MOSP - Macao Scientific Publishers

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PAMAM-drug complex for delivering anticancer drug across blood-brain barrier in-vitro and in-vivo

Daming Cui, Qiwu Xu, Shixin Gu, Jinlong Shi and Xiaoming Che*

Abstract: The delivery of anticancer drugs to the brain is profoundly limited by blood-brain barrier (BBB). The purpose of this work is to develop a new carrier for doxorubicin to overcome the BBB. Polyamidoamine (PAMAM) dendrimer, a novel nanoscopic high- branching polymer, was exploited as an efficient carrier of doxorubicin. The MTT assay showed that PAMAM (generation 3) had little cytotoxicity in brain capillary endothelial cells (BCECs) . The results of fluorescence intensity assay and fluorescent microscopy showed that the cellular uptake of PAMAM/doxorubicin complex was much higher than that of free doxorubicin and exhibited concentration and time dependent manners. The action of PAMAM in increasing the cellular uptake of doxorubicin was stronger than that of verapamil, a P-glycoprotein (P-gp) inhibitor. In body distribution study, the brain uptake of doxorubicin in PAMAM/doxorubicin group increased dramatically (about 6-fold) compared to that in free doxorubicin group. These data suggest that the novel PAMAM/drug complex is a simple but efficient system, which showed great capability to cross the BBB. PAMAM dendrimer could be used as an effective carrier to deliver anticancer drugs to the brain.[...] Read More.

Keywords: PAMAM, doxorubicin, blood-brain barrier, p-glycoprotein.

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Ethnophytotherapeutic information for the treatment of high blood pressure among the people of Ilugun, Ilugun area of Ogun State, south-west Nigeria

Lawal, I. O.*, Uzokwe, N. E., Ladipo, D. O., Asinwa, I. O. and Igboanugo, A. B. I.

Abstract: Ethnophytotherapeutic information includes the contribution of indigenous knowledge using plants to provide native remedies for varieties of ailment. In African, various species of plants are used in the traditional medicine for the cure of chronic cardio-vascular diseases, where hypertension is one of them. A structured questionnaire was used to obtain enthnomedical information on the treatment of high blood pressure in the Yoruba speaking communities of Ilugun area of Ogun State. Nine species: (Ficus exasperata, Heliotropium indicum, Afromomum melegueta, Justicia schimperi, Persea americana, Talinium triangulare, Afraegle paniculatum, Newboldia laevis and Chenopodium ambrosioides) from different families were identified as being used for curing high blood pressure. Plants are documented for further research on chemical composition and active ingredients contained in these plant parts.[...] Read More.

Keywords: Ethnophytotherapy, herbal treatment, high blood pressure, Ilugun people, traditional medicines.

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Phytochemical and antimicrobial screening of crude extracts from the root, stem bark, and leaves of Terminalia glaucescens

Adebayo, E. A. and Ishola, O. R.

Abstract: The root, stem-bark and leaves of Terminalia glaucescens were investigated for activity against some pathogenic organisms. Phytochemical screening revealed the presence of alkaloids, tannins, saponins, steroids, flavonoids, anthraquinones and phlobatannins (mostly in root and stem -bark). The results of in-vitro antimicrobial screening of the crude methanol extract exhibited a wide range of activity on Salmonella typhi, Escherichia coli, Staphylococcus aureus, Proteus mirabilis and Candida albicans. The crude leaf extracts inhibited the growth of E. coli, S. aureus, S. typhi and C. albicans at a concentration of 50, 80, 40 and 60 mg/ml respectively, while the stem-bark extract had minimum inhibitory concentration (MIC) of 40 mg/ml on K. pneumoniae, S. aureus, S. typhi and 30 mg/ml on C. albicans. The extract from the root inhibited the growth of E. coli at a concentration of 10 mg/ml while K. pneumoniae, P. mirabilis and C. albicans were inhibited at a concentration of 60 mg/ml. The findings indicated that the extracts from T. glaucescens, contained bioactive components that have antimicrobial properties. Key word: Terminalia glaucescens, phytochemical, antimicrobial agents, crude extract, minimum inhibitory concentration.[...] Read More.

Keywords: Terminalia glaucescens, phytochemical, antimicrobial agents, crude extract, minimum inhibitory concentration.

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Gentamicin and erythromycin modify post prandial glucose excursion in New Zealand rabbits

Bello, Shaibu Oricha* and Chika, Aminu

Abstract: The influence of gentamicin and erythromycin on glucose excursion after oral glucose loads was evaluated in twelve New Zealand rabbits, weighting between 1278 and 1861 g. The rabbits were randomized into three equal groups and were given either 5 mg/kg of Gentamicin i.m., 50 mg/kg of Erythromycin per oral or 0.9% Saline. One hour later, all the rabbits were given 2.5 g/kg of glucose per oral in 5 mls of 0.9% saline. Blood glucose levels were determined just before oral glucose loads, then every 1 h for 4 h, using commercial glucometer. Gentamicin pre-treatment significantly increased the peak glucose level (1 h) and significantly reduced the half -life of the rise in glucose level compared to controls. On the other hand, erythromycin pre-treatment caused significant increase in the glucose levels at 3 and 4 h while the peak glucose level (1 h) was not significantly different. The perturbation of glycemic response to glucose load revealed by both drugs may be clinically important in persons undergoing screening for glycemia and patients under care.[...] Read More.

