Category Archives: Enzymes

Kombucha from Rhizophora mucronata

J Pharm Pharmacogn Res 8(5): 410-421, 2020.

Original Article

The kombucha from Rhizophora mucronata Lam. herbal tea: Characteristics and the potential as an antidiabetic beverage

[Kombucha del té de hierbas de Rhizophora mucronata: Características y potencial como bebida antidiabética]

Hardoko*, Evi K. Harisman, Yunita E. Puspitasari

Department of Fisheries and Product Technology, Faculty of Fisheries and Marine Science, Brawijaya University, Jalan Veteran No. 1, Malang 65145, East Java, Indonesia.
Abstract

Context: Kombucha from tea is reported to be beneficial for health. Moreover, it can be used as a hepatoprotective, antiproliferative, antimicrobial, antidiabetic, and antilipidemic agent and is capable of healing stomach ulcers. But kombucha from other herbal has not been studied, including kombucha from the mangrove (Rhizophora mucronata) fruit.

Aims: To evaluate the characteristics and the antidiabetic potential of kombucha herbal tea from R. mucronata fruit based on in vitro, chemistry, and physical analysis.

Methods: This study was conducted by an experimental method using R. mucronata herbal tea as a kombucha drink with different sugar concentrations (10, 20, 30%) and fermentation time (7, 14, 21 days) with three replications on each experiment. The analyzed parameters were the inhibition of the α-glucosidase enzyme for antidiabetic activity, total phenolics, total acids, and organoleptic characteristics.

Results: The sugar concentration and fermentation time significantly affected the characteristics of the produced kombucha in inhibiting α-glucosidase. The optimum treatment in inhibition was at 10% sugar concentration and 14 days of fermentation time with IC50 of 33.95 ppm. The kombucha from R. mucronata fruit had a pH of 3.11 and contained a total phenolics of 19,679.82 mg GAE/100g, 0.52% of total acids, and was quite preferred by panelists.

Conclusions: Kombucha herbal tea of R. mucronata fruit has the potential as an antidiabetic drink with a lower IC50 value than acarbose drug and commercial kombucha tea.

Keywords: antidiabetic; fruit; a-glucosidase; herbal tea; kombucha; Rhizophora mucronata.

Resumen

Contexto: Se informa que la kombucha del té es beneficiosa para la salud. Además, puede usarse como un agente hepatoprotector, antiproliferativo, antimicrobiano, antidiabético y antilipidémico y es capaz de curar úlceras estomacales. Pero no se ha estudiado la kombucha de otras hierbas, incluida la kombucha de la fruta del mangle (Rhizophora mucronata).

Objetivos: Evaluar las características y el potencial antidiabético del té de hierbas kombucha de la fruta de R. mucronata con base en análisis in vitro, químicos y físicos.

Métodos: Este estudio se realizó mediante un método experimental utilizando té de hierbas de R. mucronata como bebida de kombucha con diferentes concentraciones de azúcar (10, 20, 30%) y tiempo de fermentación (7, 14, 21 días) con tres repeticiones en cada experimento. Los parámetros analizados fueron la inhibición de la enzima α-glucosidasa para la actividad antidiabética, fenoles totales, ácidos totales y características organolépticas.

Resultados: La concentración de azúcar y el tiempo de fermentación afectaron significativamente las características de la kombucha producida en la inhibición de la α-glucosidasa. El tratamiento óptimo en la inhibición fue a una concentración de azúcar del 10% y 14 días de tiempo de fermentación con IC50 de 33,95 ppm. La kombucha de la fruta de R. mucronata tuvo un pH de 3.11 y contenía un contenido de fenoles totales de 19.679,82 mg GAE/100g, 0,52% del ácido total, y fue muy preferida por los panelistas.

Conclusiones: La kombucha del té de hierbas de la fruta de R. mucronata tiene el potencial de ser una bebida antidiabética con un valor de CI50 más bajo que el fármaco de acarbosa y la kombucha del té comercial.

Palabras Clave: antidiabético; fruta; a-glucosidasa; té de hierbas; kombucha; Rhizophora mucronata.

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Citation Format: Hardoko, Harisman EK, Puspitasari YE (2020) The kombucha from Rhizophora mucronata Lam. herbal tea: Characteristics and the potential as an antidiabetic beverage. J Pharm Pharmacogn Res 8(5): 410–421.

© 2020 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

Subchronic toxicity of the low-dose monocrotaline in rats

J Pharm Pharmacogn Res 8(4): 308-315, 2020.

Original Article

Subchronic toxicity of the pulmonary hypertension model due to low-dose monocrotaline in rats

[Toxicidad subcrónica del modelo de hipertensión pulmonar debido a dosis bajas de monocrotalina en ratas]

Vicente Benavides-Cordoba1, Melissa Silva-Medina1, María Ximena Varela2,3, Mauricio Palacios Gómez1*

1Department of Pharmacology, Basic Sciences School, Universidad del Valle. Cali, Colombia.
2Department of Pathology, Universidad del Valle. Cali, Colombia.
3Department of Pathology, Hospital Universitario del Valle. Cali, Colombia.
Abstract

Context: The study of pulmonary hypertension is mainly based on an experimental model that induces this condition using monocrotaline. Even though this model has been in use for decades, the toxic effect of low dose monocrotaline in other systems is not well described.

Aims: To evaluate the renal and hepatic effects of monocrotaline in order to be able to better predict the pharmacodynamic impact that it could have.

Methods: Two groups of rats were used, the first one received monocrotaline following pulmonary hypertension protocol (30 mg/kg) and the second one received saline 0.9%. At day 60 blood from the vena cava was obtained and liver and kidney were extracted for histologic exam. Fulton index (right ventricle hypertrophy measurement) was used to confirm pulmonary hypertension.

