Search

A rapid, selective, and precise high performance thin layer chromatographic method was developed and validated for the simultaneous analysis of paracetamol, caffeine, phenylephrine and chlorpheniramine in tablets. The chromatographic analysis was carried out on glass plates pre-coated with silica gel 60 F254 as a stationary phase. The optimized mobile phase was methanol : n-butanol : toluene : acetic acid (8:6:4:0.2 v/v). TLC chamber of 10 × 20 cm was used with saturation time of 15 min. The retardation factor (RF) for chlorpheniramine, phenylephrine, caffeine and paracetamol was found to be 0.15 ± 0.02, 0.29 ± 0.02, 0.50 ± 0.02, 0.68 ± 0.02 respectively. Detection was carried out at 212 nm. Validation study was done following ICH Q2 (R1) guideline. The regression data for the calibration plots showed good linear relationship with R2 = 0.997 over the concentration range of 300–1,500 ng band−1 for caffeine, R2 = 0.996 over the concentration range of 100–500 ng band−1 for phenylephrine, R2 = 0.996 over the concentration range of 200–600 ng band−1 for chlorpheniramine, R2 = 0.998 over the concentration range of 400–2,400 ng band−1 for paracetamol. The method was validated for precision, accuracy and recovery. Minimum detectable amounts were found to be 304.9 ng band−1, 87.88 ng band−1, 117.18 ng band−1 and 143.06 ng band−1 for caffeine, phenylephrine, chlorpheniramine, and paracetamol respectively while the limit of quantification was found to be 923.95 ng band−1, 266.32 ng band−1, 355.11 ng band−1, and 433.53 ng band−1 in the same order. The method was successfully applied to analyze two marketed tablets in a selective and reproducible manner.

According to World Health Organization (WHO) 10% of the medicines in the Low and Middle Income Countries (LMICs) are of poor quality posing a major public health threat. One way to circumvent such problem is the development and deployment of rapid, economical and efficient analytical methods. Hence this research aims to develop a High-Performance Thin Layer Chromatography (HPTLC) method for the determination of doxycycline hyclate. A rapid and simple HPTLC method with densitometry detection at 360 nm to determine doxycycline hyclate in capsules and tablet formulations was developed and validated. HPTLC was performed on glass plates coated with C18 reverse phase silica gel 60 F254 and pretreated with 0.27 M ethylenediaminetetraaceticacid (EDTA) solution. The mobile phase was dichloromethane: methanol: acetonitrile: 1% aqueous ammonia in the ratio of 10:22:53:15 (v/v). The linearity range lies between 200 and 1,000 ng/spot with correlation coefficient of 0.997. The Rf value is 0.5 ± 0.02%. Recoveries were in the range of 94.50–100.5%. Limit of detection and limit of quantitation values for doxycycline hyclate were 40 and 160 ng/spot respectively. The developed method was validated as per ICH guidelines. Thus, it was found to be accurate, precise, specific and robust. In forced degradation study, doxycycline hyclate was found to degrade in acidic and alkaline media, and through oxidative stress. The drug was found to be relatively stable to heat and photo degradation. The method was successfully applied for the routine quantitative analysis of dosage forms containing doxycycline hyclate. The developed method offered comparable results (as confirmed by F-test) with that of the HPLC pharmacopoeial (BP) analysis method.

Pyrazole-bearing compounds are known for their diverse pharmacological effects including potent antileishmanial and antimalarial activities. Herein, some hydrazine-coupled pyrazole derivatives were successfully synthesized and their structures were verified by employing elemental microanalysis, FTIR, and 1H NMR techniques. The in vitro antileishmanial and in vivo antimalarial activities of the synthesized pyrazole derivatives (9–15) were assessed using the clinical isolate of the Leishmania aethiopica strain and mice infected with Plasmodium berghei ANKA strain, respectively. The result revealed that compound 13 displayed superior antipromastigote activity (IC50 = 0.018) that was 174- and 2.6-fold more potent than the standard drugs miltefosine (IC50 = 3.130) and amphotericin B deoxycholate (IC50 = 0.047). The molecular docking study conducted on Lm-PTR1 justified the better antileishmanial activity of compound 13. Furthermore, the target compounds 14 and 15 elicited better inhibition effects against Plasmodium berghei with 70.2% and 90.4% suppression, respectively. In conclusion, the hydrazine-coupled pyrazole derivatives may be considered potential pharmacophores for the synthesis of safe and effective antileishmanial and antimalarial agents.

