Anticarcinogenic activity of methanol extract of Melastoma malabathricum leaves is attributed to the presence of phenolics compounds and the activation of endogenous antioxidant system / Actividad anticancerígena del extracto metanólico de hojas de Melastoma malabathricum atribuida a la presencia de compuestos fenólicos y a la activación del sistema antioxidante endógeno

Melastoma malabathricum (M. malabathricum) extracts have been reported to exert various pharmacological activities including antioxidants, anti-inflammatory and antiproliferative activities. The objective of the present study was to determine the anticarcinogenic activity of its methanol extract (MEMM) against the azoxymethane (AOM)-induced early colon carcinogenesis in rats. Rats were randomly assigned to five groups (n=6) namely normal control, negative control, and treatment (50, 250 or 500 mg/kg of MEMM) groups. Colon tissues were harvested for histopathological analysis and endogenous antioxidant system determination. MEMM was also subjected to HPLC analysis. Findings showed that MEMM significantly (p<0.05) reversed the AOM-induced carcinogenicity by: i) reducing the formation of aberrant crypt foci (ACF) in colon tissues, and; ii) enhancing the endogenous antioxidant activity (catalase, superoxide dismutase and glutathione peroxidase). Moreover, various phenolics has been identified in MEMM. In conclusion, MEMM exerts the in vivo anticarcinogenic activity via the activation of endogenous antioxidant system and synergistic action of phenolics.

Se ha informado que los extractos de Melastoma malabathricum (M. malabathricum) ejercen diversas actividades farmacológicas, incluidas actividades antioxidantes, antiinflamatorias y antiproliferativas. El objetivo del presente estudio fue determinar la actividad anticancerígena de su extracto de metanol (MEMM) contra la carcinogénesis de colon temprana inducida por azoximetano (AOM) en ratas. Las ratas se asignaron al azar a cinco grupos (n=6), a saber, los grupos de control normal, control negativo y tratamiento (50, 250 o 500 mg/kg de MEMM). Tejidos de colon fueron recolectados para análisis histopatológico y determinación del sistema antioxidante endógeno. MEMM también se sometió a análisis de HPLC. Los hallazgos mostraron que MEMM invirtió significativamente (p<0.05) la carcinogenicidad inducida por AOM al: i) reducir la formación de focos de criptas aberrantes (ACF) en los tejidos del colon, y; ii) potenciar la actividad antioxidante endógena (catalasa, superóxido dismutasa y glutatión peroxidasa). Además, se han identificado varios fenólicos en MEMM. En conclusión, MEMM ejerce la actividad anticancerígena in vivo mediante la activación del sistema antioxidante endógeno y la acción sinérgica de los fenólicos.

Dicranopteris linearis: a potential medicinal plant with anticancer properties / Dicranopteris linearis: una planta medicinal potencial con propiedades anticancerígenas

Several investigations have demonstrated Dicranopteris linearis (Burm.f.) Underw. (Gleicheniaceae) plant extracts possess numerous health-promoting properties. This review is aimed to summarize and highlight the potential possess by D. linearisto be developed into future pharmacological entity especially as anticancer agent. This study used several electronic search engines to compile and integrate a number of scientific publications related with D. linearis. Scientifically, D. linearishas been reported to have antinociceptive, anti-inflammatory, antipyretic, chemopreventive and antioxidant properties which can be linked to its potential to treat various kinds of ailments including inflammatory-related diseases and cancer. A number of scientific evidences related with anticancer studies suggested the ability of D. linearis-based phytochemicals to act as potent anticancer lead compounds. In conclusion, D. linearis has the potential to be developed into potent anticancer agent as depicted by a number of isolated phytochemicals which can work synergistically to contribute to its anticancer properties.