Results: The monocrotaline group presents focal interstitial lymphoid infiltration and regeneration foci in the kidney as well as venous congestion of the liver in some of the animals, these changes were not found in the control group. Kidney and liver function tests showed no significant differences. These results show that low-dose monocrotaline model for pulmonary hypertension generates changes on liver and kidney; however, these alterations were not consistent, making it a viable model for evaluating new drugs in this condition.

Conclusions: The present study demonstrates that the low dose of monocrotaline (30 mg/kg) in animals exposed for 60 days does not cause consistent changes in liver and kidney; there were findings in some animals that could be caused by cardiovascular changes generated by pulmonary hypertension.

Keywords: animal models; monocrotaline; pulmonary hypertension; right ventricular hypertrophy, subacute toxicity.

Resumen

Contexto: El estudio de la hipertensión pulmonar se basa principalmente en un modelo experimental que induce esta condición usando monocrotalina. Aunque este modelo ha estado en uso durante décadas, el efecto tóxico de las dosis bajas de monocrotalina en otros sistemas no está bien descrito.

Objetivos: Evaluar los efectos renales y hepáticos de la monocrotalina con el fin de mejorar la predicción del impacto farmacodinámico que podría tener.

Métodos: Se utilizaron dos grupos de ratas, el primero recibió monocrotalina siguiendo el protocolo de hipertensión pulmonar (30 mg/kg) y el segundo recibió solución salina al 0.9%. En el día 60 se obtuvo sangre de la vena cava y se extrajeron hígado y riñón para examen histológico. Se utilizó el índice de Fulton (medición de hipertrofia del ventrículo derecho) para confirmar la hipertensión pulmonar.

Resultados: El grupo de monocrotalina tuvo focos de infiltración linfoide intersticial focal y focos de regeneración en el riñón, así como congestión venosa del hígado en algunos de los animales, estos cambios no se encontraron en el grupo de control. Las pruebas de función renal y hepática no mostraron diferencias significativas. Estos resultados muestran que el modelo de dosis bajas de monocrotalina para la hipertensión pulmonar genera cambios en el hígado y los riñones; sin embargo, estas alteraciones no fueron consistentes, por lo que es un modelo viable para evaluar nuevos medicamentos en esta condición.

Conclusiones: El presente estudio demuestra que la dosis baja de monocrotalina (30 mg/kg) en animales expuestos durante 60 días no ocasiona cambios consistentes en el hígado y los riñones; Hubo hallazgos en algunos animales que podrían ser causados por cambios cardiovasculares generados por la hipertensión pulmonar.

Palabras Clave: hipertensión pulmonar; hipertrofia ventricular derecha; modelos animales; monocrotalina; toxicidad subaguda.

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Citation Format: Benavides-Cordoba V, Silva-Medina M, Varela MX, Palacios Gómez M (2020) Subchronic toxicity of the pulmonary hypertension model due to low-dose monocrotaline in rats. J Pharm Pharmacogn Res 8(4): 308–315.

© 2020 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

Pleurotus restores liver function in malnutrition

J Pharm Pharmacogn Res 8(1): 32-42, 2020.

Original Article

Restoration of liver function in malnourished mice orally administered with Pleurotus ostreatus fruiting bodies extract

[Restablecimiento de la función hepática en ratones malnutridos administrados oralmente con un extracto de cuerpos fructíferos de Pleurotus ostreatus]

Gabriel Llauradó1*, Yaixa Beltrán1, Humberto J. Morris1, Ebert Marcos2, Usnavia Díaz3, Jane Marcos2, Jesús García4, Dunilka Disotuar4, Paul Cos5

1Centre of Studies for Industrial Biotechnology (CEBI), Universidad de Oriente, Ave. Patricio Lumumba s/n, Reparto Jiménez, Santiago de Cuba 5, CP 90500, Cuba.
2Centre of Toxicology and Biomedicine, Medical University of Santiago de Cuba, Autopista Nacional km 1 1/2. Apdo Postal 4033. Santiago de Cuba, Cuba.
3Faculty of Medicine, Medical University of Santiago de Cuba, CP 90400, Santiago de Cuba 4, Cuba.
4Pharmacy Department, Faculty of Natural and Exact Sciences, University of Oriente, Ave. Patricio Lumumba s/n, Reparto Jiménez, Santiago de Cuba 5, CP 90500, Cuba.
5Laboratory for Microbiology, Parasitology and Hygiene (LMPH), Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, University of Antwerp, Universiteitsplein 1, 2610 Antwerp, Belgium.
Abstract

Context: Malnutrition is considered worldwide as an important burden because it provokes serious damage in several physiological and metabolic mechanisms, among them the hepatic function. Currently, natural products are being used to reduce the negative impact of some pathological disorders in liver. Pleurotus genus of edible mushrooms has shown a wide spectrum of medicinal effects, but its role in the management of liver complications associated to malnutrition is not clear.

Aims: To evaluate the restoration of hepatic function in BALB/c malnourished mice, orally administered with a crude water extract (CW-P) from Pleurotus ostreatus fruiting bodies.

Methods: Animals (8-week old female BALB/c mice) were  starved  for  3  days  and  then  refed  with  commercial  diet  supplemented  with  or  without CW-P (100 mg/kg) for 8 days. Serum ALP, GGT and amylase activities, hepatic enzymes (ALT, AST, ALP, LDH, GGT), and liver histological examination were assayed.