Milk is a complete food useful to promote growth and development of the infant mammals as it contains vital nutrients (proteins, essential fats, vitamins, and minerals) in a balanced proportion. It is also a nutritious food for adults too. Milk can also contain hazardous chemicals and contaminants including heavy metals which can be a risk for health. This study was aimed at determining the level of heavy metals in cow's milk collected from Butajira and Meskan districts, south Ethiopia. Cows' milk was collected from 193 healthy lactating cows. Samples were digested by optimized microwave digestion method using HNO

Many complex mixtures usually constitute hundreds or even thousands of individual components of interest. Such mixtures are much too complicated to be separated for analytical duties in a reasonable period of time using only a single-dimensional chromatographic method. However, if a complex mixture is separated by an initial dimension using multi-dimensional liquid chromatography, a simpler portion of that separation is collected and goes to the second dimension. Each of these fractions will be analyzed separately, allowing exceedingly complex mixtures to be resolved in a short period of time. This chapter explains the fundamental principles, theoretical discussions as well as various applications with typical examples of multi-dimensional liquid chromatography in different fields.

Satureja punctata Benth. Briq. (Lamiaceae) is a small shrub known by its vernacular name “Lomishet”. It is used in Ethiopian traditional medicine for the treatment of hypertension, diabetes, liver disease, headache and febrile illness. Mean Arterial Blood Pressure (MABP) lowering effect and vasorelaxant activity of the aqueous extract of aerial parts of the plant were studied. Intravenous administration of the aqueous extract at different doses brought a fall in MABP in normotensive guinea pigs and also in renovascular hypertensive guinea pigs. The extract also caused a dose-dependent relaxation of precontracted aorta; with a maximum relaxation of 98.19% achieved at 40 mg/ml. Preparative reversed-phase HPLC analyses of the extract resulted in the isolation of two phenolic compounds, namely, rosmarinic acid and linarin. The structures of these compounds were elucidated using UV, IR, MS, and NMR (1D and 2D) techniques. Furthermore, rosmarinic acid showed significant (p < 0.01) reduction of MABP in normotensive guinea pigs at doses of 0.75, 1.50 and 3.00 mg/kg. The findings of this study suggest that the aerial parts of S. punctata have genuine antihypertensive activity.

Background Iodine is one of the crucial micronutrients needed by the human body, and is vitally important during pregnancy. This study aimed to determine the relationship between the iodine status of pregnant women and their knowledge, and practices regarding iodized salt. All participants were enrolled in the Butajira nutrition, mental health and pregnancy (BUNMAP) cohort, Butajira, Ethiopia in February-May, 2019. Methods In this cross-sectional study, 152 pregnant women without hypertension or known thyroid disease before or during pregnancy were randomly selected from the BUNMAP mother to child cohort (n = 832). Spot urine samples were collected to estimate the level of urinary iodine concentration (UIC). Salt samples were also collected from their homes. The Sandall-Kolthoff (S-K) method was used to measure the level of iodine in the urine samples, and iodometric titration was used to measure the level of iodine in the salt. Data was entered and cleaned using Epi-info version 3.5.3 and then exported to SPSS version 20 for further analysis. Multivariate logistic regression analysis was performed to identify associations in the collected data. Results The WHO recommended level of iodine for populations of pregnant women is 150–249 F06Dg/L. The median UIC among pregnant women in this study was 151.2 μg/L [interquartile range (IQR) = 85.5–236.2 F06Dg/L], at the low end of this range. About half (49.65%) of the participants were likely to be iodine deficient. There was a significant association between having a formal job (AOR = 2.56; CI = 1.11–5.96) and iodine sufficiency. Based on a cutoff of >15 ppm (mg/kg), 91.7% (95% CI: 87.2–96.2) of the salts collected from the household had adequate iodine content. The median iodine level of the collected salt samples was 34.9 mg/kg (ppm) (IQR = 24.2–44.6 mg/kg). Conclusions The UNICEF 2018 guidelines for adequate iodine nutrition in pregnant women include both a recommended median range of 150–249 μg/L, and an upper limit of 20% on the fraction of the population with UIC below 50 μg/L. Because our study population’s median level is 151.2 μg/L and the percentage of pregnant women with urinary iodine concentration of less than 50 μg/L is 9.7% (14/145), the women received adequate iodine nutrition. The availability of adequately iodized salt in households is more than 90%, as recommended by WHO. In light of previous iodine deficiency in this region of Ethiopia, the salt iodization program promotes the health of babies and mothers.

BackgroundMilk is a complete food useful to promote growth and development of the infant mammals as it contains vital nutrients including proteins, essential fats, vitamins, and minerals, in a balanced proportion. Milk can also contain chemical hazards and contaminants, such as heavy metals which can be a risk for health. This study was aimed at determining the level of the heavy metals in cow’s milk collected from Butajirra and Meskan districts, south Ethiopia. Cows’ milk was collected from 193 healthy and lactating cows. Samples were digested by optimized microwave digestion method using HNO 3 and H 2 O 2 . Analysis was done using ICP-OES for Cd, Cr, Cu, Fe, Mn, Ni, Pb, and Zn. MP-AES was used for Ca, Mg, K and Na. ResultsNi was not detected in all the milk samples. The concentrations of metals in the studied milk samples were, Cd (0.0 – 0.03), Cr (0.0 – 0.4), Cu (0.03 – 1.1), Fe (0.0– 1.9), Mn (0.0– 0.7), Pb (0.0– 12.3), Zn (0.0–8.2), Ca (380.1– 532.4), Mg (159.6– 397.9), K (1114.2–1685.8) and Na (495.9–1298.3) ppm. These values were compared with guide lines of different international organizations for food and other available literatures. Cd, Cr, Cu, Mn, Pb, Zn and Mg were found over the permissible limits. ConclusionSpecial attention should be given to the level of heavy metals in cows’ milk, since they are difficult to remove from the body and are dangerous to health once they accumulate to a level greater than their limit.

