Larvicidal Activity of Some Plants Extracts and Their Partitioned Fractions against Culex quinquefasciatus

Aim:The methanol extracts of fifteen plants and their partitioned fractions were screened for larvicidal activity against the fourth instar of larvae Culex quinquefasciatus, the vector of lymphatic filariasiswith a view to identifying the active ones.Methodology:The plant parts were collected,separatelydried and milled. Each powdered material was extracted in methanol at room temperature for 3 days, with agitation. The extract was filtered and concentrated in vacuo. Each extract was tested against the fourth instar larvae of Cx. quinquefasciatus. The methanol extracts were suspended in water and successively partitioned into n-hexane and ethylacetate. Each partitioned fraction was also tested against the fourth instarlarvae of Cx. quinquefasciatus.Results:About fifty six percent (56.3%) of the tested extracts had moderate larvicidal activity after 48 hours. The fruitextract of Thevetia neriifoliaand the leaf extracts of Calotropis procera andOriginal Research Article Solanum macrocarpon were the most active. After partitioning the methanol extracts, each of the plant extracts had one or two highly active partitioned fractions after 48 hours. The n-hexane fractions of S. macrocarpon(0.78 ± 0.03 mg/mL) and Spondias mombin(0.81 ± 0.03 mg/mL) were the most active.Conclusion:The non-polar fractions of S. macrocarponand S. mombinwere the most active. Purification of these highly active fractions could lead to the isolation of potent larvicidal compounds that could be used in the control of Cx. quinquefasciatus mosquito

Anti-Acetylcholinesterase Compounds Isolated from the Leaves of Kigelia africana (LAM) Benth (Bignoniaceae)

Acetylcholinesterase (AChE) is an enzyme that is involved in the breakdown of some neurotransmitters. Its inhibition is one of the treatment strategies employed in the management Alzheimer diseases. Flavonoids isolated from the leaves of Kigelia africana were investigated for their comparative AChE inhibition. The extract of the leaves was subjected to vacuum liquid chromatography (VLC) to obtain four fractions using n-hexane (n-hex, 100%), n-hexane/dichloromethane (hex/DCM, 1:1), dichloromethane/ethyl acetate (DCM/EtOAc, 1:1) and ethyl acetate/methanol (EtOAc/MeOH, 1:1). The four fractions were subjected to AChE inhibitory study with DCM/EtOAc (1:1) fraction showing the highest inhibitory activity. Three flavonoids were isolated from this fraction and their structures were elucidated and characterised using 1D- and 2D-nuclear magnetic resonance (NMR) spectroscopy and mass spectrometry (MS) techniques. Their spectroscopic data compared well with literature. The compounds demonstrated considerable inhibition of AChE activity with luteolin (1), rutin (2) and quercetin (3) that showed IC50 of 945.0, 282.1, 254.8 μg/ml respectively as against the IC50 of 38.93 μg/ml for rivastigmine, a well-known cholinesterase inhibitor. Compound 3 showed 17.89 ± 0.57 and 7.70 ± 0.64 μ/l/mg protein at 200 and 400 μg/ml respectively, for AChE activity as against 10.37 ± 0.99 and 6.24 ± 1.24 μ/l/mg protein showed by rivastigmine at 200 and 400 μg/ml respectively. This study showed that the constituents responsible for the AChE inhibition in the crude extract as reported by Falode et al., 2017 resided in the DCM/EtOAc (1:1) fraction. The structure-activity relationship of the flavonoids revolves around substitution in position 3 of the compounds.

Anti-diabetic Activity of Convallatoxin Isolated from the Root Bark of Parquetina nigrescens (Afzel.) Bullock (Asclepiadaceae)

This study investigated the anti-diabetic activity of the root bark extract of Parquetina nigrescens and the isolated compound, convallatoxin, from the root bark. A powdered sample of the plant was extracted with methanol, and the extract (A) was tested in glucose-loaded normal rats at 100, 200 and 400 mg/kg for the determination of the most active dose. The anti-diabetic activity of A at 200 mg/kg was carried out on streptozotocin-induced diabetic rats. A was further partitioned to obtain its n-hexane (B1), dichloromethane (B2), ethyl acetate (B3) and mother liquor (B4) fractions that were tested for blood glucose lowering activity using glucose-loaded normal rats model. The anti-diabetic activity of the isolated compound from B3 was carried out on streptozotocin-induced diabetic rats. The results were subjected to one way ANOVA followed by Bonferroni post hoc tests and p< 0.05 was considered significant. A showed dose-independent and time dependent blood glucose level reduction activity at 200 mg/kg with the highest percentage of 30% at 4 h that was comparable to the standard, glibenclamide at 5 mg/kg. A at 200 mg/kg showed a blood glucose level reduction of 49, 68 and 70% by Day 4, 7 and 10 respectively as against glibenclamide at 5 mg/kg of 18, 33 and 39% by Day 4, 7 and 10 respectively on streptozotocin-induced diabetic rats. B3 showed a time-dependent blood glucose level reduction activity up to the fourth hour similar to glibenclamide with 35% as against 38% of glibenclamide. B1, B2 and B4 were devoid of blood glucose level reduction activity. Convallatoxin isolated from B3 gave 83 % blood glucose levels reduction at day 10 as against 38% of glibenclamide. The anti-diabetic activity of convallatoxin was significantly (p<0.05) more than glibenclamide at all-time point. The structure of convallatoxin was determined using IR, 1D and 2D NMR spectroscopy and the spectroscopic data compared well with published data in the literature.