Results: CW-P (34.3 % proteins, 42.6 % carbohydrates and 3.8 g/ 100 g of phenolics) administered to malnourished mice: (i) increased total serum proteins concentration that was correlated with the stimulation in liver protein anabolism, (ii) alleviated hepatic damage markers such as decrease serum ALP levels as well as, in ALP, GGT y AST activities in liver samples, and (iii) improved liver histological architecture similar to control group with decreased lipid accumulation.

Conclusions: CW-P supplementation favored liver restoration in malnourished mice. Nutritional interventions with this mushroom extract may be suggested to prevent liver complications associated to malnutrition.

Keywords: liver restoration; Pleurotus ostreatus; protein-energy malnutrition.

Resumen

Contexto: La malnutrición se considera un importante problema al provocar daños en varios mecanismos fisiológicos y metabólicos, entre ellos, la función hepática. Los productos naturales son utilizados para reducir el impacto negativo de ciertas patologías en el hígado. Las setas Pleurotus exhiben un amplio espectro de efectos medicinales; sin embargo, no está dilucidado su papel en el tratamiento de trastornos hepáticos asociados a la malnutrición.

Objetivos: Evaluar el restablecimiento de la función hepática en ratones malnutridos y administrados por vía oral con un extracto crudo de cuerpos fructíferos de Pleurotus ostreatus (CW-P).

Métodos: Ratones BALB/c hembras de 8 semanas fueron mantenidos en ayuno durante 3 días, y posteriormente alimentados por 8 días con dieta comercial suplementada o no con CW-P (100 mg/kg). Se evaluó la actividad de las enzimas ALP, GGT y amilasa en suero, de ALT, AST, ALP, LDH y GGT en hígado, y se realizó, además, el examen histológico del órgano.

Resultados: CW-P (proteínas: 34.3%, carbohidratos: 42.6% y fenoles totales: 3.8 g/100 g) administrado a ratones malnutridos: (i) incrementó la concentración de proteínas séricas, correlacionado con la estimulación del anabolismo proteico, (ii) redujo el daño hepático, evidenciado por la disminución de actividad ALP en suero, y ALP, GGT y AST en hígado, y (iii) regeneró la arquitectura histológica del hígado, similar al grupo control, con una disminución de la acumulación de lípidos.

Conclusiones: La suplementación con CW-P favoreció la restauración hepática en ratones malnutridos. La intervención nutricional con dicho extracto podría prevenir complicaciones hepáticas asociadas a la malnutrición.

Palabras Clave: malnutrición proteico-energética; Pleurotus ostreatus; recuperación hepática.

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Citation Format: Llauradó G, Beltrán Y, Morris HJ, Marcos E, Díaz U, Jane Marcos, García J, Disotuar D, Cos P (2020) Restoration of liver function in malnourished mice orally administered with Pleurotus ostreatus fruiting bodies extract. J Pharm Pharmacogn Res 8(1): 32–42.

© 2020 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

Subchronic toxicity studies of cocoa pod husk pectin

J Pharm Pharmacogn Res 6(4): 271-284, 2018.

Original Article | Artículo Original

Subchronic toxicity studies of cocoa pod husk pectin intended as a pharmaceutical excipient in Sprague Dawley rats

[Estudios de toxicidad subcrónica de la pectina de la cáscara de la vaina de cacao destinada a ser un excipiente farmacéutico en ratas Sprague Dawley]

Ofosua Adi-Dako1, 2, Kwabena Ofori-Kwakye1*, Kennedy K.E. Kukuia3, Jerry Asiedu-Larbi4, Alexander Nyarko3, Doris Kumadoh4, Christina Osei-Asare5

1Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, College of Health Sciences, Kwame Nkrumah University of Science and Technology (KNUST), PV Obeng Avenue, Tackie Building, PMB, Kumasi, Ghana.
2Department of Pharmaceutics and Microbiology, University of Ghana School of Pharmacy, Volta Road, Tetteh Larway Building, GA-490-8344, Legon, Accra, Ghana.
3Department of Pharmacology and Toxicology, University of Ghana School of Pharmacy, Volta Road, Tetteh Larway Building, GA-490-8344, Legon, Accra, Ghana.
4Centre for Plant Medicines Research, N4 Mampong, E2-0606-1025, N4, Mampong-Akuapem, Ghana.
5Department of Pharmaceutical Science, Central University, Central University College Road, GN-0370-4944, Miotso, Ghana.

*E-mail: kokwakye.pharm@knust.edu.gh

Abstract

Context: Excipients play a key role in the quality of medicines and contribute to viable delivery systems. This has intensified the search for new natural polymer pharmaceutical excipients. Cocoa pod husks (CPHs) are a rich source of pectin. A study of CPH pectin showed that it possesses the requisite physicochemical properties to be employed as a multi-functional pharmaceutical excipient.  However, the safety of this natural polymer has not been evaluated.

Aims: To conduct sub-chronic toxic effects of CPH pectin in Sprague Dawley rats to assess its safety as a pharmaceutical grade excipient.

Methods: CPH pectin at doses of 0.714, 7.14, and 71.4 mg/kg were administered to male and female Sprague-Dawley rats by oral gavage over a 90-day period. Parameters assessed were food and water intake, urinalysis, serum biochemistry, wet organ weights, histopathology and pentobarbital-induced sleeping time.

Results: CPH pectin at the orally administered doses had no significant effects on feed and water intake nor on biochemical parameters, except elevations in alkaline phosphatase at the medium and high dose in the female rat. There were also reductions in creatine kinase in both male and female rats at the medium dose after 60 days, suggesting a potential cardioprotective effect of CPH pectin.