Crinum abyscinicum Hochst. ExA. Rich bulb is traditionally used in Ethiopia for the treatment of various ailments including internal parasites, mastitis, rabies, colic diseases of animals, and cancer. Despite its importance in traditional cancer treatment, no research work has been reported on the antiproliferative activity of the bulb extract and its major constituents. Phytochemical investigation of the bulb extract of C. abyscinicum by PTLC over silica gel resulted in the isolation of two alkaloids, which were unequivocally identified as 6-hydroxycrinamine and lycorine on the basis of 1H- and 13C-NMR and MS analysis. The bulb extract, 6-hydroxycrinamine, and lycorine possessed significant antiproliferative activity, lycorine being the most active exhibiting GI50 values of 2.8 μg/ml and 3.4 μg/ml against A2780 and MV4-11 cells, respectively. Cell cycle analysis and annexin V/propidium iodide double staining in A2780 cells revealed that both compounds increased the percentage of cells in the S-phase at 30 μg/ml without inducing apoptosis. Our results suggest that the antiproliferative activities of the bulb extract of C. abyscinicum, 6-hydroxycrinamine, and lycorine could support the traditional claim of the plant against cancer.

Introduction: Bromazepam is hydrolyzed in acidic aqueous solution leading to a series of degradation products. The rate of acidic hydrolysis is believed to be dependent on the state of protonation of the pyridyl and azomethine nitrogen atoms. Stability test is important in pharmaceutical industry to provide evidence on how the quality of an active substance or pharmaceutical product varies with time under the influence of a variety of environmental factors. Objective: The aim of the study was to develop a simple stability indicating method for the determination of bromazepam. Method: Bromazepam solution was prepared and forced degradation of bromazepam was performed under acid hydrolysis using sulphuric acid. High performance liquid chromatography determination of pure and degraded bromazepam and bromazepam-copper (II) complex was performed using reversed phase octyl C-8 column under isocratic conditions and the chromatographic conditions were set as follows; the flow rate of the mobile phase was 1.5 mL/min; injection volume was 10 μL, column temperature was 30oC and the detector wavelength being 309 nm. Results: Bromazepam, its degradation product and bromazepam chelated with copper (II) were determined using the developed mobile phase with flow rate of 1.5 mL/min. Good separation with sharp peak, minimum tailing and retention time repeatability was obtained. The rate order, rate constant and half-life of degradation were also determined, and it was observed that the degradation reaction follows the first order kinetics. Conclusion: Chromatographic separation of bromazepam chelated with copper (II) was achieved and the method can be further used in drug manufacturing quality control.

Honey is an important bee product of greater nutritional value. Ethiopia is one of the main producers of it. Honey is known to accumulate trace metals which are essential as well as toxic. Moreover , as bees collect nectar from flora of nearly in an area of around 100 km radius, the level of toxic metals in honey is an important indicator for environmental pollution by toxic metals. Thus, in this study, the qualities of 12 Ethiopian multi-floral honey samples were evaluated in terms of common physicochemical parameters, namely, moisture content, pH, free acidity, lactonic acidity, and total acidity. The values found were moisture content from 14.23 to19.2 %; pH from 3.4 to 4.8; free acidity from 30.6 to 97.6 meq Kg−1; lactonic acidity from 8.06 to 14.4 meqKg−1, and Total acidity from 42.96 up to 107.4 meqKg−1. The analyzed samples showed proper maturity, absence of undesirable fermentation, and were in agreement with standard values (Codex Alimentarius) and reported literatures. The concentrations of trace heavy metals (Cd, Cr, Cu, Mn, Ni, Pb, and Zn) in 12 multi-floral honey samples were also evaluated using flame absorption spectrometry after wet digestion. The accuracy of the method was assessed by spiking honey samples with known amounts of standard metals and examining recovery. The contents of trace metals in honey samples were found to be in the range of Non-Detectable (ND)-0.017 μgg−1, ND-0.15 μgg−1, 0.02–1.15 μgg−1, ND-7.29 μgg−1, ND, ND-2.53 μgg−1and 9.96–16.03 μgg−1for Cd, Cr, Cu, Mn, Ni, Pb, and Zn, respectively. Results obtained are in agreement with a report in the literatures and with codex limits and thus they did not pose as such any health risk.