Clinical neuropsychiatric correlates and EEG findings among children with developmental disorders in Lagos, Nigeria

Abstract Objective: Developmental disorders with or without associated neuropsychiatric complications continue to be one of the major health problems in Africa. The grossly inadequate management/ rehabilitative facilities further worsen this. A prospective study aimed at finding the types of developmental disorders and associated neuropsychiatric complications among children aged ≤15 years that presented with developmental disorder in the study centers over 36 month study duration. Methods: The study was carried out in the paediatric and child psychiatric clinics as well as the Electroencephalographic (EEG) unit of two major health facilities in Lagos, Nigeria: Lagos University Teaching Hospital (LUTH) and Psychiatric Hospital, Yaba, Lagos. For each subject, socio-demographic data was obtained and appropriate clinical evaluation was carried out to obtain the necessary data and clinical diagnoses. Furthermore, each of the subjects had waking EEG recording using 20-channel computerized Medelec® EEG machine. The EEG interpretation was blinded to the clinical history of the subjects. Results: Overall, one hundred and eleven (111) subjects were evaluated over the 36 month study period. The cohort was made up of 63 (56.8%) males and 48 (43.2%) females. The mean age was 4.8 (±3.9) years, with most subjects falling in the age group of 0-5 years(69.4%). Mixed specific developmental disorders were most common (55%) followed by that of specific developmental disorders of speech and language (34.2%). Forty-one (36.9%) subjects suffered from one or more types of complications, with seizure, 22(19.8%) being the most common. The waking EEG recording was normal in 22 (19.8%) subjects; while abnormal epileptiform activities were found in 85 (76.6%) of recordings. No statistically significant relationship existed between EEG abnormalities and the factors of age and clinical diagnoses (i.e developmental abnormalities). Conclusion: The small number of subjects in this study is a major hindrance to drawing a general conclusion. However, it has been shown that a number of the cohort in addition to their developmental disorders suffered from such complications as seizures, hyperactivity etc. Furthermore, a significant proportion had EEG abnormalities of the epileptiform types possibly reinforcing the previously known fact of prevalent subtle brain damage among African children. The need for preventive health care is therefore emphasized

Determination of the physicochemical properties of pyronaridine - a new antimalarial drug

The physicochemical properties of pyronaridine, a new antimalarial drug, have been determined for the first time in this study, since these parameters are comprehensively not available in literature. UV-Vis spectral analysis of both pyronaridine and its tetraphosphate salt were carried out in various solvents, in addition to solubility of the two drugs in these solvents. Partition coefficient was done in n-octanol-water mixture using the Leo-Hansch method as well hydrophobicity index determination. pKa determination was carried out on the tetraphosphate. UV-Vis spectral characteristics showed that both the base and the tetraphosphate salt have significant light absorption in the range 190-380nm. Solubility in different solvents revealed that pyronaridine base is sparingly soluble in chloroform [1.34%] while it is slightly soluble in methanol [0.29%] and ethanol [0.42%] and very slightly soluble in octanol and distilled water. The tetraphosphate salt was sparingly soluble in water [1.46%] while it is only very slightly soluble in other solvents. The higher aqueous solubility of the salt was further revealed by a greater Rm value on extrapolation to 100% water concentration in hydrophobicity index determination. Log P value determination showed that the base [log P of 0.26 +/- 0.02] is more liposoluble than the salt [logP of - [1.24 +/- 0.21]]. Four prominent pKa values were obtained for the tetraphosphate titrated which when extrapolated to the base gave values of 7.08 +/- 0.05, 7.39 +/- 0.05, 9.88 +/- 0.05 and 10.30 +/- 0.10. The results should guide in formulation of appropriate dosage forms to improve bioavailability of the drug especially from oral routes

Hyperlipidemia among Saudi diabetic patients-Pattern and clinical characteristics

