Band 23, Heft 4

Background: Yoyo Bitters is an indigenous polyherbal preparation widely consumed in Nigeria. In spite of its wide consumption there is little scientific data on the safety/toxicity profile of Yoyo Bitters. This study determined the biochemical effect of daily administration of Yoyo Bitters on rat serum, kidney and liver. Methods: A total of 20 Wistar rats, of average weight between 175 and 200 g, were randomly distributed into four groups of five rats each. Group A served as controls and received distilled water. Groups B, C and D were given Yoyo Bitters at various dosages. Treatments were orally administered for 28 days. Results: Yoyo Bitters caused lipid peroxidation as reflected in serum and liver malondialdehyde (MDA) levels which were significantly (p<0.05) elevated in a dose-dependent manner. In groups treated with 1206.5 mg and 804.3 mg/kg dosages of Yoyo Bitters, serum superoxide dismutase (SOD) levels were also significantly (p<0.05) increased. By contrast, Yoyo Bitters caused a dose-dependent reduction in reduced glutathione (GSH) levels. It is not clear if free radicals or lipid peroxidation caused changes in SOD and GSH levels. However, Yoyo Bitters may have enhanced free radical generation and ensuing lipid peroxidation leading to increased SOD and subsequent dose-dependent depletion of GSH levels. Conclusions: In light of this, caution and adherence to dosage prescription is strongly advised. This study is a contribution to scientific knowledge on the safety/toxicity profile of Yoyo Bitters among the growing list of Nigerian herbal remedies.

Background: Many plant-derived products exhibit potent chemopreventive activity against animal tumor models as well as rodent and human cancer cell lines. They have low side effects and toxicity and presumably modulate the factors that are critical for cell proliferation, differentiation, senescence and apoptosis. The present study investigates the effects of some medicinal plant extracts from generally recognized as safe plants that may be useful in the prevention and treatment of cancer. Methods: Clonogenic assays using logarithmically-growing cells were performed to test the effect. The cytotoxic effects of Curcuma longa and Zingiber officinale were studied using sulforhodamine B assay, tetrazolium dye assay, colony morphology and microscopic analysis. Results: Out of the 13 lyophilized plant-derived extracts evaluated for growth-inhibitory effects on the PC-3M prostate cancer cell line, two extracts derived from C. longa and Z. officinale showed significant inhibitory effects on colony-forming ability. The individual and augmentative effects of these two extracts were tested for their narrow range effective lower concentration on PC-3M in clonogenic assays. At relatively lower concentrations, C. longa showed significant inhibition of colony formation in clonogenic assays; whereas at same concentrations Z. officinale showed only moderate inhibitory effects. However, when both the agents were tested together at the same concentrations, the combined effects were much more significant than their individual ones. On normal prostate epithelial cells both C. longa and Z. officinale had similar effects but at a lower magnitude. These observations were confirmed by several cytotoxicity assays involving the morphological appearance of the colonies, microscopic observations, per cent inhibition in comparison to control by sulforhodamine B and tetrazolium dye assay. Conclusions: From these observations, it was concluded that the combined effects of C. longa and Z. officinale are much greater than their individual effects, suggesting the role of multiple components and their synergistic mode of actions to elicit stronger beneficial effects.

