Isolation,fractionation and evaluation of the antiplasmodial properties of Phyllanthus niruri resident in its chloroform fraction

Objective:To investigate the antiplasmodial activity of Phyllanthus niniri(P.niruri) methanol extract(ME) and its fractions in mice.Methods:P.niruri methanol extract and its chloroform. ethanol and aqueous portions were tested against chloroquine-sensitive Plasmodium berghei berghei in early,established and repository models of infection using Knight and Peter’s 4-day suppressive model,Rvlev and Peters curative model and Peters prophylactic model respectively. Results:Chemosuppression of parasitemia(37.65%-50.53%) was elicited by 100-400 mg/kg(b.w.) of ME.Al doses of 100 mg/kg b.w..the chloroform fraction(F1) significantly(P【0.01) suppressed parasitaemia by 85.29%,while ethanol and aqueous fractions(F2 and F3.respectively) elicited 67.06%and 51.18%chemosuppression.the most active fraction.F1 was selected for further antiplasmodial screening.In established infection.ME reduced parasitaemia(15.81%- 62.96%) while F1 significantly(P【0.01) reduced parasitaemia(44.369—90.48%).with effects comparable to that of chloroquine(96.48%).The prophylactic antiplasmodial activity of ME(92.50%suppression) was also significant(P【0.01) and was more effective than pyrimethamine(85.00%).additionally, cell membrane integrity of non-parasitized erythrocytes intubated with 125-500 mg/mL F1 was maintained.Conclusions:These findings indicate the antiplasmodial efficacy of P.niruri methanol extract,and the localization of this effect in its chloroform fraction.

Identification of sitosteryl glucoside palmitate in a chloroform-derived fraction of Phyllanthus niruri with antiplasmodial and peripheral antinociceptive properties

Objective:To evaluate the antiplasmodial properties of fractions of chloroform portion of Phyllanthus niruri(P.niruri) methanol extract and identify a suitable chemical marker present therein.Methods:Chloroform portion of P.niruri methanol extract was separated from silica gel using gradient systems of hexane,ethylacetate and methanol.The fractions were screened for antiplasmodial activity against Plasmodium falciparum HB3 and FcM29.Fractions with IC_(50)<10μg/ml.against parasites were further screened for peripheral analgesic activity,while cytotoxicity was evaluated using THP-1 cells.Results:Fractions 12-14 were very active(IC_(50)<10 μg/mL) against Plasmodium falciparum and showed no significant cytotoxicity.Fractions 12 and 13 exhibited significant(P<0.01) reduction in acetic acid-induced writhing in mice,decreasing the number of writhes by 66.67% and 65.22% respectively and comparable with 100 mg/kg aspirin(65.22%).From fraction 12,a compound was isolated and identified as sitosteryl-6-β-D-glucoside-6'-palmitate by ~1H,^(13)C nuclear magnetic resonance and mass spectroscopies.Conclusions:Our findings illustrate antiplasmodial column fractions of P.niruri with analgesic activity and identify sitosteryl glucoside pahmitate as a chemical marker of activity.

Chemometric Analysis of Volatile Compounds of NIPRINEEM Oil and Other Brands of Neem Seed Oils Sold in Nigeria

Azadirachta indica A. Juss (neem, family Meliaceae) is a reputable medicinal plant. Various parts of the plant are used as a remedy against different ailments, as a natural pesticide, as raw material in the cosmetic industry, and for marking other commodities. The seed oil is a major product of the plant and its quality depends on the seed quality and extraction methods employed. In this study, the chemical profile of NIPRDNEEM oil is compared with that of other brands of neem seed oils by using gas chromatography-mass spectrometry (GC-MS) and chemometrics. The fatty acid identified in NIPRDNEEM oil were: oleic acid (34.09%), stearic acid (11.4%), linoleic acid (15.94%), palmitic acid (23.4%), arachidic acid (0.73%), and the other compounds were: 1-Monolinoleoylglycerol trimethylsilyl ether (0.95%) and farnesyl alcohol (13.20%). The branded oils were composed predominantly of oleic acid (13.50% - 26.76%), palmitic acid (6.88% - 11.99%), linoleic acid (7.32% - 11.17%), stearic acid (4.29% - 13.08%), and arachidic acid (0.53% - 1.27%). The unbranded oil contained oleic acid (30.04%), stearic acid (14.91%), linoleic acid (14.62%), palmitic acid (12.34%), and arachidic acid (0.93%). Stigmasterol, stigmasterol acetate, and sitosterol were the sterols identified in the oils. Characterization of the fatty acid profile of neem seed oil is vital for industrial and economic purposes. The fatty acids profile of the NIPRDNEEM oil and other neem seed oil were comparable. Both PCA plots and HCA dendrogram from the chemometric analysis shows three main grouping of all samples. While NIPRDNEEM and the local neem oil were grouped, suggesting a high degree of resemblance of both samples.

