Pharmacognosy

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    Access to Biosimilars in Federal Hospitals in Addis Ababa: Assessment of the National Medicines Regulatory Framework and Healthcare Professionals’ Perspectives
    (Addis Ababa University, 2025-05-13) Shimelis Ayele; Tsige Gebre-Mariam
    The introduction of biopharmaceuticals brought remarkable clinical outcomes, particularly in the treatment and management of challenging chronic diseases. However, the high cost of originator biologics limits their accessibility. The adoption of biosimilars offers a cost-effective alternative, reducing healthcare expenditures and improving patient access to biologic therapies. Despite their potential benefits, the national regulatory framework and lack of understanding and confidence of healthcare professionals hinder the accessibility and uptake of essential biosimilars.
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    Aminoalkyl and Oxazine of 2-Naphthol Derivatives: Synthesis, In vitro Antimicrobial and In Silico Studies
    (Addis Ababa University, 2024-02) Motbaynor,Gizachew; Bisrat,Daniel(PhD); Asres,Kaleab(PhD)
    Despite remarkable advancements in the past decade, infectious diseases continue to pose a significant threat, affecting millions and burdening global public health systems and economies. Currently, there is growing interest in 2-naphthol derivatives, particularly 1-aminoalkyl-2- naphthol derivatives, owing to their biological activities and their potential application in synthesizing other significant bioactive molecules. Therefore, in this study, two compounds were synthesized from a 2-naphthol framework. The synthesized compounds were purified through column chromatography, and their chemical structures were identified using 1H and 13C, DEPT- 90, and DEPT-135 NMR spectral data, as 1-(phenyl(ortho-tolylamino)methyl)naphthalene-2-ol (37) and 2-benzyl-2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazine (39). The potential antimicrobial activity of the synthesized compounds was evaluated by the disk diffusion and broth dilution method. At the same time, molecular docking and ADMET studies were conducted to investigate their possible mechanism of action and drug-like properties. From our findings, both synthesized compounds exhibited promising antibacterial activity against most tested bacterial strains at 200 μg/ml, showing zones of inhibitions (ZOIs) ranging from 6.0 mm to 15.5 mm. The positive standard ciprofloxacin demonstrated ZOIs between 11.5 mm and 20.5 mm. Compound 37 exhibited greater susceptibility against E. coli with a MIC value of 25 μg/ml followed by V. cholera (MIC) at 50 μg/ml. v In contrast, Gram-positive bacteria such as Bacillus pumilus and B. subtilis demonstrated the lowest sensitivity to compounds (37) and (39), displaying a ZOI value of 6.0 mm at 200 μg/ml. Both compounds 37 and 39 also displayed antifungal activity against most tested fungal species. In molecular docking analysis, compounds (37) and (39) demonstrated significant binding energy within the binding pocket of E. coli DNA gyrase B, yielding docking scores of -8.092 and -7.754 kcal/mol, respectively. Similarly, with C. albicans lanosterol 4α-demethylase, they displayed docking scores of -7.792 and -8.995 kcal/mol, respectively. Following the ADMET prediction analysis, both synthesized compounds exhibit favorable pharmacokinetics and drug-like characteristics, making them suitable for oral administration. In addition to the in vitro bioassay activity test, molecular docking results and ADMET predictions collectively convey the promising antimicrobial properties of both synthesized compounds. These findings imply that conducting further synthesis and evaluation of 2-naphthol derivatives could be beneficial in the ongoing efforts to develop antimicrobial drugs for combating infectious diseases and microbial resistance.