Objective: In this study four tea samples Gumero black, Wushwush black and Wushwush green from Agri- Ceft Plc and East Africa black tea leaves from East African Agribusiness Plc were investigated for total polyphenols, caffeine, catechin and L-theanine content. Materials and Methods: The aqueous extracts were investigated for their antioxidant and antileishmanial property and effect on amphotericin B, miltefocine and sodium stibogluconate, the commonly used antileishmanial drugs. Antileishmanial studies were conducted on L. aethiopica . Results: Wushwush green tea had the highest content of polyphenol (19.98 ± 1.15 mg gallic acid equivalent /100 g dry leaf weight), catechin (37.06 mg/g) and L-theanine (48.54 mg/g but the lowest caffeine content). It exhibited the highest antioxidant activity. The highest antioxidant effect of Wushwush green tea may be attributed to the highest polyphenol content. East African black tea had the lowest L-theanine (20.72 mg/g) and antioxidant activity but the highest caffeine (16.60 mg/g) content. Conclusion: Wushwush green tea showed slight inhibitory effect on L. aethiopica while the lack tea extracts (Gumero, East Africa and Wushwush) exhibited no antileishmanial activity. Wushwush green tea did not show any synergistic or antagonistic effect on the antileishmanial drugs used in this study while Gumero, East Africa and Wushwush black tea extracts exhibited dose dependant inhibitory activity to the commonly used antileishmanial drugs included in this study.

The present study investigated the bioaccumulation of organochlorines in two milk-producing animals (goats and cows) grazed on the same feed to explore the extent of organochlorines availability in milk and any species effect on the bioaccumulation pattern. Six organochlorine pesticides: aldrin, α-endosulfan, β-endosulfan, p,p′-DDE, o,p′-DDT and p,p′-DDT were determined in samples collected from four regions in Ethiopia. Aldrin (11.6 μg kg−1) was detected only in one cow milk sample and α-endosulfan was detected in one goat milk sample at a level of 142.1 μg kg−1, and in one cow milk sample (47.8 μg kg−1) from the same region. p,p′-DDE was detected in 40% of the milk samples analyzed while o,p′-DDT and p,p′-DDT were found in high amounts in almost all samples. The average total DDT (excluding DDD) in the samples was 328.5 μg kg−1. Regions known for their malaria epidemics were the most contaminated with DDT residue. The accumulation pattern in both species was not clear under natural sampling.

Background Ajuga remota Benth is traditionally used in Ethiopia for the management of diabetes mellitus. Since this claim has not been investigated scientifically, the aim of this study was to evaluate the antidiabetic effect and phytochemical screening of the aqueous and 70% ethanol extracts on alloxan-induced diabetic mice. Methods After acute toxicity test, the Swiss albino mice were induced with alloxan to get experimental diabetes animals. The fasting mean blood glucose level before and after treatment for two weeks in normal, diabetic untreated and diabetic mice treated with aqueous and 70% ethanol extracts were performed. Data were statistically evaluated by using Statistical Package for the Social Sciences software version 20. P-value

A simple, specific, precise and accurate simultaneous high-performance thin-layer chromatographic method of analysis for hydrocortisone and clotrimazole was developed and validated. The method employed HPTLC glass plates (20x10) mm precoated with silica gel 60 F 254 as the stationary phase. The solvent system consisted of Toluene: Propanol: Ammonia (13:3:0.1v/v) that gave compact spots with R f value of 0.27 ± 0.01 and 0.58 ± 0.02 for hydrocortisone and clotrimazole, respectively. Densitometric analysis of hydrocortisone and clotrimazole was carried out in the absorbance/reflectance mode at 226nm. The calibration curves showed good linear relationship with R2 = 0.996 + 0.003 and 0.996 + 0.002 in the concentration range of 200-1200 and 200-1000 ng/µl for hydrocortisone and clotrimazole, respectively. The method was validated for precision, recovery and robustness. The LOD & LOQ were found to be 35.31, 107.01 and 34.93, 105.87 ng/µl for hydrocortisone and clotrimazole respectively. Statistical analysis proved that the method is repeatable, specific and accurate for the estimation of the studied drugs. Resolution of hydrocortisone, clotrimazole and their degradation products formed under different stress conditions (acid-base hydrolysis, oxidation and thermal degradation) was successfully achieved with the developed method indicating that it can be employed as a stability indicating method.

Two series of pyridine derivatives were synthesised and evaluated for their in vivo anti-malarial activity against Plasmodium berghei. The anti-malarial activity was determined in vivo by applying 4-day standard suppressive test using chloroquine (CQ)-sensitive P. berghei ANKA strain-infected mice. Compounds 2a, 2g and 2h showed inhibition of the parasite multiplication by 90, 91 and 80%, respectively, at a dose level of 50 µmol/kg. Moreover, The most active compounds (2a, 2g and 2h) were tested in vitro against CQ-resistant Plasmodium falciparum RKL9 strains where compound 2g showed promising activity with IC(50) = 0.0402 µM. The compounds were non-toxic at 300 and 100 mg/kg through the oral and parenteral routes, respectively. The docking pose of the most active compounds (2a, 2g and 2h) in the active site of dihydrofolate reductase enzyme revealed several hydrogen and hydrophobic interactions that contribute to the observed anti-malarial activities.