Keywords: Gentamicin, erythromycin, glucose, insulin, rabbits, kinetics, prandial.

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The protective effect of quercetin, green tea or malt extracts against experimentally-induced lung fibrosis in rats

Nesrine S. El-Sayed* and Sherine M. Rizk

Abstract: The possible protective potentials of quercetin (50 mg/kg, p.o.), green tea extract (1 mg/kg, p.o.) malt extract (625 mg/kg, p.o.) and deprenyl (10 mg/kg, i.p.) against paraquat (PQ) -induced lung injury in rats were examined. PQ was administered twice a week (20 mg/kg, i.p.) with or without daily pretreatment with any of the chosen agents for 3 successive weeks. Changes in the enzymatic activities of myeloperoxidase (MPO), superoxide dismutase (SOD) and lactate dehydrogenase (LDH) as well as reduced glutathione (GSH), protein thiols (Pr-SHs) and nitric oxide (NO) contents of the lungs were determined. In addition, estimation of lung content of thiobarbituric acid reactive substances (TBARS) measured as malondialdehyde. Moreover, histopathological examination of the lung tissue was performed. On the biochemical level, PQ provoked remarkable lung damage noted by elevation of neutrophils MPO activity accompanied by decreased activities of cytosolic SOD and LDH, depletion of GSH and Pr-SHs contents as well as increased production of NO and TBARS. Furthermore, histopathological examination revealed marked edema, subpleural hemorrhage, acute inflammation and lymphocytic infiltration. Treatment significantly protected against most of PQ-induced lung biochemical and histopathological changes. It could be concluded that quercetin, green tea, malt extract and deprenyl offered remarkable protection against PQ-induced lung injury.[...] Read More.

Keywords: Paraquat, quercetin, green tea, malt, deprenyl, lung, rats.

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Saffron (Crocus sativus) increases gastric acid and pepsin secretions in rats: Role of nitric oxide (NO)

Fatemeh Nabavizadeh*, Ehsan Salimi, Zahra Sadroleslami, Seyed Morteza Karimian and Jalal Vahedian

Abstract: This study was designed to investigate the effects of saffron extract on gastric acid and pepsin secretion. In this study wistar rats (n = 8) were divided into 3 groups, N-L-Nitro-L- arginine methyl ester (LNAME) + saffron and control groups. In the saffron group 100 mg/kg saffron extract was administered orally for 5 days. In the LNAME + saffron group, 40 mg/kg LNAME was injected intraperitoneally 1 h before using saffron extract. In the control group normal saline was given orally for 5 days before the experiment. Under general anesthesia with 50 mg/kg intraperitoneal (i.p) sodium thiopental, laparotomy was done and a cannula was inserted into the duodenum. Gastric content was collected by wash out technique. Basal and stimulated acid and pepsin secretions were measured using titration and the Anson method, respectively. In this study, pentagastrin (25 µg/kg, i.p) was used as a stimulator. In the saffron group, basal and stimulated acid and pepsin secretions were significantly more than control group (p = 0.006, p = 0.008). But there were no significant differences in basal and stimulated acid and pepsin secretions in the LNAME + saffron and control groups. Saffron extract increased basal and stimulated gastric secretions. It seems that the saffron extract increases them via NO increment.[...] Read More.

Keywords: Saffron, gastric acid secretion, pepsin secretion, NO.

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Anti-diabetic properties of Tinospora cordifolia stem extracts on streptozotocin- induced diabetic rats

M. Rajalakshmi, J. Eliza, Cecilia Edel Priya, Nirmala A and P. Daisy*

Abstract: The oral administration of various extracts (hexane, ethyl acetate and methanol) of Tinospora cordifolia stem (TCS) were found to have potent antidiabetic activity that reduces blood sugar level in streptozotocin-(STZ) induced diabetic rats. In this study, the chronic (100 days) antihyperglycemic effect of the extracts at a dose of 250 mg/kg b.w.p.d of TCS were investigated. Insulin was used as a reference drug at a dose of 3 I.U/kg.b.w.p.d. Fasting blood glucose, glycosylated hemoglobin (HBA1C), serum insulin, C- peptide and liver enzymes levels were evaluated in normal, diabetic and treated rats. Supplementation of methanol extract significantly reduces the fasting blood glucose level when compared to other 2 extracts. Moreover this supplementation significantly decreases the glycosylated hemoglobin level as compare to diabetic control (p < 0.001), reduced glucokinase and increased glucose-6- phoaphatase activity were reversed significantly by the treatment of TCS methanol extract in respect to diabetic group. In the TCS treated groups, the insulin and C-peptide levels were improved which shows the regeneration of -cell which secretes insulin, histopathological studies of pancreas of TCS methanol extract treated groups substantiate the regenerating capacity of extract.[...] Read More.