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    Analgesic and Antinflammatory Activities of the Root extract of Grewia schweinfurthii and its Constituent and Determination of Nutritional and Antinutritional Compositions of its Fruit
    (Addis Ababa University, 2023) Leta,Abdi; Hymete, Ariaya (PhD); Tadesse,Solomon(PhD); Giday,Mirutse(PhD)
    The utilization of current treatments can often result in harmful side effects, and cause patients to experience pain and inflammation. In Ethiopian, traditional healers have relied on medicinal herbs, such as Grewia schweinfurthii, which possess analgesic and anti-inflammatory properties. Despite their widespread use, studies regarding the nutritional content of wild edible plants (WEPs) in low-income nations like Ethiopia are limited. This study aimed to evaluate the analgesic and anti-inflammatory effects of 80% methanolic root extract of G. schweinfurthii and its chemical constituents, as well as to examining the nutritional and antinutritional content of its fruit. The root extract of G. schweinfurthii and its constituents were evaluated for their analgesic activity using acetic acid-induced writhing and hot plate tests. The root extract was subjected to column chromatography (silica gel) to isolate a compound coded as AL-03 and tentatively identified as 4-(2''-(4'-isopropylphenyl) propan-2''-yl)-2,3-dihydrofuran based on spectroscopic (1H, 13C NMR & HSQC) data. The root extract G. schweinfurthii demonstrated significant analgesic activity (p < 0.001) in the acetic acid-induced writhing test at doses of 200 and 400 mg/kg. Additionally, in the hot plate method, a dose of 400 mg/kg of root extract showed noteworthy analgesic activity (p < 0.001). In the carrageenan-induced acute inflammation model, all doses (100, 200, 400 mg/kg) of the root extract resulted in a significant decrease in paw edema compared to the negative control. Compound AL-03 also exhibited antinflammatory activities in a dose-dependent manner against carrageenan-induced paw edema. XI Proximate analysis was used to assess various nutritional parameters of G. schweinfurthii fruit, including crude protein, fat, total ash, crude fiber, and carbohydrates. In this regard, G. schweinfurthii fruit revealed the following composition: moisture (4.09 ± 0.10%); crude protein (11.24 ± 0.68%); fat (1.99 ± 0.01%); total ash (5.36 ± 0.20%); crude fiber (32.50 ± 0.50%); carbohydrate (44.82 ± 0.82%); and total energy (242.12 ± 1.72 kcal). Furthermore, phytate (62.97 ± 0.83%), tannin (3.97 ± 0.12%), and oxalate (0.28 ± 0.03%) were identified as antinutritional components. Overall, G. schweinfurthii fruit was found to be a reliable source of nutrients and bioactive compounds. The findings support the traditional medicinal use of the plant for analgesic and antinflammatory activities. Further research is recommended to explore additional bioactive compounds from the root extract of G. schweinfurthii and to analyze the mineral composition, such as amino acids, and vitamin C content of G. schweinfurthii fruit, as well as to conduct sub-acute and chronic toxicology testing
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    Anthelmintic Activity of the Seed Oil of Ricinus communis
    (Addis Ababa University, 2023-03) Berhanu,Temesgen; Asres, Kaleab(Prof.); Bisrat, Daniel(Dr.)
    Helminthic infections are among the most widespread parasitic infections in humans. It is estimated that more than half of the world’s population suffer from parasitic infections. It poses morbidity particularly in children and pregnant women. Helminthic infections are more common in developing countries with poorer personal and environmental hygiene. Plant-derived drugs and herbal remedies remain important resources to alleviate and cure diseases, especially in developing countries. Variety of plants from various families including Ricinus communis from the family Euphorbiaceae are used to treat helminthiasis across the world. R.communis is an annual oilseed crop commonly known as castor. Antimicrobial, antifungal, anticancer, antidiabetic, anti-inflammatory and antimalarial are some of the pharmacological activities that have been reported from extracts of R. communis. In the present study, the petroleum ether seed extract of R. communis, its base hydrolysate and the major constituent of the hydrolysate were tested for their anthelmintic activities against the model organism Caenorhabditis elegans. The dried and powdered seeds were extracted using petroleum ether and then the oil collected was subjected to base hydrolysis to obtain the hydrolysate. Fractionation of the hydrolysate by column chromatography packed with silica gel 60-G resulted in the isolation of the hydroxylated fatty acid (9Z)-12-hydroxyoctadec-9-enoic acid (ricinoleic acid). The isolated free fatty was esterified by 5% Potassium hydroxide solution in methanol to get ricinoleic acid methyl ester. Structural elucidation of the compounds was achieved by spectroscopic techniques including ESI-MS, 1H and 13C-NMR spectral data. Results of the anthelmintic assay revealed that VIII ricinoleic acid and its methyl ester are strongly active against C. elegans worms compared to the oil. Ricinoleic acid exhibited 97% mortality at the tested concentration of (1 mg/ml). In conclusion, the present study demonstrated that the oil of R. communis seeds possesses strong anthelmintic activity against the model nematode C. elegans worms and the activity of the oil would be attributed to the presence of ricinoleic acid as a major constituent.