A high performance thin layer chromatography (HPTLC) method was developed and validated for determination of two anti-asthmatic drugs, salmeterol xinafoate and fluticasone propionate in co-formulations. Study was performed on pre-coated silica gel HPTLC plates using n-hexane:ethyl acetate:acetic acid (5:10:0.2) as a mobile phase. A TLC scanner set at 250nm was used for direct evaluation of the chromatograms in reflectance/absorbance mode. Method was validated according to ICH guidelines. Determination coefficients of calibration curves were found 0.9977 and 0.9936 in the ranges 100–1000 and 200–2000ngband−1 for salmeterol and fluticasone, respectively. Method had an accuracy of 99.5% for salmeterol and 102.01% for fluticasone. Method had the potential to determine these drugs simultaneously from dosage forms without any interference.

A high-performance thin-layer chromatographic method (HPTLC) for the simultaneous determination of lamivudine and zidovudine in a binary mixture has been developed. The method developed was based on HPTLC separation of the two drugs followed by densitometric measurements of spots at 276 and 271 nm for lamivudine and zidovudine, respectively. Separation was carried out on Merck HPTLC silica-gel 60 F254 plates, using toluene/chloroform/methanol (1:6:3 v:v) as the mobile phase. Validation of the method was performed based on The International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use (ICH) guidelines in terms of linearity, accuracy, precision, limit of detection, limit of quantification, and robustness. Second-order polynomial equations were obtained for the regression line in the ranges of 250–1400 and 250–1700 ng/spot for lamivudine and zidovudine respectively. Correlation coefficient (r) values were 0.9998 for both analytes. The method...

For ages, the practice of drug discovery has relied heavily on the one-drug one-target design strategy of medicinal chemistry. However, despite the tremendous advances made in chemical and biological sciences and in the discovery technologies the number of drugs/drug candidates coming out from this one-drug one-target approach is paradoxically dwindling. It is now well recognized that the age old philosophy of medicinal chemistry lacks a fundamental conceptual framework. This is particularly so in disorders such as depression where a multiple of pathways are simultaneously deregulated and which basically result from multiple molecular abnormalities, not just from a defect in a single pathway. The recent times has seen a shift towards one drug-multiple target selective design strategy. This novel paradigm has already produced a diverse set of multiple acting structures for depression. Largely as a consequence of the unacceptable side effects, tolerability and low level of efficacy of the currently used drugs (tricyclic antidepressants, mono amine oxidase and selective serotonin reuptake inhibitors), other new generation agents are increasingly being identified that act at more than one target in depressive disorders. Multitarget selective antidepressant research has produced a number of diverse and novel chemistries with a huge potential for the treatment of this debilitating disorder. This manuscript reviews the latest developments surrounding multitarget selective agents for depression, the benefits of such multi acting agents and the implications for the future design of potent and selective dual, triple or even poly-target active antidepressants.

In Ethiopia, malaria control has been complicated due to resistance of the parasite to the current drugs. Thus, new drugs are required against drug-resistantPlasmodiumstrains. Historically, many of the present antimalarial drugs were discovered from plants. This study was, therefore, conducted to document antimalarial plants utilized by Sidama people of Boricha District, Sidama Zone, South Region of Ethiopia. An ethnobotanical survey was carried out from September 2011 to February 2012. Data were collected through semistructured interview and field and market observations. Relative frequency of citation (RFC) was calculated and preference ranking exercises were conducted to estimate the importance of the reported medicinal plants in Boricha District. A total of 42 antimalarial plants belonging to 27 families were recorded in the study area. Leaf was the dominant plant part (59.0%) used in the preparation of remedies and oral (97.4%) was the major route of administration.Ajuga integrifoliascored the highest RFC value (0.80). The results of this study revealed the existence of rich knowledge on the use of medicinal plants in the study area to treat malaria. Thus, an attempt should be made to conserve and evaluate the claimed antimalarial medicinal plants with priority given to those that scored the highest RFC values.

The essential oil composition of the leaves of Rosmarinus officinalis L. and Lippia adoensis Hochst. var. koseret Sebsebe, the leaf and stem of Foeniculum vulgare Miller, and the seeds of Coriandrum sativum L. were analyzed by GC and GC-MS. The antioxidant activity of the EOs was also examined. Hydrodistillation of leaves of F. vulgare yielded an essential oil lighter than water (0.09%), and a heavy oil fraction (0.48%), while stems gave 0.09% of EO. The percentage yield of EO from the leaves of R. officinalis and L. adoensis was 0.33% and 0.19%, respectively. The seeds of C. sativum gave an EO yield of 0.46%. A total of 18 (99.93%) and 53 (99.51%) compounds were detected from the light and heavy oils of the leaves of F. vulgare, respectively. The light leaf oil of F. vulgare was found to contain mainly aromatic compounds while the heavier oil was found to be rich in monoterpenoids. F. vulgare stem EO was observed to contain 20 (99.83%) compounds which were mostly similar to the ones in the light...

