona cherimola Miller (Ac) is a plant used in Mexican traditional medicine for the treatment of diabetes. In this work, the tea infusion extracts obtained from 1.5 g of leaf powder from Ac collected in May (AcMa), June (AcJun), July (AcJul), and August (AcAu) were evaluated on streptozocin-induced diabetic (STID) mice and for subchronic toxicity in STID and non-diabetic (ND) mice. In addition, extracts were subjected to high-performance liquid chromatography with diode array detection (HPLC-DAD). Results showed that the tea infusion extract of the sample collected in August (AcAu) exhibited the most significant antihyperglycemic activity during all acute assays. The analysis of the extracts (AcMa, AcJu, AcJul, and AcAu) by HPLC-DAD revealed that flavonoid glycosides, rutin, narcissin, and nicotiflorin were the major components. In addition, the sample AcAu contained the best concentration of flavonoids. In the case of subchronic oral toxicity, the AcAu sample did not cause mortality in STID mice, and histopathological analysis revealed significant improvement in the changes associated with diabetes in the liver and kidneys. These findings suggest that the Ac leaves collected in August may be a source of flavonoids such as rutin, with antidiabetic potential. In addition, these findings support the use of Ac to treat diabetes in traditional medicine.

The addition of different oils in the diet regulates the expression of adipocytokine signaling genes in sheep longissimus dorsi muscle.

Nutrition is an important factor that regulates the expression of several genes. The aim of this work was to analyze the effects of diets containing additions of different oils on the regulation of the adipocytokine signaling gene expressions in sheep longissimus dorsi muscle. Forty males and non-neutered sheep were kept in individual cages and fed under four different treatments: control treatment (concentrate and forage) and the other three treatments containing the concentrate and forage plus 4% oil (yellow grease, soybean and palm oils). After slaughter, samples of the longissimus dorsi muscle were collected. RNA extraction followed by Real Time PCR for five adipocytokine signaling genes. ANOVA was performed followed by the Dunnett's test (0.01). The normalized expressions of the ACLY gene were not significant between treatments to control, but for the ALDOC gene, all oil-supplemented treatments were significantly downregulated relative to the control treatment. The DUSP gene was not significantly expressed between the oil-supplemented treatments to control treatment. The ENPP1 gene was significantly upregulated with the addition of palm oil and yellow grease and the FASN gene was only significantly expressed in soybean oil-supplemented treatment to control treatment. It was concluded that the addition of different oils in the sheep diet regulated the expression of most genes for up or down, which can influence the metabolic pathways responsible for the fatty acid biosynthesis in the sheep longissimus dorsi muscle.

Antitumor Potential of Annona muricata Linn. An Edible and Medicinal Plant in Mexico: In Vitro, In Vivo, and Toxicological Studies.

Annona muricata (Am) is a plant used in traditional Mexican medicine to treat cancer. In this study, ethanol extracts of Am collected in Acapulco and Tecpan from Guerrero state were evaluated orally on Balb/c mice inoculated with 4T1 cells, for cytotoxic activity (CA) on 4T1 cells, in brine shrimp lethality assay (BSLA), and for acute oral toxicity in mice. In addition, ethanol extracts were subjected to high-performance liquid chromatography (HPLC) with diode array detection. Results showed that the extracts collected in December in Acapulco (AcDe) and Tecpan (TeDe) exhibited the most significant antitumor and cytotoxic activity. In the BSLA, the most important effect was observed in the extracts from Acapulco and Tecpan collected in June (AcJu) and August (TeAg), respectively. The samples from Acapulco (AcJu, and AcAg) and Tecpan (TeJu and TeAg) showed the highest toxicity. The analysis of the extracts, AcDe and TeDe, by HPLC revealed that flavonoids, rutin, narcissin, and nicotinflorin were the major components. These findings suggest that extracts from Am collected in Acapulco and Tecpan in the month of December may be an important source to obtain flavonoid glycosides with anticancer potential specifically against breast cancer. This also supports the use of Am to treat cancer in Mexican traditional medicine.