Premature development of atherosclerosis and increased rate of coronary artery and peripheral vascular diseases are characteristic features of patients with diabetes mellitus. Hyperlipidemia is an important precipitating factor for these diseases. Several patterns of lipid alteration among diabetics were described; the most common is hypertriglyceridemia. This study was constructed to look at the pattern of lipid alteration among Saudi diabetic patients. Forty-three percent of diabetic patients were dyslipidemic with an equal distribution of dyslipidemic patients with respect to type of dyslipidemia, i.e., combined hyperlipidemia, hypercholesterolemia and hypertriglyceridemia. There was a higher percentage of affected female patients with dyslipidemia compared with male patients. This predominance continued when risk factors such as obesity, poor glycemic control, duration and therapy of diabetes mellitus were considered. There is lack of awareness and treatment of dyslipidemic diabetic patients among practicing physicians in spite of the propagated knowledge on the decreased rate of coronary events and regression of atheroma in the vascular walls of the coronary arteries upon treatment of hypercholesterolemia. There is a need to periodically screen the diabetic population and implement vigorous therapy for dyslipidemic ones

Diabetes mellitus in Saudi Arabia: the clinical pattern and complications in 1,000 patients

A retrospective and prospective study of 1,000 ambulatory and hospitalized diabetic patients was done in Riyadh, Saudi Arabia. Saudis comprised 777 [77.7%] and non-Saudis 223 [22.3%]. Sex distribution was equal among Saudis, males 389 [50.1%] and females 388 [49.9%], but non-Saudi males were predominant at 153 [68.6%], non-Saudi females 70 [31.4%] reflecting the preponderant male expatriate labor force. A proportion of different types of diabetes was: IDDM 115 [11.7%], non-obese non-insulin dependent diabetes mellitus [NIDDM] 405 [41.0%], obese NIDDM 412 [42.1%], and early onset non-insulin dependent diabetes [diagnosis under 30 years of age], 43 [4.4%]. Regarding treatment, 388 [40.6%] received insulin followed by sulfonylurea, alone in 330 [33.5%], diet only in 117 [12.0%], combination sulfonylurea and biguanide in 113 [11.6%], biguanide alone in 13 [1.3%] and insulin plus tablets in 7 [0.8%]. Of 472 and 426 patients, 29.7% and 30.0% had elevated total cholesterol or triglycerides respectively, while 77.2% of 373 patients had elevated glycosylated hemoglobin [HbAl]. At least once in 998 patients, diabetic ketoacidosis occurred in 7.6%,hypoglycemia [BS

nature and prognosis of thyroid disorders and the heart

This is an attempt to review the current major thyroid disorders that may affect the heart directly and/ or indirectly and their prognostic pattern. It is accepted that cardiac disability can occur in thyroid dysfunction in the absence of any other underlying cardiac abnormality. This "Thyrocardiac disease" occurs more commonly within creasing age and in the elderly and may reflect occult thyroid function impairment. The advent of non-invasive cardiology particularly cross-sectional echocardiography has demonstrated ability to assess ventricular internal dimensions and function and to detect various cardiac disorders in the so called thyroid heart disease. Nevertheless great awareness has been reached in the age long controversy regarding the magnitude of cardiac abnormality in thyroid disorders

Clinical and electrophysiologic study of polyneuropathy among diabetic patients in Saudi Arabia

Seventy diabetic patients [44 males, 26 females] were evaluated for peripheral neuropathy clinically and by nerve conduction studies [NCS]. These included conduction velocity, distal latency, peak-to-peak amplitude and area in two motor [median and common perineal] and two sensory nerves [median and sural] Sixty-three patients had type II diabetes and seven had type I. Their median age was 47 years and median duration of diabetes six years. NCS results were scored using values previously obtained in healthy controls. Thirty-three patients [47.1%] had clinical neuropathy [22 definite, 11 probable] and 37 [52.8%] were normal. Clinical neuropathy showed significant association with type of treatment [x2 = 8.38, p = 0.038], but not with control of diabetes or its duration presumably because of the relatively small number of patients studied. NCS were normal in 14 patients [20%] and abnormal in 56 [80%] with the following pattern of abnormalities: mild sensorimotor neuropathy 13 [18%], moderate sensorimotor 11 [16%], severe sensorimotor 10 [14%], predominant sensory 17 [24%] predominant motor 5 [7%]. The NCS status showed no statistically significant association with type of treatment, diabetes control or duration. In multiple regression analysis, only clinical neuropathy contributed significantly to NCS status [p = 0.01]. The prevalence of clinical neuropathy in Saudi diabetic patients is similar to that in other populations and the greater sensitivity of NCS has been confirmed

effect of bacterial infection on oxidative burst activity in leukocytes from diabetic patients