Conclusions: There were no adverse effects of CPH pectin on the kidneys, wet organ weights and histopathology of the rat tissues. Subchronic administration of cocoa pod husk pectin therefore, has no significant toxic effects.

Keywords: histopathology; oral gavage; pectin; pharmaceutical excipient; Theobroma cacao.

Resumen

Contexto: Los excipientes desempeñan un papel clave en la calidad de los medicamentos y contribuyen a sistemas de administración viables. Esto ha intensificado la búsqueda de nuevos excipientes farmacéuticos de polímeros naturales. Las cáscaras de vainas de cacao (CPH) son una rica fuente de pectina. Un estudio de CPH pectina mostró que posee las propiedades fisicoquímicas requeridas para emplearse como un excipiente farmacéutico multifuncional. Sin embargo, la seguridad de este polímero natural no ha sido evaluada.

Objetivos: Evaluar los efectos tóxicos subcrónicos de la pectina CPH en ratas Sprague Dawley para valorar su seguridad como un excipiente de grado farmacéutico.

Métodos: Se administró pectina CPH a dosis de 0,714; 7,14 y 71,4 mg/kg a ratas Sprague-Dawley machos y hembras por sonda oral durante un período de 90 días. Los parámetros evaluados fueron la ingesta de agua y alimentos, el análisis de orina, la bioquímica sérica, el peso de los órganos húmedos, la histopatología y el tiempo de sueño inducido por pentobarbital.

Resultados: La pectina CPH, en las dosis administradas por vía oral, no tuvo efectos significativos en la ingesta de alimento y agua ni en los parámetros bioquímicos, excepto las elevaciones de la fosfatasa alcalina a la dosis media y alta en las ratas hembras. También hubo reducciones en la creatina cinasa en ratas machos y hembras en la dosis media después de 60 días, lo que sugiere un posible efecto cardioprotector de la pectina CPH.

Conclusiones: No hubo efectos adversos de la pectina CPH en los riñones, el peso de los órganos húmedos y la histopatología de los tejidos de la rata. Por lo tanto, la administración subcrónica de la pectina de la cáscara de la vaina de cacao no tiene efectos tóxicos significativos.

Palabras Clave: excipiente farmacéutico; histopatología; pectina; sonda nasogástrica; Theobroma cacao.

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Citation Format: Adi-Dako O, Ofori-Kwakye K, Kukuia KKE, Asiedu-Larbi J, Nyarko A, Kumadoh D, Osei-Asare C (2018) Subchronic toxicity studies of cocoa pod husk pectin intended as a pharmaceutical excipient in Sprague Dawley rats. J Pharm Pharmacogn Res 6(4): 271–284.

© 2018 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

Antioxidant and neuroprotective effects of gossypitrin

J Pharm Pharmacogn Res 6(2): 72-80, 2018.

Original Article | Artículo Original

Antioxidant and neuroprotective effects of gossypitrin, a flavonoid from Talipariti elatum, against chemical hypoxia-induced PC12 cell death

[Efectos antioxidantes y neuroprotectores de la gossypitrina, flavonoide de Talipariti elatum, frente a la muerte inducida por hipoxia química en células PC12]

María A. Bécquer-Viart1, José González-Yaque2, Luis A. Fonseca-Fonseca3, Yanier Núñez-Figueredo3, Gilberto L. Pardo Andreu1*

1Centro de Estudio para las Investigaciones y Evaluaciones Biológicas, Instituto de Farmacia y Alimentos, Universidad de La Habana, Calle 222, # 2317 e/23 y 31, La Coronela, La Lisa, CP 13600, La Habana, Cuba.
2Departamento de Farmacia, Instituto de Farmacia y Alimentos, Universidad de La Habana, Calle 222, # 2317 e/23 y 31, La Coronela, La Lisa, CP 13600, La Habana, Cuba.
3Centro de Investigación y Desarrollo de Medicamentos, Ave 26, No. 1605 Boyeros y Puentes Grandes, CP 10600, La Habana, Cuba.

*E-mail: gpardo@ifal.uh.cu

Abstract

Context: Some flavonoids have been described as neuroprotectors. Gossypitrin (Gos) is a natural occurring flavonoid and the main bioactive substance from the flowers of Talipariti elatum Sw. (Majagua azul), traditionally used in Cuba as expectorant and antiasthmatic. Only few reports have documented its antioxidant properties.

Aims: To evaluate the antioxidant and cytoprotective effects of Gos against cyanide-induced oxidative stress and cell death in PC12 cells.

Methods: Gos effects on DPPH/ ABTS radical scavenging, ferric reducing power and lipid peroxidation were examined. The ischemia/reperfusion neuronal damage was produced by exposing PC12 cells to KCN in glucose-free medium. Gos was added to the incubation medium 30 min before chemical hypoxia induction. The neuroprotective potential of Gos was assessed by measuring cell viability by the MTT assay, the antioxidant enzymes SOD and CAT, and GSH and lipid peroxidation levels. Rutin (Rut), the well-known antioxidant, was used as a reference compound.

Results: Gos showed a potent intrinsic antioxidant capacity evidenced by low IC50 and EC50 values for DPPH/ABTS/malondialdehyde and ferric reducing power, respectively. Pre-treatment of PC12 cells with Gos, significantly increased their survival against KCN, restored the levels of GSH and the SOD and CAT enzymes activities, as well as reduced the level of lipid peroxidation. Its antioxidant effects were higher than those elicited by Rut.

Conclusions: The results show for the first time the neuroprotective potential of Gos against hypoxic cell damage, probably associated to its antioxidant effects.

Keywords: antioxidant; gossypitrin; hypoxia; ischemia; neuroprotection; PC12.