Antihyperglycemic and Antilipidemic Properties of a Tea Infusion of the Leaves from Annona cherimola Miller on Streptozocin-Induced Type 2 Diabetic Mice.

The antihyperglycemic and antilipidemic effects of the tea infusion extracts of leaves from Annona cherimola Miller (IELAc-0.5, IELAc-1.5, and IELAc-3.0) were evaluated on normoglycemic (NG) and streptozocin-induced diabetic (STID) mice. In the acute test, IELAc-1.5 at 300 mg/kg bodyweight (bw) exhibited antihyperglycemic activity on STID mice since the first hour of treatment. Then, its antidiabetic potential was analyzed in a subchronic evaluation. IELAc-1.5 was able to reduce the blood glucose level, glycated hemoglobin (HbA1c), cholesterol (CHO), and triglycerides (TG); high-density lipoprotein (HDL) showed an increase at the end of treatment. IELAc-1.5 did not modify the urine profile at the end of the evaluation, and neither toxicity nor macroscopic organ damage were observed in acute and subchronic assays. In addition, a major flavonol glycoside present in the tea infusion extracts was identified using high-performance liquid chromatography with diode array detection (HPLC-DAD). The analysis of the tea infusion extracts by HPLC revealed that rutin was the major component. This study supports the use of tea infusions from Annona cherimola for the treatment of diabetes and suggests that rutin could be responsible, at least in part, for their antidiabetic properties.

Antihyperglycemic and Lipid Profile Effects of Salvia amarissima Ortega on Streptozocin-Induced Type 2 Diabetic Mice.

Salvia amarissima Ortega was evaluated to determinate its antihyperglycemic and lipid profile properties. Petroleum ether extract of fresh aerial parts of S. amarissima (PEfAPSa) and a secondary fraction (F6Sa) were evaluated to determine their antihyperglycemic activity in streptozo-cin-induced diabetic (STID) mice, in oral tolerance tests of sucrose, starch, and glucose (OSTT, OStTT, and OGTT, respectively), in terms of glycated hemoglobin (HbA1c), triglycerides (TG), and high-density lipoprotein (HDL). In acute assays at doses of 50 mg/kg body weight (b.w.), PEfAPSa and F6Sa showed a reduction in hyperglycemia in STID mice, at the first and fifth hour after of treatment, respectively, and were comparable with acarbose. In the sub-chronic test, PEfAPSa and F6Sa showed a reduction of glycemia since the first week, and the effect was greater than that of the acarbose control group. In relation to HbA1c, the treatments prevented the increase in HbA1c. In the case of TG and HDL, PEfAPSa and F6Sa showed a reduction in TG and an HDL increase from the second week. OSTT and OStTT showed that PEfAPSa and F6Sa significantly lowered the postprandial peak at 1 h after loading but only in sucrose or starch such as acarbose. The results suggest that S. amarissima activity may be mediated by the inhibition of disaccharide hydrolysis, which may be associated with an α-glucosidase inhibitory effect.

Antihyperglycemic Effects of Annona diversifolia Safford and Its Acyclic Terpenoids: α-Glucosidase and Selective SGLT1 Inhibitiors.