Background Malaria is a neglected tropical parasitic disease affecting billons of people around the globe. Though the number of cases and deaths associated with malaria are decreasing in recent years, it is the most deadly disease in the world. This study aimed at investigating the in vivo antimalarial activities of some 2,3-disubstituted-4(3H)-quinazolinone derivatives. Results The in vivo antimalarial activities of the test compounds (6–9 and 11–13) were investigated using the 4-day suppressive standard test in mice infected with chloroquine-sensitive Plasmodium berghei ANKA strain. The tested compounds showed significant antimalarial activities with mean percentage suppression of 43.71–72.86 % which is significantly higher than the negative control group (p

Background The majority of the Ethiopian population is at risk of malaria largely caused by Plasmodium falciparum. The resistance of the parasite to existing drugs is the main challenge in the control of the disease and thus new therapeutic drugs are required. In Ethiopia, people use different plant species to treat malaria. However, very few of them have so far been evaluated for their safety level and antimalarial activity. Thus, the aim of this study was to evaluate the safety and antimalarial activity of extracts of Ajuga integrifolia, Clerodendrum myricoides, Melia azedarach, Peponium vogelii and Premna schimperi, locally used by the Sidama people of Ethiopia to treat malaria. Methods The safety level of 80 % methanol extracts of the plants were evaluated using standard acute toxicity test procedure. The antiplasmodial activity of 80 % methanol extracts of the plants were assessed in vivo using Swiss albino mice against chloroquine sensitive rodent malaria parasite, Plasmodium berghei, using the standard 4-day suppressive test procedure at doses of 200,400 and 800 mg/kg/day. The 80 % methanol extract of Ajuga integrifolia that exhibited better antimalarial activity was fractionated using different solvents and screened for its phytochemical constituents and evaluated in vivo for its antimalarial activity at doses of 100, 200 and 400 mg/kg/day. Results All extracts given at the three different doses caused no lethal effect on mice in 24 h and within 10 days of observation. All extracts and fractions exhibited antimalarial activity in a dose dependant manner. The highest inhibition was exhibited by the crude extracts of A. integrifolia (35.17 %) at 800 mg/kg/day (P

Bioassay-guided fractionation using the human colorectal adenocarcinoma (HT-29) cell line of the methanol extract of dried roots of Podocarpus falcatus led to the isolation of two new type C nagilactones, 16-hydroxynagilactone F (1) and 2β,16-dihydroxynagilactone F (2), and the new totarane-type bisditerpenoid 7β-hydroxymacrophyllic acid (4), along with the seven known compounds 2β-hydroxynagilactone F (3), macrophyllic acid (5), nagilactone D (6), 15-hydroxynagilactone D (7), nagilactone I (8), inumakiol D (9), and ponasterone A (10). The structures of the new compounds were determined by 1D and 2D NMR, HRESIMS, UV, and IR and by comparison with the reported spectroscopic data of their congeners. The orientation of the C-2 hydroxy group of 3 and 8 was revised to be β based on evidence from detailed analysis of 1D and 2D NMR data and single-crystal X-ray diffraction studies. Among the isolated compounds, the nagilactones, including the new dilactones 16-hydroxynagilactone F (1) and 2β,16-dihydroxynagilactone F (2), were the most active (IC50 0.3-5.1 μM range) against the HT-29 cell line, whereas the bisditerpenoids (4 and 5) and the other known compounds 9 and 10 were inactive. The presence of the bioactive nagilactones in P. falcatus supports its traditional use.

Volatile fractions from the roots of Echinops kebericho Mesfin were obtained by hydrodistillation and solid-phase microextraction (SPME) and analysed by gas chromatography–mass spectrometry (GC–MS); 65 compounds, representing 73.9% of the volatile fraction in the hydrodistillate from the roots, and 63 compounds, representing 78.6% of the volatile compounds in the SPME extract of the roots of E. kebericho, were identified. The main constituent found in hydrodistilled essential oil was eudesm-7(11)-en-4-ol (14.3%), followed by caryophyllene oxide (9.7%) and τ-cadinol (8.3%). High amounts of β-cubebene (22.7%), followed by β-patchoulene (11.1%), longifolene (10.4%), and cyperene (8.2%), were detected by SPME. Using both extraction methods, a total of 83 compounds were detected in E. kebericho essential oil. Monoterpenoid compounds represented 2.1% (seven compounds) and 2.1% (10 compounds) of the essential oil volatiles obtained by hydrodistillation and SPME, respectively, whereas sesquiterpenoids represented 72.5% (43 compounds) and 75.7% (31 compounds), respectively. Copyright © 2006 John Wiley & Sons, Ltd.

