Volume 28, Issue 1

The global prevalence of obesity has increased considerably in the last two decades. Obesity is caused by an imbalance between energy intake (EI) and energy expenditure (EE), and thus negative energy balance is required to bring about weight loss, which can be achieved by either decreasing EI or increasing EE. Caffeine has been found to influence the energy balance by increasing EE and decreasing EI, therefore, it can potentially be useful as a body weight regulator. Caffeine improves weight maintenance through thermogenesis, fat oxidation, and EI. The sympathetic nervous system is involved in the regulation of energy balance and lipolysis (breakdown of lipids to glycerol and free fatty acids) and the sympathetic innervation of white adipose tissue may play an important role in the regulation of total body fat. This article reviews the current knowledge on the thermogenic properties of caffeine, and its effects on appetite and EI in relation to energy balance and body weight regulation.

Background: Despite the acclaimed beneficial effects of Telfaria occidentalis (TO), it is yet to be established that its aqueous extract is safe in the condition of renal impairment. Thus, the study investigated the effects of TO aqueous leaves extract on gentamycin-induced renal damage. Methods: The animals were distributed into five groups. Group A (control) was placed on standard rat feed. Groups B and C received 500 mg/kg and 80 mg/kg of TO and gentamicin for 21 days, respectively. Group D received 500 mg/kg of TO 14 days before 7 days administration of 80 mg/kg of gentamycin. Group E received 80 mg/kg of gentamicin for 14 days before 7 days administration of 500 mg/kg TO. Group F received 500 mg/kg of TO and 80mg/kg of gentamycin concurrently for 21 days. Biochemical and histological examinations were analysed by standard methods. Results: The administration of TO for 7 days after 14 days of gentamycin injection and its concomitant administration with gentamicin for 21 days caused significant reduction (p<0.05) on the relative kidney weight, creatinine and uric acid levels compared to groups C and D. There was a significant decrease (p<0.05) in the mean serum potassium level in group C compared to groups A, B, D, and F. The histological reports showed that the combination of the extract and gentamycin (group F) seems to ameliorate the deleterious effect observed when gentamycin was administered alone. Conclusions: The administration of the extract together with and after the administration of gentamycin reverses renal damage caused by gentamycin.

Background: Ashanti pepper ( Piper guineense Schumach et Thonn) seed is well known in folkloric medicine in the management of type 2 diabetes (T2DM) with little or no scientific documentation for its action. This study investigated the effect of Ashanti pepper seed on some enzymes relevant to carbohydrate hydrolysis, blood regulation and the cholinergic system, as well as the blood glucose level, lipid profile, antioxidant parameters, and hepatic and renal function markers in T2DM rats. Methods: T2DM was induced by feeding rats with high-fat diet (HFD) for 14 days followed by a single intraperitoneal dose of 35 mg/kg body weight of streptozotocin (STZ). Three days after STZ induction, diabetic rats were placed on a dietary regimen containing 2%–4% Ashanti pepper. Results: Reduced blood glucose level with decreased α-amylase, α-glucosidase and angiotensin I converting enzyme (ACE) activities were observed in Ashanti pepper seed and acarbose-treated rat groups when compared to that of the diabetic control rat group. Furthermore, the results revealed that inclusion of 2%–4% Ashanti pepper seed in diabetic rat fed group diets may ameliorate the lipid profile, antioxidant status, and hepatic and renal function in T2DM rats as much as in the acarbose-treated groups. In addition, a chromatographic profile of the seed revealed the presence of quercitrin (116.51 mg/g), capsaicin (113.94 mg/g), dihydrocapsaicin (88.29 mg/g) and isoquercitrin (74.89 mg/g). Conclusions: The results from this study clearly suggest that Ashanti pepper could serve as a promising source of phenolic compounds with great alternative therapeutic potentials in the management of T2DM.

Background: Oxidative stress plays a key role in the pathogenesis of epilepsy and contributes in underlying epileptogenesis process. Anticonvulsant drugs targeting the oxidative stress domain of epileptogenesis may provide better control of seizure. The present study was carried out to investigate the effect of clinically used anti-epileptic drugs (AEDs) on the course of pentylenetetrazole (PTZ)-induced kindling and oxidative stress markers in mice. Methods: Six mechanistically heterogeneous anticonvulsants: phenobarbital, phenytoin, levetiracetam, pregabalin, topiramate, and felbamate were selected and their redox profiles were determined. Diazepam was used as a drug control for comparison. Kindling was induced by repeated injections of a sub-convulsive dose of PTZ (50 mg/kg, s.c.) on alternate days until seizure score 5 was evoked in the control kindled group. Anticonvulsants were administered daily. Following PTZ kindling, oxidative stress biomarkers were assessed in homogenized whole brain samples and estimated for the levels of nitric oxide, peroxide, malondialdehyde, protein carbonyl, reduced glutathione, and activities of nitric oxide synthase and superoxide dismutase. Results: Biochemical analysis revealed a significant increase in the levels of reactive oxygen species with a parallel decrease in endogenous anti-oxidants in PTZ-kindled control animals. Daily treatment with levetiracetam and felbamate significantly decreased the PTZ-induced seizure score as well as the levels of nitric oxide (p<0.001), nitric oxide synthase activity (p<0.05), peroxide levels (p<0.05), and malondialdehyde (p<0.05). Levetiracetam and felbamate significantly decreased lipid and protein peroxidation whereas topiramate was found to reduce lipid peroxidation only. Conclusions: An AED that produces anticonvulsant effect by the diversified mechanism of action such as levetiracetam, felbamate, and topiramate exhibited superior anti-oxidative stress activity in addition to their anticonvulsant activity.