Resumen

Contexto: Algunos flavonoides se han descrito como neuroprotectores. La gossypitrina (Gos) es un flavonoide natural y la principal sustancia bioactiva en las flores de Talipariti elatum Sw. (Majagua azul), tradicionalmente usada en Cuba como expectorante y antiasmático. Pocos reportes documentan sus propiedades antioxidantes.

Objetivos: Evaluar los efectos antioxidantes y citoprotectores de la Gos frente al estrés oxidativo y la muerte celular inducidos por cianuro en células PC12.

Métodos: Se examinaron los efectos de la Gos en el secuestro de los radicales DPPH/ABTS, su poder reductor férrico y sobre la peroxidación lipídica. El daño neuronal por isquemia/reperfusión se produjo al exponer células PC12 a KCN en un medio libre de glucosa. La Gos se añadió al medio 30 min antes de la inducción de la hipoxia química. Se determinaron la viabilidad celular, las enzimas antioxidantes SOD y CAT, y los niveles de GSH y de lipoperoxidación. La rutina (Rut), conocido antioxidante, se usó como compuesto de referencia.

Resultados: La Gos mostró una potente capacidad antioxidante evidenciada por bajos valores de CI50 y CE50 para el DPPH/ABTS/malonildialdehido y el poder reductor férrico, respectivamente. El pre-tratamiento con Gos incrementó la sobrevivencia celular frente al KCN así como las actividades enzimáticas SOD y CAT, restauró las concentraciones de GSH y redujo la lipoperoxidación. Sus efectos antioxidantes fueron superiores a los de la rutina.

Conclusiones: Los resultados muestran por primera vez el potencial neuroprotector de la Gos frente al daño celular por hipoxia, asociado probablemente a sus efectos antioxidantes.

Palabras Clave: antioxidante; gossypitrina; hipoxia; isquemia; neuroprotección; PC12.

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Citation Format: Bécquer-Viart MA, González-Yaque J, Fonseca-Fonseca LA, Núñez-Figueredo Y, Pardo Andreu GL (2018) Antioxidant and neuroprotective effects of gossypitrin, a flavonoid from Talipariti elatum, against chemical hypoxia-induced PC12 cell death. J Pharm Pharmacogn Res 6(2): 72–80.
This article has been cited by:
Felipe González A, Hernández Balmaseda I, Gutiérrez Gaitén YI, Scull Lizama R, Carmenate García LM, Pieters L, Rodeiro Guerra I, Delgado Hernández R (2019) Phytochemical study and antioxidant activity of three fractions from the stem of Caesalpinia bahamensis Lam. J Pharm Pharmacogn Res 7(1): 12–20. Website
González J, Bécquer-Viart MA, Cuéllar A, Pérez J, Monan M (2018) GC/MS analysis of gossypitrin sample with antioxidant and neuroprotective effects against chemical hypoxia-induced PC12 cell death. Annals of Advanced Agricultural Sciences 2(3): 37-44. DOI: 10.22606/as.2018.23002

© 2018 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

Nephroprotective effects of Tribulus terrestris

J Pharm Pharmacogn Res 4(4): 144-152, 2016.

Original Article | Artículo Original

Nephroprotective and hepatoprotective effects of Tribulus terrestris L. growing in Saudi Arabia

[Efectos nefroprotector y hepatoprotector de Tribulus terrestris L. que crece en Arabia Saudita]

Maged S. Abdel-Kader1,6*­­­, Abdullah Al-Qutaym­2, Abdulaziz S. Bin Saeedan­3, Abubaker M. Hamad4, Khalid M. Alkharfy­5

1Department of Pharmacognosy, College of Pharmacy; 2Undergraduate Student, College of Pharmacy; 3Department of Pharmacology, College of Pharmacy; 4Department of Medical Laboratory Sciences, College of Applied Medical Sciences; 5Department of Clinical Pharmacy, College of Pharmacy, Prince Sattam Bin Abdulaziz University, P.O. Box 173, Al-Kharj 11942, Saudi Arabia.
6Department of Pharmacognosy, College of Pharmacy, Alexandria University, Alexandria 21215, Egypt.

*E-mail: mpharm101@hotmail.com

Abstract

Context: Tribulus terrestris (Zygophyllaceae) is a popular leafy prostrate branching herb used in folk medicine as a diuretic and urinary antiseptic.

Aims: To evaluate the hepatoprotective and nephroprotective activities of the ethanolic plant extract and petroleum ether, dichloromethane and aqueous methanol fractions against CCl4 induced toxicity in adult Wistar rats.

Methods: The total 95% ethanol extract at 200 and 400 mg/kg and petroleum ether, dichloromethane and aqueous methanol at 200 mg/kg was administered p.o. for seven days followed by one dose of CCl4 (1.25 mL/kg, p.o.) at day six. Serum and tissue parameters for both liver and kidney functions were measured. Histopathological study of both tissues was conducted. Results were compared with normal rats, negative controls receiving only CCl4 and positive controls treated with silymarin (10 mg/kg, p.o.).

Results: Effect of the total 95% ethanol extract at 400 mg/kg on serum and tissue liver parameters were weak. However, protective effect on kidney was promising. The best effect was observed on the urea and creatinine levels. Both malondialdehyde and non-protein sulfhydryl groups in kidney tissues were improved to levels comparable with those obtained by silymarin.

Conclusions: The current study confirmed the positive effect of the plant on the kidney tissues and function. The activity was trapped to the dichloromethane fraction that could provide pure active compounds.

Keywords: Biochemical parameters; creatinine; ethanol extract; rats; urea.