The essential oil and headspace volatiles from the root, stem, leaf and flower head of Echinops ellenbeckii O. Hoffm. were obtained by steam distillation and headspace solid-phase microextraction (HS-SPME). The samples were then analyzed by gas chromatography-mass spectroscopy (GC-MS). Using the HS-SPME analysis, twenty-eight compounds (20.4 %) were identified in the root, twenty-three (55.4 %) in the stem, nineteen (32.2 %) in the leaf and fourteen (16.0 %) in the flower. From the steam distillate, twenty-two (18.7 %), four (15.4 %), nine (39.7 %) and twenty-eight (92.9 %) compounds were observed in the root, stem, leaf and flower, respectively. Using both methods of extraction, seventy compounds were detected in the whole plant. The main sesquiterpene constituents were β-selinene (3.14 %) in the flower, β-maaliene (4.04 %) in the root, caryophyllene oxide (4.93 %) in the leaf and cyperene (8.64 %) in the root. The root were found to have the largest number of sesquiterpene constituents followed...

The concentration of some heavy metals was determined in barley locally grown for brewing and its malt in Ethiopia. The samples were digested in nitric acid and hydrogen peroxide, and analysed by atomic absorption spectrometry equipped with deuterium arc background corrector. The concentrations of Cd, Cu, Mn, Pb and Zn in barley, and the levels of Cu, Mn and Zn in malt were above the maximum permissible limits in cereal grains set by Food and Agriculture Organization/World Health Organization except Cd in barley grains from West Arsi Zone. Even though Cd and Pb were found in barley grains, they were below the limits of detection in malt. The result of the survey confirmed that the Cd and Pb content in locally malted barley do not pose a risk to consumers’ health though the bio-important metals could do. However, the levels of heavy metals in locally grown barley and its malt need to be regularly monitored.

The synthesis of a novel series of 1H-pyrazole derivatives was achieved by condensation of pyrazole aldehyde 1 with hydrazine hydrate to give hydrazone 7. On the other hand, cyclization of α,β-unsaturated ketone counterpart 2 using hydrazine hydrate in liquid aliphatic acids rendered compounds 4-6 and hydrazine hydrate in ethanol afforded compound 3. The later was allowed to react with aroyl chloride giving rise to compounds 8, 9. All compounds were tested for their in vivo anti-malarial and in vitro antileishmanial activities. The anti-malarial activity was performed using Plasmodium berghei infected mice, while the anti-leishmanial activity of the compounds was determined against Leishmania aethiopica promastigotes using alamar blue reduction assay. Compound 3, 1-(4-methylphenyl)-3-phenyl-4-[3-(2-thienyl)-2-pyrazolin-5-yl]-1H-pyrazole, possessed the highest anti-malarial activity with suppression of 70.26%. The highest anti-leishmanial activity was exhibited by compound 2, 1-(4-methylphenyl)-3-phenyl-4-[1-(2-thienyl)-prop-2-en-1-one]-1H-pyrazole, with an IC50 of 0.079μg/ml. Hydrazone 7 showed appreciable dual anti-malarial (suppression = 62.30%) and anti-leishmanial activity (IC50 = 1.823μg/ml).

Background Leishmaniasis is a neglected tropical parasitic diseases affecting millions of people around the globe. Quinazolines are a group of compounds with diverse pharmacological activities. Owing to their promising antileishmanial activities, some 3-aryl-2-(substitutedstyryl)-4(3H)-quinazolinones were synthesized in good yields (65.2% to 86.4%). Results The target compounds were synthesized by using cyclization, condensation, and hydrolysis reactions. The structures of the synthesized compounds were determined using elemental microanalysis, infrared (IR), and proton nuclear magnetic resonance (1H NMR). The in vitro antileishmanial activities of the synthesized compounds were evaluated using Leishmania donovani strain. All the synthesized compounds displayed appreciable antileishmanial activities (IC50 values, 0.0128 to 3.1085 μg/ml) as compared to the standard drug miltefosine (IC50 = 3.1911 μg/ml). (E)-2-(4-chlorostyryl)-3-p-tolyl-4(3H)-quinazolinone (7) is the compound with the most promising antileishmanial activities (IC50 = 0.0128 μg/ml) which is approximately 4 and 250 times more active than the standard drugs amphotericin B deoxycholate (IC50 = 0.0460 μg/ml) and miltefosine (IC50 = 3.1911 μg/ml), respectively. Conclusions The results obtained from this investigation indicate that the synthesized and biologically evaluated quinazoline compounds showed promising antileishmanial activities and are good scaffolds for the synthesis of different antileishmanial agents. Electronic supplementary material The online version of this article (doi:10.1186/s13588-014-0010-1) contains supplementary material, which is available to authorized users.