Background: Purine metabolism specificity, namely the high level of uric acid in the blood, is considered to be significant in the appearance of intellectually-developed primates, as well as in later periods of human development, for personal activity and achievements and even for the formation of genius. Nowadays hyperuricemia is mostly associated with the pathogenesis of hypertension and metabolic syndrome. Its influence on the central nervous system is predominantly set aside. Methods: The behavioral reactions of random-bred mice with uricase inhibition due to potassium oxonate or xanthine oxidase suppression with allopurinol for three weeks were investigated. Results: Potassium oxonate reduced signs of anxiety in the elevated plus maze. A positive correlation appeared between latency to enter a dark arm and uricemia, so anxiety reduction can be associated with uric acid metabolism changes. Allopurinol reduced anxiety that was not related to the metabolic changes of uric acid, so the involvement of changes in uric acid precursor concentrations cannot be excluded. Potassium oxonate but not allopurinol reduced immobility in a tail suspension test. There was a tendency to increase the duration of swimming to exhaustion against the potassium oxonate background. At the same time, potassium oxonate reduced research activity in the combined open field test and increased the vegetative maintenance of behavioral responses. Allopurinol did not change the results of this test. Conclusions: A reduction in anxiety and depression level and a tendency to augment physical performance against the potassium oxonate background partly conform to the beneficial evolutionary role of hyperuricemia.

Background: Aframomum species are widely used as a food supplement and remedy in folklore medicine for the management of several diseases. This study was designed to investigate the acetylcholinesterase inhibitory activity and antioxidant properties of phenolic-rich extracts from two Aframomum species: Aframomum danielli (Hook F.) K. Schum (Zingiberaceae) and Aframomum melegueta (Roscoe) K. Schum (Zingiberaceae) seeds. Methods: Acetylcholinesterase inhibitory activity and antioxidant properties [inhibition of quinolinic acid (QA)-induced lipid peroxidation in rat brain, reducing properties, 2,2-azinobis (3-ethylbenzo-thiazoline-6-sulfonate) (ABTS) and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging abilities] using in vitro models were evaluated. Phenolic composition of the seed extracts using reversed phase high performance chromatography (RP-HPLC) and gas chromatography coupled with flame ionization detector (GC-FID) were also assessed. Results: Both extracts exhibited acetylcholinesterase inhibitory activity in a dose-dependent manner (125–1000 μg/mL); however, A. melegueta extract (IC 50 =373.33 μg/mL) had a significantly higher (p<0.05) acetylcholinesterase inhibitory activity than A. danielli extract (IC 50 =417.10 μg/mL). Furthermore, both extracts significantly decreased QA-elevated brain malondialdehyde (MDA) contents, reduced Fe 3+ to Fe 2+ and scavenged DPPH and ABTS radicals. Phenolic characterization of the seeds by RP-HPLC at 280 nm showed abundance of quercetin and kaempferol in A. melegueta and chlorogenic acid in A. danielli , whereas GC-FID revealed that p-hydroxybenzoic acid was abundant in both seeds. Conclusions: Inhibitory effect of these extracts on acetylcholinesterase activity and their antioxidant property could be attributed to the combined effect of phenolic and non-phenolic constituents of the seeds. These effects could be part of the possible biochemical mechanism by which these seeds elicit their protection against oxidative stress in brain; however, A. melegueta showed the more promising potential.

Background: Methotrexate (MTX) is a folic acid antagonist widely used as a cytotoxic chemotherapeutic agent for many malignancies. Its use is limited due to wide-ranging toxicities. MTX generates reactive oxygen species. Here, we investigated the efficacy of vitamin E supplementation on MTX-induced alterations in vitro. Methods: Rat heart mitochondria were isolated and used to assess the extent of swelling, lipid peroxidation and alterations in mitochondrial-specific enzyme activities caused by the addition of 80 μM MTX in the presence and absence of 1.2 μM vitamin E. Control for both groups was maintained. Result: MTX substantially affects mitochondrial function by increasing lipid peroxidation and mitochondrial swelling. Significant losses in the activities of the tricarboxylic acid cycle enzymes, complex I, II and IV, and an increase in the activity of calcium ATPase were observed in MTX-treated rat mitochondria. Enrichment of the media with vitamin E led to a reduction in swelling and restoration of enzyme activities. Conclusions: The present study suggests that vitamin E plays a vital role in suppressing MTX-induced mitochondrial toxicity, and affords protection either by reversing the decline of antioxidants or by direct scavenging of free radicals.