Resumen

Contexto: Tribulus terrestris (Zygophyllaceae) es una hierba rastrera frondosa ramificada que se usa en la etnomedicina como diurético y antiséptico urinario.

Objetivos: Evaluar las actividades hepatoprotectora y nefroprotectora del extracto etanólico de la planta y las fracciones de éter de petróleo, diclorometano y metanol acuoso contra la toxicidad inducida por CCl4 en ratas Wistar adultas.

Métodos: El extracto total en etanol 95% a 200 y 400 mg/kg y las fracciones de éter de petróleo, diclorometano y metanol acuoso a 200 mg/kg fueron administradas p.o. por siete días seguidas por una dosis de CCl4 (1.25 mL/kg, p.o.) en el día seis. Se midieron los parámetros séricos y tisulares para las funciones hepáticas y renales. Se realizó el estudio histopatológico de ambos tejidos. Los resultados se compararon con ratas normales, los controles negativos recibieron sólo CCl4 y los controles positivos se trataron con silimarina (10 mg/kg, p.o.).

Resultados: El efecto del extracto total de etanol 95% (400 mg/kg) sobre los parámetros séricos y tisulares del hígado fue débil. Sin embargo, el efecto protector renal fue superior. El mejor efecto se observó en las concentraciones de urea y creatinina. Tanto los grupos sulfhidrilo no proteicos como malondialdehído en los tejidos renales mejoraron a niveles comparables con los obtenidos por la silimarina.

Conclusiones: El presente estudio confirma el efecto positivo de la planta en el tejido y la función renal. La actividad se atribuye a la fracción de diclorometano que podría proporcionar compuestos activos puros.

Palabras Clave: Creatinina; extracto etanólico; parámetros bioquímicos; ratas; urea.

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Citation Format: Abdel-Kader MS, Al-Qutaym­ A, Bin Saeedan AS­, Hamad AM, Alkharfy KM (2016) Nephroprotective and hepatoprotective effects of Tribulus terrestris L. growing in Saudi Arabia. J Pharm Pharmacogn Res 4(4): 144-152.
This article has been cited by:
Nagarathna PKM, Bhutia GT, Yadav K, Martin Lou DM (2018) A Review on evaluation of nephroprotective activity. International Journal of Research and Analytical Reviews 5(4): 126-129. Website
Azhar M (2018) Effect of herbal Unani formulation on nephrotic syndrome: A case study. Indian Journal of Traditional Knowledge 17(4):807-810. Website
Vaidya VV, Kondalkar PL, Shinde MA and Gotmare S (2018) HPTLC fingerprinting for simultaneous quantification of harmine, kaempferol, diosgenin and oleic acid in the fruit extract of Tribulus terrestris L. and its formulation. International Journal of Pharmaceutical Sciences and Research 9(7): 3066-3074. DOI: 10.13040/IJPSR.0975-8232.9(7).3066-74.
Dutt-Roy R, Kayalvizhi E, Chandrasekhar M (2017) Evaluation of the antidepressant activity of Tribulus terristris in diabetic depression in rat model. International Journal of Pharmaceutical Sciences and Research 8(12): 5392-5399. DOI: 10.13040/IJPSR.0975-8232.8(12).5392-99

© 2016 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

Ovariectomy-induced hypernociception in rats

J Pharm Pharmacogn Res 3(6): 148-161, 2015.

Original Article | Artículo Original

Ovariectomy-induced chronic abdominal hypernociception in rats: Relation with brain oxidative stress

[Hipernocicepción abdominal crónica inducida por ovariectomía en ratas y su relación con el estrés oxidativo cerebral]

Bárbara B. Garrido-Suárez1, Gabino Garrido-Garrido2, Marian Castro Labrada1, Addis Bellma Menéndez1, Roberto Menéndez Soto del Valle3, René Delgado-Hernández1

1Laboratorio de Farmacología y Toxicología, Centro de Investigación y Desarrollo de Medicamentos. Ave. 26 No. 1605 e/ Boyeros y Puentes Grandes, Nuevo Vedado, Plaza. Apdo. Postal 10600. La Habana, Cuba.
2Departamento de Ciencias Farmacéuticas, Facultad de Ciencias, Edificio Ñ3, Universidad Católica del Norte, Angamos 0610, Antofagasta, Chile.
3Departamento de Farmacología, Centro de Bioproductos Marinos (CEBIMAR). Calle Loma entre 35 y 37, Alturas del Vedado, Plaza de la Revolución, Apdo. Postal. 10400. La Habana, Cuba.
Abstract

Context: Ovarian hormone deficiency observed in menopausal women increases the production of reactive oxygen species, which could be implicated in central sensitization subjacent in chronic functional pain syndromes.

Aims: To examine the hyperalgesic state induced by ovariectomy in adult rats and its relation to some oxidative stress outcomes.

Methods: The female Wistar rats were divided into normal, sham ovariectomized (OVX) and OVX groups, which were tested for mechanical and thermal hypernociception during 6 weeks and a single acetic acid-induced test 6 weeks after surgery. Redox biomarkers determinations of superoxide dismutase (SOD) enzyme activity, glutathione (GSH) and nitrates/nitrites as an indicator of nitric oxide (NO) concentrations were determined in the brain and cerebellum of 6 animals of each group.

Results: Exclusivity OVX rats developed a robust state of mechanical hypernociception and allodynia in the abdomen, hindlimbs and proximal tail. Besides, thermal pain thresholds (hot plate) decreased. That was established 3-4 weeks after OVX and lasted for the 6 weeks of the experiment. Increases in visceral sensitivity were also observed in OVX rats. SOD enzyme activity decreased in OVX rats, which showed major deficit for this enzymatic defense under visceral inflammatory injury. However GSH concentrations were increased in brain of OVX animals that allow the balance during acute inflammation. NO concentrations were raised only in OVX rats exposure to chemical inflammatory injury.