Background: Nymphaea lotus (NL) is an aquatic perennial plant used traditionally in the management of various liver diseases. In this study, the protective effect of methanol extract of NL against carbon tetrachloride (CCl 4 )-induced chronic hepatotoxicity in rats was investigated. Methods: Male Wistar rats were assigned into six groups of five rats each. Group I received corn oil (0.5 mL p.o.) and served as control, group II received CCl 4 (1 mL/kg i.p., 1:3 in corn oil), group III received NL (200 mg/kg), and groups IV, V, and VI received CCl 4 +NL (50, 100, and 200 mg/kg, respectively) for 6 weeks. Twenty-four hours after the last exposure, rats were bled and killed. Results: The activities of alanine aminotransaminase (ALT), aspartate aminotransferase (AST), and levels of total bilirubin (TB) in the serum, thiobarbituric acid reactive substances (TBARS), superoxide dismutase, catalase, glutathione peroxidase (GPx) and glutathione (GSH) in the liver, and histopathology of the liver were determined using standard procedures. NL significantly (p<0.05) lowered the levels of ALT, AST, and TB and exhibited antioxidant potentials in rats exposed to CCl 4 relative to the control values. Specifically, NL at 100 and 200 mg/kg significantly (p<0.05) increased CCl 4 -induced decrease in hepatic GSH and GPx and also decreased the level of hepatic TBARS in CCl 4 -intoxicated rats. Histopathological findings revealed cellular infiltration and fibrosis in rats that received CCl 4 only, which were ameliorated in rats that received NL+CCl 4 . Conclusions: The data suggest that NL exhibited hepatoprotective effects in CCl 4 -intoxicated rats via antioxidative mechanism.

Background: Persicaria orientalis , an ornamental medicinal plant, has been used in traditional medicine for the treatment of various diseases. Although the plant is reported to have some important pharmacological effects, many medicinal values remain unidentified. Our objective was to evaluate the anti-inflammatory, anti-diarrheal, thrombolytic, and cytotoxic properties of the methanol extract of P. orientalis leaves (Po-MeOH). Methods: Anti-inflammatory activity was measured by the inhibition of hypotonicity-induced human red blood cell hemolysis and albumin denaturation technique in vitro of Po-MeOH. Diarrheal episodes were examined in mice with castor oil-induced diarrhea. The clot lysis and brine shrimp lethality bioassay in vitro were used to evaluate the thrombolytic and cytotoxic activities of the plant extract, respectively. Results: Using in vitro anti-inflammatory models, the results demonstrated that Po-MeOH at the five different dose ranges from 31.25 to 500 μg/mL significantly (p<0.05) protected (0.98%–50.71%) the erythrocyte membrane against lysis induced by hypotonic medium solution and protein denaturation (38.27%–79.22%) of bovine albumin, respectively. The extract exhibited a significant reduction of severity (75.17%) of castor oil-induced diarrhea in mice at the highest dose of 400 mg/kg compared to loperamide (82.06%) at 5 mg/kg. Po-MeOH also showed 33.14% clot lytic activity in the thrombolytic test and cytotoxicity with LC 50 value 58.91 μg/mL in the brine shrimp bioassay. Conclusions: These findings suggest that Po-MeOH has significant anti-inflammatory and anti-diarrheal effects along with moderate thrombolytic and lower cytotoxic properties that may warrant the further exploration.

Background: Surgical injury leads to postoperative pain hypersensitivity preceded by central nervous sensitization, due to lowered pain threshold in peripheral nociceptors and increased excitability of the spinal neurons. Pre-emptive analgesia is intended to decrease pain perception and overall analgesic need by use of drug regimen seizing central nervous system sensitization before exposure to painful stimuli. Earlier, few studies support pre-emptive analgesic efficacy of novel antiepileptic agent gabapentin. But topiramate and lamotrigine though proven analgesic in animal models of chronic pain and clinical studies of gabapentin resistant neuropathic pain; literature search revealed scarce data on its pre-emptive analgesic efficacy. The present study is designed to study and compare the pre-emptive analgesic efficacy of lamotrigine, topiramate and gabapentin (as control) in postoperative pain control. Methods: This randomized clinical trial included 90 patients of either sex, between 18 and 70 years undergoing major surgeries. Patients were randomly allocated into control and test groups and received respective treatment 30 min before induction of anesthesia. Aldrete’s score and pain score were recorded using visual analogue scale and facial and behavioral rating scales at awakening and at 1, 2, 4, 6 and 24 h. Postoperative rescue analgesic consumption for 24 h was recorded. Data were analyzed using OpenEpi and SciStatCalc statistical softwares. Results: Significantly higher pain scores were observed in the topiramate group postoperatively for 2 h on all pain scales (p<0.05). Lamotrigine-treated patients were more comfortable throughout the study with significantly less (p<0.05) postoperative analgesic requirement comparable to gabapentin. Conclusions: Study results are strongly suggestive of pre-emptive analgesic efficacy of single oral dose lamotrigine comparable to gabapentin and superior to topiramate in postoperative pain control.