Annona diversifolia Safford and two acyclic terpenoids were evaluated to determine their antihyperglycemic activity as potential α-glucosidase and selective SGLT-1 inhibitiors. Ethanolic extract (EEAd), chloroformic (CHCl3Fr), ethyl acetate (EtOAcFr), aqueous residual (AcRFr), secondary 5 (Fr5) fractions, farnesal (1), and farnesol (2) were evaluated on normoglycemic and streptozocin-induced diabetic mice. EEAd, CHCl3Fr, Fr5, (1) and (2) showed antihyperglycemic activity. The potential as α-glucosidase inhibitors of products was evaluated with oral sucrose and lactose tolerance (OSTT and OLTT, respectively) and intestinal sucrose hydrolysis (ISH) tests; the potential as SGLT-1 inhibitors was evaluated using oral glucose tolerance (OGTT), intestinal glucose absorption (IGA), and urinary glucose excretion (UGE) tests. In OSTT and OLTT, all treatments showed significant activity at two and four hours. In ISH, half maximal effective concentrations (CE50) of 565, 662 and 590 µg/mL, 682 and 802 µM were calculated, respectively. In OGTT, all treatments showed significant activity at two hours. In IGA, CE50 values of 1059, 783 and 539 µg/mL, 1211 and 327 µM were calculated, respectively. In UGE Fr5, (1) and (2) showed significant reduction of the glucose excreted compared with canagliflozin. These results suggest that the antihyperglycemic activity is mediated by α-glucosidase and selective SGLT-1 inhibition.

Exercitando o corpo e alegrando a alma: relato de experiência sobre incentivo à atividade física / Exercising the body and cheering the soul: experience report about the incentive to physical activity / Ejercitando el cuerpo y alegrando el alma: relato de experiencia sobre incentivo a la actividad física

A construção do Sistema Único de Saúde fomentou a reorganização de todo o sistema, sendo a implementação da Atenção Básica uma das principais estratégias para alcançar esse objetivo. Nesse contexto, a parceria entre Residências Multiprofissionais em Saúde e as equipes de Estratégia de Saúde da Família apresenta-se como uma alternativa para promover a mudança da prática assistencial em saúde. A Política Nacional de Promoção da Saúde aponta alguns eixos de atuação, entre eles, o incentivo a atividade física. Portanto, o objetivo deste trabalho foi descrever a experiência de residentes multiprofissionais em Saúde da Família, na condução de um grupo de atividade física com usuários de uma unidade básica de saúde. Para tanto, iniciou-se o grupo no mês de abril de 2015, realizando encontros semanais, com duração de uma hora e participação de duas agentes comunitárias de saúde. A faixa etária das participantes variou entre 35 a 70 anos. Percebeu-se que as atividades de educação em saúde, como as realizadas nesta pesquisa, possibilitaram a percepção da importância da inserção e colaboração da residência nas atividades desenvolvidas pela Estrategia de Saúde da Família. Assim, concluiu-se que a colaboração da residência fortalece o vínculo do profissional de saúde com a comunidade e possibilita que ele levante as demandas da comunidade e atue efetivamente sobre elas.

The construction of the Unified Health System has fostered the reorganization of the entire system, being the implementation of Primary Care one of the main strategies to achieve this goal. In this context, the partnership between Multiprofessional Residencies in Health and the Family Health Strategy teams presents itself as an alternative to promote the change in health care practice. The National Health Promotion Policy points to some areas of activity, among them, the incentive to physical activity. Therefore, the objective of this study was to describe the experience of multiprofessional residents in Family Health, in the conduction of a physical activity group with users of a basic health unit. For that purpose, the group started in April 2015, holding one-hour weekly meetings with the participation of two community health agents. The participants' age ranged from 35 to 70 years. It was noticed that Health education activities such as those carried out by this research enabled the perception of the importance of the insertion and collaboration of residency in the activities developed by the Family Health Strategy. Thus, it was possible to conclude that the collaboration of residency strengthens the bond between the health professional and the community and enables him to raise the demands of the community and act effectively on them.