Essential oil from the seeds and husks of Aframomum corrorima (Braun) P.C.M. Jansen were analysed by gas chromatography (GC–MS), and 55 compounds were identified. The main constituents found in the seed oil were the monoterpenes 1,8-cineole (44.3%) and sabinene (17.3%), whereas sesquiterpenic structures (≥2%) such as (E)-nerolidol (17.2%), β-caryophyllene (9.7%) and caryophyllene oxide (6.9%), dominated in the husk oil. Copyright © 2006 John Wiley & Sons, Ltd.

Different beer brands produced in Ethiopia were surveyed for the presence of Cd, Cu, Pb, Mn and Zn. The samples were digested in nitric acid and hydrogen peroxide, and analysed by atomic absorption spectrometry equipped with deuterium arc background corrector. The mean concentrations of metals in beer were as follows: Cd, 0.0014 mg/l; Cu, 0.0368 mg/l; Mn, 0.0954 mg/l; Pb, 0.006 mg/l; Zn, 1.5206 mg/l. The estimated daily intakes were calculated based on Ethiopian annual per capita beer consumption of 8.75 liters. The mean intakes of Cd, Cu, Pb, Mn and Zn through beer were estimated to be 0.0006, 0.0232, 0.0024, 0.0378 and 0.6076 μg/kg bw/day, respectively. The risk assessment of mean levels indicated that health risk associated with these heavy metals through consumption of beer was absent.

Leishmaniasis is a vector-borne parasitic disease caused by protozoan parasites belonging to the family Trypanosomatidae and genus Leishmania. The disease prevails in 88 subtropical and tropical countries in five continents where about 350 million people live. Approximately two million incidences of new cases are recorded every year, causing high morbidity and mortality with a wide spectrum of clinical manifestations in humans. Treatment for leishmaniasis depends on pentavalent antimonials developed 50 years ago as first-line drugs, whereas a limited range of other drugs such as paromomycin, miltefosine, and amphotericin B exist to supplement them. However, potential toxicity, costs, and emergence of drug-resistant pathogens are the most serious obstacles for successful treatment of the disease in most endemic areas. This demands the development of new antileishmanial agents. In this regard, the search for new drugs from various synthetic products continues, and involves also compounds isolated from natural sources and drugs used for the treatment of other ailments (cancer, viral infections, TB, immunosuppression, etc.) in order to discover compounds with unknown chemical structures and with potential novel modes of action. Medicinal and aromatic plants are a major source of natural organic compounds which are widely used as medicine. The extensive ethnomedicinal knowledge, diversity of plant species, and the disease burden worldwide necessitates the status of natural products in treatments of leishmaniasis to be assessed. This chapter will review plant crude extracts and fractions/active principles obtained from medicinal plants which are used in or have potential for the treatment of leishmaniasis. Plant species are systematically presented by family, bioactive phytochemicals in various classes, and results obtained on specific organisms tested. Recent empirical and rationale approaches for antileishmanial drug targeting and development of novel drugs derived from natural products will be discussed.

A validated HPLC method for the simultaneous determination of diminazene diaceturate and phenazone has been established for the analysis of the compounds in veterinary granules for injection and in bulk powders. The compounds were separated using a Symmetry RP 18 analytical column and detected by UV absorbance at 250 nm. Linearity, accuracy as well as the intra-assay precision, inter-day precision and specificity of the method were established. The limits of detection and quantification were 3.2 and 9.7 μg mL-1 for diminazene diaceturate and 9.57 and 28.99 μg mL-1 for phenazone. Method had the potential to determine these drugs simultaneously from dosage forms without any interference with each other.

Potential toxicity, costs, and drug-resistant pathogens necessitate the development of new antileishmanial agents. Medicinal and aromatic plants constitute a major source of natural organic compounds. In this study, essential oils of Artemisia absinthium L. and Echinops kebericho Mesfin were investigated by GC and GC/MS analyses. Isolated oils were screened for antileishmanial activity against two Leishmania strains (L. aethiopica and L. donovani), and toxicity on the human monocytic leukemia (THP-1) cell line and red blood cells in vitro. GC/MS Analysis revealed 65 compounds (93.74%) for Artemisia absinthium and 43 compounds (92.85%) for Echinops kebericho oil. The oils contained the oxygenated monoterpene camphor (27.40%) and the sesquiterpene lactone dehydrocostus lactone (41.83%) as major constituents, respectively. Both oils showed activity against promastigote (MIC 0.0097-0.1565 μl/ml) and axenic amastigote forms (EC(50) 0.24-42.00 nl/ml) of both leishmania species. Weak hemolytic effect was observed for both oils, showing a slightly decreased selectivity index (SI 0.8-19.2) against the THP-1 cell line. Among the two oils tested, E. kebericho exerted strong antileishmanial activity that was even higher than that of amphotericin B with significant cytotoxicity. This study, therefore, demonstrated the potential use of both oils as source of novel agents for the treatment of leishmaniasis.