Varias investigaciones han demostrado que los extractos de la planta Dicranopteris linearis (Burm.f.) Underw. (Gleicheniaceae) poseen numerosas propiedades promotoras de la salud. El objetivo de esta revisión es resumir y resaltar el potencial que posee D. linearispara convertirse en una entidad farmacológica futura, especialmente como agente anticancerígeno. Este estudio utilizó varios motores de búsqueda electrónicos para compilar e integrar una serie de publicaciones científicas relacionadas con D. linearis. Científicamente, se ha informado que D. linearis tiene propiedades antinociceptivas, antiinflamatorias, antipiréticas, quimiopreventivas y antioxidantes que pueden estar vinculadas a su potencial para tratar varios tipos de dolencias, incluidas las enfermedades asociadas a inflamación y el cáncer. Una serie de evidencias científicas relacionadas con los estudios anticancerosos sugirieron la capacidad de los fitoquímicos basados en D. linearis para actuar como potentes compuestos anticancerígenos. En conclusión, D. linearis tiene el potencial de convertirse en una fuente de potentes agentes anticancerígeno, como se describe en una serie de fitoquímicos aislados que pueden actuar de forma sinérgica para contribuir a sus propiedades anticancerígenas.

In vitro characterization and in vivo performance of mefenamic acid-sodium diethyldithiocarbamate based liposomes

Mefenamic acid (MFA) is a hydrophobic drug with low dissolution rate. This study aimed to develop stable and reproducible aqueous formulations of MFA using liposomes as drug carriers. The drug entrapment, particles size and drug release profiles, and stability and reproducibility of the liposomes were determined. In addition, the maximum tolerated dose (MTD) was determined in rats via the oral and intraperitoneal routes of administration. Also, the anti-inflammatory efficacy of these liposomes was evaluated using carrageenan-induced paw edema model in rats. MFA-DDC based liposomes demonstrated a drug entrapment efficacy of 93.6%, particles size of 170.9 nm, and polydispersity index of 0.24 which were not statistically affected when stored in room and refrigerated temperatures for at least 4 weeks. The MTD of the intraperitoneally administrated MFA-loaded liposomes was 20 mg MFA/kg, whereas for those of oral administrations, it was up to 80 mg MFA/kg. Intraperitoneal dose (80 mg MFA/kg) of MFA-DDC liposomes induced extrapyramidal symptoms associated with significant elevation in serum potassium and muscle enzymes. Moreover, significant inhibition of paw edema was demonstrated by the oral and intraperitoneal routes. These findings suggest that MFA-DDC based liposomes are an effective formulation of MFA and recommend the use of bioequivalence assessments with commercial formulations.

Antinociceptive effect of semi-purified petroleum ether partition of Muntingia calabura leaves

ABSTRACT Muntingia calabura L., Muntingiaceae, is a medicinal plant for various pain-related diseases. The aims of the present study were to determine the antinociceptive profile and to elucidate the possible mechanisms of antinociception of petroleum ether partition obtained from crude methanol extract of M. calabura leaves using various animal models. The antinociceptive profile of petroleum ether fraction (given oral; 100, 250 and 500 mg/kg) was established using the in vivo chemicals (acetic acid-induced abdominal constriction and formalin-induced paw licking test) and thermal (hot plate test) models of nociception. The role of glutamate, TRPV1 receptor, bradykinin, protein kinase C, potassium channels, and various opioid and non-opioid receptors in modulating the partition's antinociceptive activity was also determined. The results obtained demonstrated that petroleum ether partition exerted significant (p < 0.05) antinociception in all the chemicals-, thermal-, capsaicin-, glutamate-, bradykinin, and phorbol 12-myristate 13-acetate (PMA)-induced nociception models. The antinociceptive activity was reversed following pretreatment with opioid antagonists (i.e. naloxone, β-funaltrexamine, naltrindole and nor-binaltorphimine), and the non-opioid receptor antagonists (i.e. pindolol (a β-adrenoceptor), haloperidol (a non-selective dopaminergic), atropine (a non-selective cholinergic receptor), caffeine (a non-selective adenosinergic receptor), and yohimbine (an α2-noradrenergic)). In addition, pretreatment with L-arginine (a nitric oxide (NO) donor), NG-nitro-L-arginine methyl esters (L-NAME; an inhibitor of NO synthase (NOS)), methylene blue (MB; an inhibitor of cyclic-guanosine monophosphate (cGMP) pathway), or their combination failed to inhibit petroleum ether partition's antinociception. In conclusion, petroleum ether partition exerts antinociceptive activity at the peripheral and central levels via the modulation of, partly, the opioid (i.e. µ, κ and δ) and several non-opioids (i.e. β-adrenergic, dopaminergic, cholinergic, adenosinergic, and α2-noradrenergic) receptors, glutamatergic, TRPV1 receptors, PKC and K+ channels systems, but not L-arg/NO/cGMP pathway.