La construcción del Sistema Único de Salud fomentó la reorganización de todo el sistema, siendo la implementación de la Atención Básica una de las principales estrategias para alcanzar ese objetivo. En ese contexto, la asociación entre Residencias Multiprofesionales en Salud y los equipos de Estrategia de Salud de la Familia presentase como una alternativa para promover el cambio de la práctica asistencial en salud. La política nacional de promoción de la salud apunta algunos ejes de actuación, entre ellos, el incentivo a la actividad física. Por lo tanto, el objetivo de este trabajo fue describir la experiencia de residentes multiprofesionales en Salud de la Familia, en la conducción de un grupo de actividad física con usuarios de una unidad básica de salud. Para ello, fue iniciado el grupo en el mes de abril de 2015, realizando encuentros semanales, con duración de una hora y participación de dos agentes comunitarias de salud. El grupo de edad de las participantes varió entre 35 y 70 años. Percibióse que las actividades de educación en salud, como las realizadas en esta investigación, posibilitaron la percepción de la importancia de la inserción y colaboración de la residencia en las actividades desarrolladas por la Estrategia de Salud de la Familia. Así, concluyóse que la colaboración de la residencia fortalece el vínculo del profesional de salud con la comunidad y posibilita que él levante las demandas de la comunidad y actúe efectivamente sobre ellas.

Antiprotozoal Activities of Tiliroside and other Compounds from Sphaeralcea angustifolia (Cav.) G. Don.

BACKGROUND: Sphaeralcea angustifolia (Malvaceae) is extensively used in Mexican traditional medicine for the treatment of gastrointestinal disorders such as diarrhea and dysentery. OBJECTIVE: The current study was to validate the traditional use of S. angustifolia for the treatment of diarrhea and dysentery on biological grounds using in vitro antiprotozoal activity and computational experiments. MATERIALS AND METHODS: The ethanol extract, subsequent fractions, flavonoids, phenolic acids, and a sterol were evaluated on Entamoeba histolytica and Giardia lamblia trophozoites. Moreover, molecular docking studies on tiliroside were performed; it was tested for its affinity against pyruvate:ferredoxin oxidoreductase (PFOR) and fructose-1,6-bisphosphate aldolase (G/FBPA), two glycolytic enzymes of anaerobic protozoa. RESULTS: Bioassay-guided fractionation of extract of the aerial parts of S. angustifolia gives tiliroside and apigenin, caffeic acid, protocatechuic acid, and ß-sitosterol. The in vitro antiprotozoal assay showed that tiliroside was the most potent antiprotozoal compound on both protozoa with 50% inhibitory concentration values of 17.5 µg/mL for E. histolytica and 17.4 µg/mL for G. lamblia. Molecular docking studies using tiliroside showed its probable antiprotozoal mechanism with PFOR and G/FBPA. In both cases, tiliroside showed high affinity and inhibition constant theoretic for PFOR (lowest free binding energy from -9.92 kcal/mol and 53.57 µM, respectively) and G/FBPA (free binding energy from -7.17 kcal/mol and 55.5 µM, respectively), like to metronidazole, revealing its potential binding mode at molecular level. CONCLUSION: The results suggest that tiliroside seems to be a potential antiprotozoal compound responsible for antiamoebic and antigiardial activities of S. angustifolia. Its in vitro antiprotozoal activities are in good agreement with the traditional medicinal use of S. angustifolia in gastrointestinal disorders such as diarrhea and dysentery. SUMMARY: Bioassay-guided fractionation of extract of the aerial parts of S. angustifolia gives: tiliroside and apigenin, caffeic acid, protocatechuic acid) and ß-sitosterol. The in vitro antiprotozoal assay showed that tiliroside was the most potent antiprotozoal compound on both protozoa with IC50 values of 17.5 mg/mL for E. histolytica and 17.4 µg/mL for G. lamblia. Molecular docking studies using tiliroside showed its probable antiprotozoal mechanism with PFOR and G/FBPA. In both cases tiliroside showed high affinity and inhibition constant theoretic for PFOR (lowest free binding energy from -9.92 kcal/mol and 53.57 mM, respectively) and G/FBPA (free binding energy from -7.17 kcal/mol, respectively and 55.5 µM), like to metronidazole, revealing its potential binding mode at molecular level. The results suggest that tiliroside seems to be a potential antiprotozoal compound responsible for antiamoebic and antigiardial activities of Sphaeralcea angustifolia. Abbreviations Used: PFOR: Pyruvate:ferredoxin oxidoreductase; G/FBPA: Fructose 1,6 bisphosphate aldolase.