Anti-Tubercular Activities and Molecular Characterization of Salivary Extract of Leech (<i>Hirudo medicinalis</i>) against <i>Mycobacterium tuberculosis</i>

Leech salivary extract (LSE) was screened for the anti-tubercular activity against Mycobacterium tuberculosis using microbroth dilution method. The bioactive components in LSE were determined using Shimadzu GC-MS QP2010 SE. The LSE exhibited bactericidal effects on M. tuberculosis at 50% (v/v). The result of the GC-MS analysis of LSE revealed seventeen (17) bioactive components. The major fatty acid components were oleic acid (33.9%) and palmitic acid also known as hexadecanoic acid (22.6%). Other bioactive components detected in appreciable amounts in LSE include, 4-bromobutyric acid (16.86%), 6,17-Octadiene-1-ol acetate (9.78%) and octahydro-1,4,9,9- tetramethyl (5.21%). The anti-tubercular activity of the LSE was attributed to these bioactive components. The results obtained suggest that leech salivary extract could be used in treating tuberculosis.

Evaluation of <i>In-Vitro</i>Anti-Tuberculosis Activity of <i>Tetrapleura tetraptera</i>Crude and Fractions on Multidrug Resistant <i>Mycobacterium tuberculosis</i>

The management, control and elimination of tuberculosis (TB) have been difficult with the advent of HIV and cases of multidrug resistant (MDR-TB) tuberculosis. The cases of multidrug resistance to rifampicin and isoniazid pose greater challenges on first line and second line drugs to eliminate TB. The study is aimed at establishing anti-tuberculosis activity of Tetrapleura tetraptera against Mycobacterium tuberculosis and MDR-TB and the phytochemical present. The leaves of Tetrapleura tetraptera were collected, weighed, dried and pulverized to powder. The pulverized leaves of Tetrapleura tetraptera were subjected to 70% methanol extraction and screened for phytochemical. The crude extract was further purified into fractions using silica gel and thin layer chromatography techniques. M. tuberculosis and MDR-TB were obtained from positive acid fast bacilli sputa of TB patients and confirmed using GeneXpert to differentiate genotypic drug susceptible M. tuberculosis and MDR-TB. The sputa were digested using sodium hydroxide-cysteine technique and cultured in Middlebrook 7H9. The crude extract and fractions were screened for anti-tuberculosis activity using tetrazolium microtitre plate assay. The results showed that Tetrapleura tetraptera crude had activities against M. tuberculosis at 7.4 ± 0 mg/ml and 27.5 ± 0 mg/ml for MDR-TB. One of the fractions inhibited the growth of M. tuberculosis at 0.24 ± 0 mg/ml and MDR-TB at 0.89 ± 0 mg/ml. The phytochemical screened includes tannins, alkaloids, saponins, flavonoids, phenols and resins. T. tetraptra possesses anti-tuberculosis potential at low concentration on MDR-TB and can be a lead compound in drug development for the treatment of tuberculosis and multidrug resistant tuberculosis.

Antimalarial potency of the leaf extract of Aspilia africana(Pers.) C.D.Adams

Objective:To investigate the antimalarial activity of ethanol extract of Aspilin africana (A.africana) leaf.Methods:The ethanol extract of A.africana leaf(100-400 mg/kg) was screened for blood schizonticidal effect against chloroquine-sensitive Plasmodium berghei(P. berghei) in mice both in early and established models of antimalarial studies.Results:The leaf extract exhibited significant(P【0.05) antiplasmodial activity in 4-day early infection and in established infection tests with a considerable mean survival time comparable to that of standard drug,chloroquine(10 mg/kg).Conclusions:The findings show thai ethanol extract of A.africana leaf possesses potent antiplasmodial activity which justify the use in ethnomedicine and can be developed in malaria therapy.

Seropositivity of Chlamydophila pneumoniae immunoglobulin G antibody of HIV/AIDS patients in Abuja,Nigeria

Objective:To detect IgG antibody to Chlamydophila pneumoniae(CP) in sera of HIV/AIDS patients and provide rationale for inclusion of routine screening for anti-CP antibodies and anti-chlamydial agents in the Nigerian National H1V/AIDS Management Plan.Methods:Serum samples from 34 consenting HIV/AIDS patients attended a Government-approved Antiretroviral Treatment Facility in Abuja were screened by enzyme-linked immunosorbent assay for anti-CP IgG antibody using ImmunoComb? Chlamydia Bivalent IgG Test kit(Orgenics,Israel).Results: Anti-CP IgG antibody was detected in 20(58.8%) of 34 patients tested.The detection rale was higher among the males(8/13:61.5%) than the females(12/21:57.1%).Patients of the age group 16-30 years had the highest(7/10:70%) detection of anti-CP IgG antibody.Conclusions:The result of the present study suggests the presence of anti-CP antibodies in sera of the HIV/AIDS patients,and reinforces the need for routine screening for anti-CP antibodies as a necessary intervention to reduce the burden of Chlamydophila pneumoniae(C.pneumoniae) infections and to reduce HIV-positive morbidity in Nigeria.The outcome of this study also provides justification for the possible inclusion of anti-chlamydial agents in the National HIV/AIDS Management Plan to provide prophylaxis against or treat active C.pneumoniae infections.