Keywords: Tinospora cordifolia, streptozotocin, hypoglycemic, glycosylated hemoglobin (HBA1C), serum insulin, C-peptide, glucokinase and glucose-6-phoaphatase.

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Potential antioxidant phenolic metabolites from doum palm leaves

Omayma A. Eldahshan, Nahla A. Ayoub*, Abdel-Nasser B. Singab and Mohamed M. Al-Azizi

Abstract: The antioxidant activity of the aqueous ethanolic extract of doum leaves, Hyphaene thebaica L. (Palmae) was studied. Data obtained showed that the extract can inhibit reactive oxygen species attack on salicylic acid (IC50 = 1602 µg/ml) in a dose dependant manner using xanthine/hypoxanthine oxidase assay. Four major flavonoidal compounds were identified by LC/SEI as; Quercetin glucoside, Kaempferol rhamnoglucoside and Dimethyoxyquercetin rhamnoglucoside. While, further in-depth phytochemical investigation of this extract lead to the isolation and identification of fourteen compounds; their structures were elucidated based upon the interpretation of their spectral data (UV, 1H, 13C NMR and ESI/MS) as; 8-C- -D-glucopyranosyl-5, 7, 4`-trihydroxyflavone (vitexin) 1, 6-C- -D-glucopyranosyl-5, 7, 4`-trihydroxyflavone (iso-vitexin) 2, quercetin 3-O- - 4C1-D-glucopyranoside 3, gallic acid 4, quercetin 7-O- -4C1-D-glucoside 5, luteolin 7-O- -4C1-D-glucoside 6, tricin 5 O- -4C1-D-glucoside 7, 7, 3` dimethoxy quercetin 3-O-[6''-O- -L-rhamnopyranosyl]- -D-gluco-pyranoside (Rhamnazin 3-O-rutinoside) 8 kaempferol-3-O-[6''-O- -L-rhamnopyranosyl]- -D-glucopyranoside (nicotiflorin) 9, apigenin 10, luteolin 11, tricin 12, quercetin 13 and kaempferol 14.[...] Read More.

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Pilot study comparing technologies to test for substandard drugs in field settings

Roger Bate, *, Richard Tren, Kimberly Hess, Lorraine Mooney and Karen Porter

Abstract: Researchers procured a range of antimalarial, antibiotic and antimycobacterial drugs from cities in six countries: Ghana, India, Kenya, Nigeria, Tanzania, and Uganda. Semi-quantitative thin-layer chromato-graphy (TLC) and disintegration tests, Raman spectrometry, and near-infrared (NIR) spectrometry were used to measure the concentration of active ingredients and excipients (spectrometry only) to deter-mine whether the tested samples were of good quality. Overall, 15% of tested samples failed TLC, 13% of tested samples failed disintegration tests, 41% of tested samples failed NIR spectrometry, and 47% of tested samples failed Raman spectrometry. The drug testing technologies were qualitatively compared in terms of time, cost, and reliability for identifying substandard drugs in the field. NIR and Raman spectrometry compared favorably to TLC in most respects except cost. If the indirect costs of TLC— including requirements for a climate controlled location and trained laboratory staff—are considered, the cost advantage of TLC may disappear in developing countries.[...] Read More.

Keywords: Raman and near-infrared spectrometry, thin-layer chromatography, counterfeit and substandard drug production, regulation of drug quality.

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The modulatory effect of Cochlospermum tinctorium a rich aqueous root extract on liver damage induced by carbon tetrachloride in rats

E. U. Etuk*, B. M. Agaie, M. J. Ladan and I. Garba

Abstract: The aqueous root extract of Cochlospermum tinctorium (CTR) was investigated for its phytochemical composition; acute oral toxicity and hepatoprotective effect on carbon tetrachloride (CCl4) induced liver damage in rats. Phytochemical screening indicates the presence of alkaloids, tannins, cardiac glycosides, saponins, flavonoids, triterpenes, cyanogenic glycosides and volatile oils while steroids and anthraquinones were absent. Administration of 5000 mg/kg (body weight) of the extract orally did not produce any death in the rats within the observable period. The extract at 100 – 300 mg/kg (body weight) significantly and dose dependently reduced the levels of Alanine aminotransferase (ALT), Aspartate aminotransferase (AST) and Alkaline phosphatase (ALP) enzymes levels in the CCl4 -treated rats. The values of serum albumin, serum total protein and reduced glutathione in the extract treated groups of rats remained comparatively higher than its values in the CCl4 - treated group. The pretreatment of the rats with the extract produced a significant (P < 0.05) reduction in blood clotting time. The histopathological findings were in support of the biochemical changes recorded during the study. These results suggest that aqueous root extract of CTR possess hepatoprotective effect against CCl4- induced liver damage in rats and the extract at 5000 mg/kg body weight appeared to be safe when administered orally.[...] Read More.

Keywords: Cochlospermum tinctorium, carbon tetrachloride, transaminases, hepatoprotective.

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