Antihyperglycemic Activity of the Leaves from Annona cherimola Miller and Rutin on Alloxan-induced Diabetic Rats.

BACKGROUND: Annona cherimola, known as "chirimoya" has been reported in Mexican traditional medicine for the treatment of diabetes. OBJECTIVE: The aims of the present study were to validate and assess the traditional use of A. cherimola as an antidiabetic agent. MATERIALS AND METHODS: The ethanol extract from A. cherimola (300 mg/kg, EEAc), subsequent fractions (100 mg/kg), and rutin (30 mg/kg) were studied on alloxan-induced type 2 diabetic (AITD) and normoglycemic rats. In addition, oral glucose tolerance test (OGTT) and oral sucrose tolerance test (OSTT) were performed in normoglycemic rats. Molecular docking technique was used to conduct the computational study. RESULTS: Bioassay-guided fractionation of EEAc afforded as major antihyperglycemic compound, rutin. EEAc attenuated postprandial hyperglycemia in acute test using AITD rats (331.5 mg/dL) carrying the glycemic levels to 149.2 mg/dL. Rutin after 2 h, attenuated postprandial hyperglycemia in an acute assay using AITD rats such as EEAc, with maximum effect (150.0 mg/dL) being seen at 4 h. The antihyperglycemic activities of EEAc and rutin were comparable with acarbose (151.3 mg/dL). In the subchronic assay on AITD rats, the EEAc and rutin showed a reduction of the blood glucose levels since the 1st week of treatment, reaching levels similar to normoglycemic state (116.9 mg/kg) that stayed constant for the rest of the assay. OGTT and OSTT showed that EEAc and rutin significantly lowered blood glucose levels in normoglycemic rats at 2 h after a glucose or sucrose load such as acarbose. Computational molecular docking showed that rutin interacted with four amino acids residues in the enzyme α-glucosidase. CONCLUSION: The results suggest that rutin an α-glucosidase inhibitor was responsible in part of the antihyperglycemic activity of A. cherimola. Its in vivo antihyperglycemic activity is in good agreement with the traditional use of A. cherimola for the treatment of diabetes. SUMMARY: The ethanol extract from Annona cherimola (300 mg/kg, EEAc), subsequent fractions (100 mg/kg) and rutin (30 mg/kg) were studied on alloxan-induced type 2 diabetic (AITD) and normoglycemic rats. The results suggest that rutin; an α-glucosidase inhibitor was responsible in part of the antihyperglycemic activity of A. cherimola. Its in vivo antihyperglycemic activity is in good agreement with the traditional use of A. cherimola for the treatment of diabetes. Abbreviations Used: EEAc: The ethanol extract from Annona cherimola, AITD: Alloxan-induced type 2 diabetic rats, OGTT: Oral glucose tolerance test, OSTT: Oral sucrose tolerance test, DM: Diabetes mellitus.

Antiprotozoal Constituents from Annona cherimola Miller, a Plant Used in Mexican Traditional Medicine for the Treatment of Diarrhea and Dysentery.