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    Anti Tuberculosis Drug Induced Hepatotoxicity in Hiv Positive and Negative Patients
    (Addis Ababa University, 2005-06) Yimer, Getnet; Aseffa, Abraham(PhD)
    Anti-tuberculosis drug induced hepatotoxicity (DIH) is a common problem in the management of tuberculosis. This study was intended to identify possible risk factors for development of DIH, including degree of immunosuppression. In this prospective 2-month cohort study, 103 HIV positive and 94 HIV negative newly diagnosed tuberculosis patients were followed after initiation of DOTS (direct observed treatment short course). CD4 count was measured for the HIV positive patients. All patients were also evaluated for different risk factors including HBsAg, Anti-HCV, alcohol intake, use of other drugs including traditional medicines, acetylation status and presence of chronic illness. Patients were monitored biochemically (by liver function tests) and clinically for development of DIH weekly in the first month and bi-weekly in the second month after start of therapy. Biochemical hepatotoxicity was seen in 17.3% of the patients. CD4 counts of these patients were 0-50 for 7 (35%), 51-100 for 8 (40%), 101-200 for 4 (20%), and > 200 for 1 (5%). Three patients were positive for HBsAg and none had anti-HCV. Five patients died of non-hepatic causes among the patients who developed DIH. Eight out of the 34 patients with biochemical hepatotoxicity (23.5%) developed clinical hepatotoxicity that necessitated discontinuation of their anti-TB drugs. Seven of the eight were HIV positive, seven were female, and 2 were positive for HBsAg. Biochemical hepatotoxicity was significantly associated with HIV co-infection (p=0.002), concomitant drug intake (p=0.008), decrease in CD4 count (p=0.001), high mortality (p=0.001), and having Wt/Wt allele for acetylation status (p=0.026). Clinical hepatotoxicity is also significantly associated with being female (p=0.027), HIV co-infection (p=0.043), concomitant drug intake (p=0.003), HBsAg (p=0.046), decrease in CD4 count (p=0.025), and high mortality (p=0.0001). No significant association was seen between hepatotoxicity with alcohol intake, age, body mass index, type of TB and anti HCV positivity. The findings would assist in selectively managing patients at risk. It is recommended to have a regular biochemical and clinical follow up for those patients who are at risk of developing DIH .These patients include HIV positive patients, with special emphasis to those with a lower CD4 count, and patients who take drugs other than their anti TB medication. We also recommend that further work should be done to explore the reason for the observed association between DIH and female sex, HBsAg positivity, and acetylation status. Key words: Tuberculosis, HIV, Hepatotoxicity, Acetylation status, NAT2 gene
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    Antidiarrheal Activity of Crude Extract and Coumarins from Psydrax schim- periana (A. Rich.) Bridson. Roots in Swiss Albino Mice, and Evaluation of Nu- tritional Composition and Anti-nutritional Factors of Its Fruits
    (Addis Ababa University, 2023) Damissie,Getahun; Hymete,Ariaya(PhD); Tadesse,Solomon (PhD); Tolossa,Ketema (PhD)
    Despite considerable improvements in the accessibility of medical services, diarrheal illnesses continue to claim the lives of children, accounting for up to 9% of all pediatric fatalities world- wide. The roots of Psydrax schimperiana is traditionally used to treat diarrhea and its fruits are consumed for nutritional purposes in Ethiopia. This study aimed to investigate in vivo antidiar- rheal activity of crude extract and coumarins isolated from the roots of P. schimperiana to pro- vide a pharmacological basis for its traditional use as diarrhea agent and to evaluate the nutri- tional composition and anti-nutritional factors from its fruits. Maceration with 80% methanol was used to prepare the crude extract from the powdered roots of P. schimperiana. The crude roots extract of P. schimperiana