Background: The aim of this study was to compare the effect of adrenaline on blood glucose concentration in patients with diabetes undergoing tooth extraction under local anesthesia and also to find out whether blood glucose concentration differs if local anesthetics are injected in clinical doses with and without adrenaline. Methods: Patients included had a tooth in need of extraction, were in the 25–55 years age group, had a random blood sugar level ≤140 mg/dL and were on oral antidiabetic drugs. The 25 patients in Group A were injected with 2 mL of lignocaine hydrochloride without adrenaline (xylocaine 2%) and the other 25 patients (Group B) were injected with 2 mL lignocaine hydrochloride along with adrenaline 1:80,000. Serial blood glucose estimations were made at regular intervals of 10 min before local anesthesia and subsequently 10 and 20 min after local anesthesia. Results: A statistically significant difference of the mean blood glucose concentration was noticed at three different time intervals between the two groups. Conclusions: Dental local anesthetic solutions containing adrenaline may safely be used in patients with diabetes who had taken their hypoglycemic medications preoperatively.

Background: Many drugs are available for the treatment of diabetes mellitus and are sometimes prescribed in combination. Irrational use of drugs is increasing expenditure and strain on health budgets. The aim of this study was to determine patient demographic characteristics, analyze prescription patterns of antidiabetic drugs, distribution of complications of diabetes, distribution of co-existing illnesses, distribution of common symptoms of diabetes and distribution of adverse drug reactions. Methods: A study was carried out for 11 months in diabetic inpatients in the General Medicine Department. Data of 200 patients were collected and evaluated. Results: The pattern of drug prescription in diabetes shows that insulin (80.5%) was most frequently prescribed followed by biguanides (23%), sulfonylureas (22.5%), thiazolidinediones (11%), dipeptidyl peptidase-IV (DPP-4) inhibitors (9.5%) and meglitinides (5.5%). The percentage of patients on diet control therapy was found to be 3%. Combination therapy was prescribed to 26.5% and monotherapy to 65% of patients; 47.5% of these patients were male and 52.5% were female. The most common co-existing illness was found to be hypertension (53.5%). In addition, 67% of patients had irregular blood sugar monitoring and the remaining 33% had regular (either 4 or 6 hourly) monitoring. Conclusions: It is concluded that the prescribing trend is moving away from monotherapy with insulin and sulfonylureas and towards combination therapies. There is also a significant increase in prescriptions of newer oral antidiabetic drugs, such as DPP-4 inhibitors and insulin analogs. Most inpatients had their blood glucose checked irregularly and haphazardly by ward staff. This study strongly highlights the need for patient education or counseling on use of antidiabetic and concomitant drugs, monitoring of blood glucose and glycosylated hemoglobin (HbA 1c ) levels, diet control and correction of diabetic complications.

Background: Chemotherapy which is one of the major methods for controlling trypanosomal infections is beset with several challenges including unwanted toxicity and limited efficacy. These factors and others underscore research efforts aimed at finding safer and more effective therapeutic agents for trypanosomiasis. Homidium chloride and diminazene aceturate are registered drugs for the treatment of animal trypanosomiasis. Methods: Study investigated and compared, in an experimental Trypanosoma infection, the effects of two trypanocides on the pathology of tissues and some biochemical indices in rats. Results: Data revealed that the levels of alkaline phosphatase, alanine transaminase and aspartate transaminase in infected positive animals were significantly (p<0.05) elevated relative to uninfected negative controls but showed no significant difference when compared with the trypanocide-treatment groups. The histopathological presentations in the infected and treatment groups are a demonstration of the inimical cellular alterations associated with Trypanosoma brucei brucei infection. Conclusions: The inimical alterations to biochemical and morphological parameters observed in the infected as well as the treatment groups is an implication suggesting shortcomings of the investigated trypanocides to alleviate pathology associated with Trypanosoma brucei brucei infection. We present evidence that further supports the urgent need for the development of safer and more effective trypanocides.