Conclusions: OVX in rats provide a useful model, which mimics the functional pain in females that could be related with brain oxidative stress.

Keywords: Functional pain syndromes; hyperalgesia; hypernociception; ovariectomized rats; ovariectomy; pain.

Resumen

Contexto: La deficiencia de las hormonas ováricas en la mujer menopáusica incrementa la producción de especies reactivas de oxígeno que han sido implicadas en la sensibilización central subyacente en los síndromes de dolor funcional crónico.

Objetivos: Examinar el estado hiperalgésico inducido por ovariectomía en ratas adultas y su relación con algunas variables de estrés oxidativo.

Métodos: Ratas Wistar femeninas fueron divididas en grupos: normal, falsas ovariectomizadas (OVX) y OVX, para la evaluación de hipernocicepción mecánica y termal durante 6 semanas, así como la prueba de contorsiones abdominales inducidas por ácido acético a las 6 semanas tras la cirugía. La actividad de la enzima superóxido dismutasa (SOD), concentraciones de glutatión reducido (GSH) y de nitratos/nitritos como indicador de la producción de óxido nítrico (NO) fueron determinadas en cerebros y cerebelos de 6 animales de cada grupo.

Resultados: Las ratas OVX desarrollaron hiperalgesia mecánica y alodinia en abdomen, patas traseras y cola proximal, así como un descenso de sus umbrales al dolor térmico (plato caliente). Estos cambios fueron establecidos 3-4 semanas post-OVX y mantenidos durante las 6 semanas del experimento. La sensibilidad visceral también fue incrementada. La actividad de SOD disminuyó en las ratas OVX, que mostraron mayor deficiencia para la defensa enzimática ante la injuria inflamatoria visceral. El GSH fue incrementado en el cerebro de los animales OVX, lo cual podría facilitar el balance durante la inflamación aguda. El NO solo incrementó en las ratas OVX expuestas al daño químico inflamatorio.

Conclusiones: OVX en ratas provee un modelo beneficioso que mimetiza el dolor funcional en mujeres y que podría estar relacionado con el estrés oxidativo cerebral.

Palabras Clave: Hiperalgesia; hipernocicepción; dolor; ovariectomía; ratas ovariectomizadas; síndromes de dolor funcional.

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Citation Format: Bárbara B. Garrido-Suárez, Gabino Garrido-Garrido, Marian Castro Labrada, Addis Bellma Menéndez, Roberto Menéndez Soto del Valle, René Delgado-Hernández (2015) Ovariectomy-induced chronic abdominal hypernociception in rats: Relation with brain oxidative stress. J Pharm Pharmacogn Res 3(6): 148-161.

© 2015 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

Control of dental biofilm microorganisms by C. illinoinensis, Q. rubra and S. glyciphylla

J Pharm Pharmacogn Res 3(5): 118-129, 2015.

Original Article | Artículo Original

Effect of Carya illinoinensis, Quercus rubra and Smilax glyciphylla extracts, pectin, and papain on the dental biofilm microorganisms

[Efecto de extractos de Carya illinoinensis, Quercus rubra y Smilax glyciphylla, pectina y papaina sobre los microorganismos de la placa dental]

Elda P. Segura1*, Luis Méndez2, Eréndira Márquez1, Alejandra I. Vargas1, Karla M. Gregorio1, José L. Martínez1, Anna Ilyina1

1Nanobioscience Group, Chemistry School; 2Dentistry School. Coahuila Autonomous University. Blvd. V. Carranza e Ing. J.C. Valdés, CP 25280, Col. República, Saltillo, Coahuila, México.
Abstract

Context: Dental caries is an infectious disease resulting in destruction of tooth structure by acid-forming bacteria found in dental plaque and intraoral biofilms, which are made up of mixed-species microbial communities, and their uncontrolled outgrowth can lead to oral disease.

Aims: To analyze new biological materials (papain, pectin, three plant extracts and their combinations), for prevention, control, and treatment of oral bacteria and biofilm in vitro and in vivo.

Methods: Papain, citric pectin, extracts of Carya illinoinensis, Quercus rubra, and Smilax glyciphylla were applied. In vitro test was performed by means of the spectrophotometric assay and CFU evaluation after treatments application. In vivo tests were performed to evaluate the number of microorganisms presented in dental biofilm: before and 1.5 h after brushing with different treatments; after 10 days of brushing with various treatments in 10 groups of patients, signing an informed consent approved by the Institutional Ethics Committee of the Autonomous University of Coahuila.

Results: In vitro, the plant extracts inhibited the growth of Streptococcus sp. as well as a mixture of microorganisms that form dental biofilms. Papain activity was inhibited by plant extracts. In vivo, brushing of teeth with selected plant extracts reduced the number of bacteria in the dental plaques.

Conclusions: The extracts of Quercus rubra, Carya illinoinensis and Smilax glyciphylla and papain (with or without pectin) had an inhibitory effect on the dental biofilm formation. In vitro test demonstrated the bacteriostatic effect of plant extracts or their mixture.

Keywords: Aqueous extract; Carya illinoinensis; oral microorganisms control; papain; pectin; Quercus rubra; Smilax glyciphylla.

Resumen

Contexto: La caries dental es una enfermedad infecciosa; destruye la estructura dentaria por bacterias formadoras de ácido existentes en la placa dental y la biopelícula intraoral, compuestos por comunidades de distintas especies microbianas, la reproducción descontrolada de dichos microorganismos puede causar diversas enfermedades en la cavidad oral.