BACKGROUND: Annona cherimola Miller (Annonaceae) is a medicinal plant frequently recommended in Mexican traditional medicine for the treatment of gastrointestinal disorders such as diarrhea and dysentery. OBJECTIVE: This work was undertaken to obtain information that support the traditional use of A. cherimola, on pharmacological basis using in vitro and computational experiments. MATERIAL AND METHODS: Bioassay-guided fractionation of the ethanol extract of the leaves of A. cherimola afforded five phenolic compounds: caffeic acid, quercetin, kaempferol, nicotinflorin, and rutin. RESULTS: The in vitro antiprotozoal assay showed that kaempferol was the most potent antiamoebic and antigiardial compound with IC50 values of 7.9 µg/mL for Entamoeba histolytica and 8.7 µg/mL for Giardia lamblia. Computational molecular docking study showed that kaempferol interacted in a region different than metronidazole in the enzyme pyruvate: ferredoxin oxidoreductase (PFOR). CONCLUSION: Considering that PFOR is a target of metronidazole; kaempferol may be a lead compound for the development of novel antiprotozoal agent. Also, these findings give support to the use of A. cherimola in the traditional medicine from México for the treatment of diarrhea and dysentery. SUMMARY: Bioassay-guided fractionation of the ethanol extract of the leaves of Annona cherimola afforded five phenolic compounds: caffeic acid, quercetin, kaempferol, nicotinflorin and rutin. The in vitro antiprotozoal assay showed that kaempferol was the most potent antiamoebic and antigiardial compound with IC50 values of 7.9 µg/mL for Entamoeba histolytica and 8.7 µg/mL for Giardia lamblia. Computational molecular docking study showed that kaempferol interacted in a region different that metronidazole in the enzyme pyruvate: ferredoxin oxidoreductase. Abbreviations used: PFOR:Pyruvate:ferredoxin oxidoreductase, G: lamblia: Giardia lamblia, E: histolytica: Entamoeba histolytica.

Evaluation of the medicinal properties of Cyrtocarpa procera Kunth fruit extracts.

BACKGROUND: The fruit of Cyrtocarpa procera is used to treat stomach diseases by people living in San Rafael, Coxcatlan, Puebla. This work investigated the antibacterial, antioxidant, cytotoxic and anti-inflammatory activities of the fruit produced by this species. METHODS: Methanol extract was obtained by maceration. After obtaining the methanol extract (MeOH1), methanol subextract (MeOH2) and hexane (H) were obtained. The antibacterial activities of MeOH1, MeOH2 and H were evaluated through disc-diffusion. The quenching of free radicals was evaluated by decolorizing a methanolic DPPH solution. The cytotoxic activity of MeOH2 was evaluated by in vitro assay system of growth inhibition of human cervical carcinoma cell line (CasKi). The IL-1ß and TNF-α were determined through ELISA in the supernatants of the macrophage cell line (RAW 264.7). The MeOH2 subextract was separated by column chromatography, seventy-three fractions were collected. RESULTS: The Gram-positive and -negative bacteria examined were sensitive to MeOH1 and MeOH2; the MeOH2 was bactericidal toward Staphyloccocus aureus (MIC = 4 mg/mL) and Vibrio cholera (MIC = 4 mg/mL). The MeOH2 inhibited the DPPH radical (SC50 = 69.7 µg/mL), but a cytotoxicity assay revealed that the extract is not toxic according to the National Cancer Institute (LD50 = 22.03 µg/mL). The production of proinflammatory cytokines (IL- 1ß and TNF- α) by LPS- stimulated macrophages was reduced after the treatments. The methanol extract contained various organic acids, such as citric acid, palmitic acid and α- linoleic acid. CONCLUSIONS: The fruits of Cyrtocarpa procera are employed to treat ailments such as diarrhea, in this study were demonstrated some biological activities involved in a bacterial infection. This is the first research about of the medicinal properties of C. procera fruit.

Anti-diarrheal activity of (-)-epicatechin from Chiranthodendron pentadactylon Larreat: experimental and computational studies.