Preparation and evaluation of colon targeted drug delivery systems for albendazole using kneading,extrusion and compaction technology

Albendazole is an orally administered broad-spectrum benzimidazole anthelmintic used against helminthiasis,hydatid cyst disease and neurocysticercosis.The objectives of this investigation are to develop a sustained release drug delivery system for albendazole,and to target its delivery to colon.Albendazole matrix tablets containing varying proportions of single and binary blends of four polymers;polyacrylic acid(carbopol 971),ethylcellulose(Etcell),eudragit L100-55(EUD),and sodium carboxymethyl cellulose(CMC) were prepared by a modified wet granulation technique of kneading,extrusion and compaction.In vitro release profiles of albendazole was sequentially determined in simulated gastric fluid(SGF),simulated intestinal fluid(SIF) without enzymes and in rat caecal content medium(RCCM) at 37 ℃.The in vitro drug release from matrix tablets containing CMC and Etcell as single polymers showed initial burst effect in the first 2 h(>20% and 50% respectively),followed by a slow release in SIF.However,matrix tablets containing polymer blends showed that no appreciable drug release occurred up to 5 h.Drug release from tablets containing polymer blends in the dissolution medium containing rat caecal material suddenly increased to ≥30% after 5 h(RCCM),and reaching up to 90% in 24 h.Albendazole matrix tablets containing carbopol 971,Etcell,EUD,and CMC as single polymers and as blends were formulated for oral use.Drug release from the tablet matrices containing carbopol alone,binary blends of carbopol/Etcell,and CMC/EUD were found to be very slow and dependent on polymer concentration.Matrix tablets containing blends of these polymers formulated using kneading,extrusion and compaction technique could provide sustained drug release and can be utilized in the colonic delivery of albendazole.

Sero-Prevalence of Human Immunodeficiency Virus (HIV-1) among High Risk Groups in Abuja, Nigeria

Measurement of HIV prevalence among the general population as well as among specific sub-groups who are at high risk of infection is crucial for planning and for providing health care for those who are infected. This study was aimed to determine the prevalence of HIV-1 infection among high risk groups in Abuja. The testing for the presence of HIV antibodies was carried out using Determine&#174;HIV-1/2 Test Cards (Inverness Medical, Japan), UnigoldTM kit (Trinity Biotech, Ireland) and Stat Pak&#174;HIV-1/2 (Chembio Diagnostic Systems, Inc. USA). A total of 1587 high risk persons were screened for HIV-1, 739 (46.6%) were males while 848 (53.4%) were females. 261 (16.4%) tested HIV-1 positive, out of which 74 (5.3%) were males and 190 (11.1%) were females. This study indicates that the incidence of HIV-1 is higher among the females. Prevalence is higher within the age range of 26 - 30 years (5.17%) and highest prevalence was observed within the age range of 31 - 35 years in males (1.32%) and of 26 - 30 years in females (3.91%). Commercial sex workers had the highest prevalence of HIV-1 (7.01%), while Commercial Motorcyclists had the least (2.02%) (p ≤ 0.05). This study has shown that there are local sub-epidemics of HIV infection in Abuja.

Prevalence of HIV among Adolescent Children in Abuja, the Federal Capital Territory, Abuja Nigeria

Adolescents in Africa have low HIV testing rates. Determining the HIV prevalence among this group is very important because adolescents living with HIV (ALHIV) have worse health outcome than other populations of people living with HIV. This study aimed at determining the prevalence of HIV among children of adolescents age (10 - 18 years) that come for HIV testing in virology laboratory of National Institute for Pharmaceutical Research and Development, Abuja from January 2013 to December 2018. The result was expressed in percentage and disaggregated by sex. Out of 533 adolescents tested over 6 years, 252 (51.9%) females and 234 (48.1%) were males. A total of 69 (14.1%) of them were tested HIV positive which 42 (8.6%) were females and 27 (5.5%) were males. The result of this study indicates that there is epidemics of HIV among adolescents living in Federal Capital Territory Abuja. It is also evident that females are more vulnerable to HIV infection than the males. There is therefore need for urgent standard and comprehensive procedure for adolescents living with HIV transitioning from paediatric to adult care. This also calls for intensive enlightment on HIV education especially in our basic and post basic schools in Abuja.