Respiratory burst activity in phagocytes was assessed by measuring luminal dependent chemiluminescence [CL] in whole blood and isolated polymorphonucleocytes [PMNs] from four groups of subjects in the basal state and after stimulation with phorbol myristate acetate [PMA]. The groups were: healthy controls [group I]; diabetics with bacterial infection [group II]; diabetics without infection [group III]; and non-diabetics with bacterial infection [group IV]. In the basal state with whole blood, there was a statistically significant difference in resting CL response only between groups I and II, [p<0.05, by ANOVA and t-test with Bonferoni's adjustment]. With isolated PMNs, there was no statistically significant difference between any of the groups. After stimulation with PMA, in whole blood there was a statistically significant difference, p<0.05 when group II was compared with groups I and III. With isolated PMNs, the only significant observation was between groups II and III, p<0.05. In the presence of bacterial infection, PMNs from diabetic patients demonstrated higher CL responses than controls and non-diabetic patients with infection. The findings suggest that PMNs from diabetic patients with bacterial infection can be functionally and metabolically activated. The susceptibility to infection in diabetic patients may not be due to impairment of the respiratory burst activity in PMNs

comparison of acute glycaemic and insulin response to dates [phoenix dactylifera] and oral dextrose in diabetic and non-diabetic subjects

An oral glucose tolerance test [OGTT] with 75 g dextrose and an oral dates tolerance test [ODTT] using an isocaloric [300 kcal] amount of dates [110 g] were performed in 16 well-controlled non-insulin dependent diabetic patients and 10 healthy subjects, using semi-dried Sukkari dates [AI-Qassim] in the ripe [tamer] stage. In the patients, the glucose values were significantly higher after dextrose, p<0.05, from 60 to 120 min and the incremental area under curve [IAUC] for glucose [mmol/litre 2h,mean +/- SE] following dextrose -76.1 +/- 5.2, was significantly larger than for dates - 51.4 +/- 3.1, p<0.05. Among the non-diabetic controls, there was no significant difference in the glucose levels following dextrose and dates throughout the tests and the IAUC for dextrose -21.6 +/- 2.2 and dates - 11.9 +/- 2.1 were not significantly different, p>0.05. The glycaemic index [Gl] for dates in patients -67 +/- 6 was not significantly different from the value in controls -56 +/- 8.5, p>0.2. The IAUC [micro U/ml 2 h, mean +/- SE] for insulin in patients were: dextrose -147.9 +/- 25.7, dates -129.4 +/- 17.0, p>0.5. In controls, the values were dextrose: 164.6 +/- 22.7, dates: 61.0 +/- 14.7, p<0.025, reflecting a significantly blunted response to dates. The glycaemic potential of the variety of dates used in this study was two-thirds that of pure dextrose in well-controlled diabetic patients but just over half in healthy volunteers. Dates stimulated less insulin secretion than dextrose in healthy subjects. Further studies are necessary to determine whether dates will adversely affect the control of diabetes significantly

Short stature at the University College Hospital Ibadan; Nigeria

Twenty four patients (female and male) were evaluated for short stature at the University College Hospital; Ibadan; Nigeria; over a seven years period. The causes of short stature were linked to various diseases. Although comprehensive hormonal data were not available in most of these patients; the clinical descriptive study is the first attempt at reporting some of the causes of short stature in Nigerians

Computerised axial tomographic scanning in neuropsychiatric disorders

The invention of the computerised tomography scanner - a product of modern bio-medical technology has significantly enhanced the diagnosis capability of physicians in the management of brain disorders. Despite the development of newer neuro-radiological equipment; the CT scanner remains a most invaluable diagnostic tool and should be given priority consideration in health vote allocation

Pattern of diabetic foot lesions in Saudi Arabia: experience from King Khalid University Hospital, Riyadh

A retrospective study was carried out to estimate the magnitude and pattern of foot lesions seen in diabetics living in Saudi Arabia. A review of the records of 1010 diabetic patients seen at King Khalid University Hospital, Riyadh, revealed an overall prevalence of 10.4% for diabetic foot lesions. Of these, 88 patients were further characterized; 55 [62 .5%] were males and 33 [37.5%] were females. Seventy-five patients [85.2%] were Saudis and 13 [14.8%] were non-Saudis. The average age was 58 years. Eighty-five patients had type 2 diabetes and three had type 1. The spectrum of foot lesions included: 10 cases of cellulitis, 33 cases of ulcers, 29 cases of gangrene, and 16 cases of abscess. Evidence of peripheral vascular disease was present in 48 patients [54.5%] while peripheral neuropathy was found in 43 [48.8%]. Surgical debridement with prolonged dressing was done in 58 patients [66%] while amputation was performed in 30 [34.1%]. The average hospitalization was 6.8 weeks. Diabetic foot lesions constitute a major complication of this disease in Saudi Arabia. The high amputation rate is a source of concern and improved techniques are urgently needed to reduce this serious outcome