Objetivos: Analizar nuevos materiales biológicos (papaína, pectina, tres extractos de plantas y sus combinaciones), para la prevención, control y tratamiento de las bacterias orales y biopelícula bacteriana in vitro e in vivo.

Métodos: Se aplicaron papaína, pectina cítrica, extractos de Carya illinoinensis, Quercus rubra, y Smilax glyciphylla. La prueba in vitro se realizó por espectrofotometría y CFU después de la aplicación de tratamientos. In vivo se evalúo número de microorganismos en la biopelicula; antes, 1.5 h después del cepillado y después de 10 días de cepillado con los diferentes tratamientos en 10 grupos de pacientes, firmando consentimiento aprobado por el Comité Institucional de ética de la Universidad Autónoma de Coahuila.

Resultados: In vitro, los extractos vegetales inhibieron el crecimiento de Streptococcus sp. así como la mezcla de microorganismos que forman la biopelícula bacteriana. La actividad de la papaína fue inhibida por extractos de plantas. In vivo, el cepillado de los dientes con extractos de plantas seleccionadas redujo el número de bacterias en la placa dental.

Conclusiones: Los extractos de Quercus rubra, Carya illinoinensis y Smilax glyciphylla y papaína (con y sin pectina) tuvieron efecto inhibitorio en la formación de la biopelícula dental. Las pruebas in vitro demostraron efecto bacteriostático de los extractos de plantas o sus mezclas.

Palabras Clave: Carya illinoinensis; control de microorganismos orales; extracto acuoso; papaína; pectina; Quercus rubra: Smilax glyciphylla.

 

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Citation Format: Elda P. Segura, Luis Méndez, Eréndira Márquez, Alejandra I. Vargas, Karla M. Gregorio, José L. Martínez, Anna Ilyina (2015) Effect of Carya illinoinensis, Quercus rubra and Smilax glyciphylla extracts, pectin, and papain on the dental biofilm microorganisms. J Pharm Pharmacogn Res 3(5): 118-129.
This article has been cyted by:
Vargas Segura AI, Ilyina A, Segura Ceniceros EP, Silva Belmares Y, Méndez González L (2015) Etiology and microbiology of periodontal diseases: A review. African Journal of Microbiology Research 9(48): 2300-2306. DOI: 10.5897/AJMR2015.7609

© 2015 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

C 041: THE USE OF ENZYMES FOR POLYMER CONJUGATION

J Pharm Pharmacogn Res 2(Suppl. 1): S115, 2014

Special supplement with the abstract book of LATINFARMA 2013

Conference

C 041: THE USE OF ENZYMES FOR POLYMER CONJUGATION

Pasut G.

Department of Pharmaceutical and Pharmacological Sciences, University of Padova, F. Marzolo 5, 35131, Padova, Italy.
Abstract

Biocatalysis represents a promising area of research in organic chemistry. The specificity and selectivity of enzymes can dramatically improve the yields of synthesis, especially for those involving very complex structures. In the field of polymer conjugation, enzymes have also been considered as tools for site-specific conjugation at the level of amino acids not usually addressed with chemical methods. Different enzymatic protocols have been developed and proposed for polymer conjugation to protein. The most advanced is GlycoPEGylation that, applied to coagulation factor IX, yielded a conjugate presently in clinical trials . In this case the method is based on two enzymes to mimic O-glycosylationor N-glycosylation and consequently it has the advantage to couple PEG at the site of naturally occurring glycosylation. Although innovative, this approach involves two enzymes and therefore its feasibility at industrial scale might be limited. Another approach exploits the enzyme Sortase A to couple a polymer at the C-terminus of proteins. Also in this case there are some limitations such as the requirement of a specific C-terminal consensus amino acid sequence as substrate for the enzyme.

A promising alternative is the transglutaminase (TGase) enzymes that catalyze the transfer of a primary amine (amino donor) to the gammacarboxamide group of a glutamine (acyl donor). Interestingly, these enzymes recognize other substrate than ε-amino group of a lysine as amino donor, such as for example a PEG-NH2. My lab focused in microbial TGase (mTGase) from Streptomyces mobaraense, already approved as food additive. Beside the fact that this approach can target an amino acid that otherwise cannot be modified by chemical method another advantage of mTGase is its selectively. Among the several glutamines present in a protein only those inserted in very flexible loops can be a substrate, therefore very homogeneous conjugates can be obtained. Furthermore, mTGase preserves a good level of activity in a wide range of pH and ionic strength values and also in the presence of organic co-solvents (up to 50% v/v). We exploited this feature to develop tailor-made reaction conditions for specific proteins with the aim to stabilize the protein or to reduce the number of glutamines substrate of mTGase, thus obtaining mono-PEGylated forms.

The potential of mTGase-mediated PEGylation has been compared in our lab to another known approach of site selective conjugation: Nterminal PEGylation. The methods were applied to hGH by using a 20kDa PEG, and the results were comparable in terms of yield, and pharmacokinetic/pharmacodynamic. Relevant was the efficacy of the conjugates able to produce a weight growth with a single weekly injection in hypophysectomized rats that was comparable to that obtained with 6 weekly injections of free hGH.

The present and future development of TGase as tool for PEGylation is the development of a immobilized mTGase on resin beads, which will offer the relevant advantage of a fast removal of the enzymes and the possibility of a fast screening of several reactions conditions. Furthermore, we discovered that immobilized mTGase present an increased selectivity towards the Glu inserted in the most flexible loops.

This new era of enzymatic polymer conjugation is at the beginning and it might possess greater potentials of development and feasibility for even more advanced protein conjugates.