ETHNOPHARMACOLOGICAL RELEVANCE: Chiranthodendron pentadactylon Larreat is frequently used in Mexican traditional medicine as well as in Guatemalan for several medicinal purposes, including their use in the control of diarrhea. AIM OF THE STUDY: This work was undertaken to obtain additional information that support the traditional use of Chiranthodendron pentadactylon Larreat, on pharmacological basis using the major antisecretory isolated compound from computational, in vitro and in vivo experiments. MATERIALS AND METHODS: (-)-Epicatechin was isolated from ethyl acetate fraction of the plant crude extract. In vivo toxin (Vibrio cholera or Escherichia coli)-induced intestinal secretion in rat jejunal loops models and sodium dodecyl sulphate-polyacrylamide gel electrophoresis (SDS-PAGE) analysis on Vibrio cholera toxin were used in experimental studies while the molecular docking technique was used to conduct computational study. RESULTS: The antisecretory activity of epicatechin was tested against Vibrio cholera and Escherichia coli toxins at oral dose 10 mg/kg in the rat model. It exhibited the most potent activity on Vibrio cholera toxin (56.9% of inhibition). In the case of Escherichia coli toxin its effect was moderate (24.1% of inhibition). SDS-PAGE analysis revealed that both (-)-epicatechin and Chiranthodendron pentadactylon extract interacted with the Vibrio cholera toxin at concentration from 80 µg/mL and 300 µg/mL, respectively. Computational molecular docking showed that epicatechin interacted with four amino acid residues (Asn 103, Phe 31, Phe 223 and The 78) in the catalytic site of Vibrio cholera toxin, revealing its potential binding mode at molecular level. CONCLUSION: The results derived from computational, in vitro and in vivo experiments on Vibrio cholera and Escherichia coli toxins confirm the potential of epicatechin as a new antisecretory compound and give additional scientific support to anecdotal use of Chiranthodendron pentadactylon Larreat in Mexican traditional medicine to treat gastrointestinal disorders such as diarrhea.

Antisecretory activity from the flowers of Chiranthodendron pentadactylon and its flavonoids on intestinal fluid accumulation induced by Vibrio cholerae toxin in rats.

ETHNOPHARMACOLOGICAL RELEVANCE: The flowers of Chiranthodendron pentadactylon Larreat. (Sterculiaceae) has been traditionally used as folk medicine in Mexico for the treatment of gastrointestinal disorders such as diarrhea and dysentery. AIM OF THE STUDY: This study aimed to assess the antisecretory activity which supports the therapeutic use of Chiranthodendron pentadactylon and its flavonoids to treat diarrhea. MATERIALS AND METHODS: The methanol extract of Chiranthodendron pentadactylon, subsequent fractions, and flavonoids were evaluated on cholera toxin-induced intestinal secretion in rat jejunal loops model. RESULTS: Three antisecretory flavonoids were isolated by bioassay-guided purification, namely, isoquercitrin 3, (+)-catechin 4 and (-)-epicatechin 5. Among them, epicatechin exhibited the most potent antisecretory activity with ID(50) of 8.3 microM/kg. Its potency was close that of to loperamide (ID(50) 6.1 microM/kg), drug used as control. Isoquercitrin (ID(50) 19.2 microM/kg) and catechin (ID(50) 51.7 microM/kg) showed moderate and weak activity, respectively. CONCLUSION: The results of the present study lend some support to the anecdotal report for the traditional use of the flowers of Chiranthodendron pentadactylon in the control of dysentery.

In vivo antigiardial activity of three flavonoids isolated of some medicinal plants used in Mexican traditional medicine for the treatment of diarrhea.

Mexican traditional medicine uses a great variety of plants in the treatment of gastrointestinal disorders such as diarrhea. In order to understand the properties of some of their chemical constituents, three flavonoids (kaempferol, tiliroside and (-)-epicatechin) isolated from Geranium mexicanum, Cuphea pinetorum, Helianthemum glomeratum, and Rubus coriifolius, were assayed to demonstrate their in vivo antiprotozoal activity; using an experimental infection of Giardia lamblia in suckling female CD-1 mice. Compounds tested showed antigiardial activity with values of ED(50) (micromol/kg) 0.072 for (-)-epicatechin, 2.057 for kaempferol and 1.429 for tiliroside. The most active flavonoid was the (-)-epicatechin, its activity was higher than metronidazole and emetine, drugs used as positive controls. In the case of kaempferol and tiliroside their potency was close to that of the metronidazole, but far less than emetine.