Background: Isoniazid, also called isonicotinyl hydrazine (INH), is a commonly used drug for treating tuberculosis. The main drawback is its toxic side effects. Centella asiatica has long been used in the Ayurvedic system of medicine owing to its wide medicinal properties. This study was designed to examine the effectiveness of C. asiatica ethanolic leaf extract (CA) on INH-treated albino rats. Methods: The adverse effects induced by INH (50 mg/kg bw) administration on haematological parameters, oxidative status (thiobarbituric acid-reactive substances, superoxide dismutase, catalase, and reduced glutathione), liver and kidney function markers, and their amelioration by various concentrations of CA (20, 40, 60, and 100 mg/kg bw) or silymarin (SIL) (50 mg/kg bw, administered before 1 h of INH treatment for 30 days to rats) were studied. Moreover, histological studies were carried out in liver and kidney tissues of rats treated with the most effective concentration to further support the possible effectiveness of CA on INH-intoxicated rats. Results: All the affected parameters returned to near-normal levels, and the effective concentration of extract was found to be 100 mg/kg bw. The histology of both the liver and the kidneys subsequently supported the effectiveness of CA (100 mg/kg bw). Conclusions: Altogether, the results suggest that CA at 100 mg/kg bw can substantially reduce the toxic effects of INH.

Background: Sanchezia speciosa has been used in traditional medicine for gastritis treatment in Vietnam. Some phytochemical study showed that S. speciosa contains high amounts of flavonoids and cardiac glycoside compounds. In the present study, we isolated four compounds from the ethanol extract of the S. speciosa leaf, and we evaluated the in vitro antioxidant and anti-inflammatory effect of the isolated compound from the ethanol extract of the S. speciosa leaf. Methods: The leaf of S. speciosa Leonard was extracted with ethanol 96%. Compounds were isolated using column chromatography and identified by spectroscopic method, including IR, MS, and NMR and by comparing their physicochemical and spectral data with those published in literatures. These isolated compounds were investigated for their antioxidant activity using DPPH and inflammation inhibitory activity by inhibition of albumin denaturation assay. Results: We have isolated four compounds quercetin 3- O - α - l -rhamnopyranosid ( quercitrin ) (1), quercetin 3- O-β- d -galactopyranosid (hyperosid) (2), sitosterol-3-O-β-D-glucopyranosid (daucosterol) (3), and 3-methyl-1H-benz[f]indole-4,9-dione (4) from the ethanolic extract of the S. speciosa leaf. The antioxidant activities were in the following order: compound 2 >compound 1>compound 4 >compound 3 . The IC 50 values of scavenging DPPH radicals for compound 2 was 20.83±1.29 μg/mL. For anti-inflammatory activities, the order was compound 4 >compound 3 >compound 2 >compound 1 . Compound 4 showed the strongest inhibition, with IC50 values of 193.70±5.24 µg/mL. Conclusions: These compounds 1 , 2 , and 4 were isolated for the first time from the leaves of S. speciosa. These compounds showed strong antioxidant and anti-inflammatory activity.

Background: Blepharospasm is one of the components of drug-induced Meige’s syndrome which is reported to be caused by typical antipsychotics. Reports of blepharospasm or Meige’s syndrome caused by atypical antipsychotics are rare. Case: A 30-year-old female patient presented to psychiatry out patient department (OPD) with chief complaints of inability to keep her eyes open for long and excessive blinking for 2 months, irritation of eyes, watery discharge from eyes and photophobia for last 1 month. The patient had been taking olanzapine 10 mg, sertraline 100 mg and divalproex sodium 500 mg per orally on once a day basis for the management of major depressive disorder with psychotic features for last 6 months. Routine blood analysis, thyroid function, EEG, MRI, lipid profile did not reveal any abnormality. Ocular examination was also within normal limits. Olanzapine was suspected as a culprit for the above symptoms of patient, so it was replaced with quetiapine 25 mg/day. Patient showed partial recovery of symptoms within 1 week and complete recovery within 2 months of stopping olanzapine. Causality of olanzapine-induced blepharospasm as per WHO-UMC scale was probable. Conclusions: Olanzapine (atypical antipsychotics) should also be kept in the list of suspected drugs causing blepharospasm in psychotic patients on treatment although further similar evidences from observational studies and/or reports are needed to establish the causal relationship.