Antigiardial activity of methanolic extracts from Helianthemum glomeratum Lag. and Rubus coriifolius Focke in suckling mice CD-1.

The antigiardial activity of crude methanolic extracts from Helianthemum glomeratum and Rubus coriifolius, plants used in Mexican traditional medicine for the treatment of diarrhea and dysentery, were demonstrated using experimental infections of Giardia lamblia in suckling female CD-1 mice. In vivo antigiardial activity was studied to determine the dose required to kill 50% of the trophozoites (ED50). Five single-doses between 1.25 and 20 mg extract/kg body weight were tested. Drugs metronidazole and emetine were used as reference. The ED50 (mg/kg) obtained for the extracts and drugs used as reference was 0.125 for Helianthemum glomeratum, 0.506 for Rubus coriifolius, 0.194 for metronidazole and 0.167 for emetine. Both methanolic extracts showed antigiardial activity, the extract of Helianthemum glomeratum was more active than Rubus coriifolius, and its activity is comparable to metronidazole and emetine. Our results hold the perspective for the utilization of the extracts of these plants as an option to develop of novel antigiardial phytodrugs.

Antiamoebic activity of benzyl glucosinolate from Lepidium virginicum.

In a continuation of our search for potential antiprotozoal agents from plants, we found that a crude extract from the roots of Lepidium virginicum exhibited antiprotozoal activity against Entamoeba histolytica trophozoites (IC(50) of 100.1 micro g/mL). Bioassay-guided fractionation resulted in the isolation of one known glucosinolate responsible for such activity. This compound was identified as benzyl glucosinolate. It showed in vitro activity against Entamoeba histolytica strain HM1-IMSS (IC(50) of 20.4 micro g/mL). The results support the anecdotal reports for the traditional use of L. virginicum roots in the control of diarrhoea and dysentery in the highlands of Chiapas, Mexico.

31P-spectroscopy of frontal lobe in schizophrenia: alterations in phospholipid and high-energy phosphate metabolism.

Studies using 31P-magnetic resonance spectroscopy (MRS) reported on abnormalities in frontal lobe metabolism in schizophrenia. The most consistent findings were a reduction in the resonances of phosphomonoesters (PME) and/or increased phosphodiesters (PDE), which are, respectively, the precursors and the metabolites of membrane phospholipids, thus suggesting an accelerated phospholipid metabolism in the disease. Other studies reported increased high-energy phosphates (ATP-adenosine triphosphate and PCr-phosphocreatine) in schizophrenia, reflecting decreased use of energy in the frontal lobe. We investigated 53 schizophrenic patients (DSM-IV) and 35 healthy controls. Eighteen from these patients were drug nai;ve and the remaining 35 were drug-free for an average of 6 months. Phospholipid metabolism and high-energy phosphates were assessed in the left frontal lobe using 31P-MRS. Psychopathological evaluation was done with the Brief Psychiatric Rating Scale (BPRS) and the Negative Symptoms Rating Scale (NSRS). Neuropsychological evaluation was performed with the Wisconsin Card Sorting Test (WCST), Stroop Test and Wechsler Adult Intelligence Scale. Drug-nai;ve patients showed reduced PDE in the left frontal lobe compared to controls and to previously medicated patients (p<0.05). No differences among the three groups were found regarding the other spectroscopy parameters. In healthy controls, but not in schizophrenics, a negative (and probably physiological) correlation was found between PME and PDE (p<0.01). In schizophrenic patients, ATP was correlated with negative symptoms and with neuropsychological impairment (p<0.01). The lack of a correlation between PME and PDE, as well as the reduction of PDE in schizophrenia, suggest a disrupted phospholipid metabolism in the disease, albeit on a contrary direction of that reported in literature. The relationships of ATP with negative symptoms and neuropsychological deficit suggest an alteration of energetic demand in the frontal lobe of schizophrenic patients, which is in line with the hypofrontality hypothesis of the disease.