was tested for in vivo antidiarrheal efficacy in mice utilizing castor oil-induced diarrhea, gastrointestinal transit time and enteropool- ing models at doses of 100, 200, and 400 mg/kg. Phytochemical investigation of the crude roots extract led to the isolation of two coumarins, isoscopoletin and scoparone. The structures of these compounds were established by interpretation of their spectral data, and by comparison with data reported in the literature. Isoscopoletin and scoparone were evaluated for antidiarrheal activity against castor oil-induced diarrhea model at 10 mg/kg and 20 mg/kg doses. Moisture content, ash value, crude protein, crude fibers, crude fat, phytate, tannin, and oxalate contents of P. schimperiana fruits were determined according to the standard analytical proce- dure. All generated data were analyzed using SPSS software version 26. The crude root extract of P. schimperiana, at doses of 100, 200, and 400 mg/kg, inhibited defe- cation by 37.5%, 46.2%, and 61.2%, respectively. At a dose of 20 mg/kg, scoparone and isosco- poletin reduced defecation by 61.2% and 66.6%, respectively. ii Fruits from P. schimperiana contained 31% fiber, 9.19% crude protein, 12.40% moisture, 6.38% ash, and 0.99% fat. The fruits also contained the anti-nutritional factors phytate (1.16%), oxalate (0.72%), and tannin (22.96%). The study provides a scientific basis for further development and usage of the roots of P. schimperiana, and warrants continued investigation of isoscopoletin and scoparone toward development as a novel treatment for diarrheal diseases. The fruits of P. schimperiana can be considered as a beneficial source of vital nutrients such as carbohydrate, protein, and crude fibers. However, the higher tannin content may interfere with the absorption of essential minerals and inhibit effective utilization of proteins
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    Antidiarrheal Activity of the 80% Methanol Root Extract of Thalictrum ryhnchocarpum Dill. & A. Rich and Its Major Constituent Against Castor Oil- Induced Diarrhea in Mice
    (Addis Abeba University, 2019-12) Feyisa, Kebede; Prof.Asres, Kaleab; Dr.Bisrat, Daniel
    Diarrhea is one of the main causes of infant mortality in Ethiopia and in many other developing countries, causing about 4 to 8 million deaths annually worldwide. Despite recent reductions in morbidity and mortality worldwide, diarrhea still remains one of the leading causes of death in developing countries. Like many other developing countries, people in Ethiopia strongly rely on the therapeutic benefits of traditional medicine to treat diarrhea. One such plant is Thalictrum ryhnchocarpum Dill. & A. Rich. Thus, in the present study, the 80% methanol extract of the root of T. ryhnchocarpum and the compound isolated thereof have been evaluated for their antidiarrheal activity. Phytochemical investigation of the 80% methanol root extract of T. ryhnchocarpum by preparative TLC over silica gel resulted in the isolation of one major alkaloid unequivocally identified as berberine using various spectroscopic techniques, including MS, 13 C-NMR and DEPT spectral data. Both the total extract and berberine were tested for their in vivo antidiarrheal activity on three models namely, castor oil-induced diarrhea, charcoal meal and enteropooling models in mice. It was shown that both the extract and berberine possess significant antidiarrheal activity in a dosedependent manner on all the tested models. Particularly, the root extract showed the maximum activity on castor oil-induced diarrhea model, with 71.4%, 74.0% and 78.0 % (P < 0.01) and berberine displayed even higher activity with 81.0%, 87.6 % and 88.3% at tested concentration of 100, 200 and 400 mg/kg, respectively. Antidiarrheal activity of the root extract and berberine was also noted on the other two models. When administered up to a dose of 2000 mg/kg, neither the root extract nor berberine showed acute toxicity in Swiss albino mice. In view of the present results, it can be concluded that the root extract of T. ryhnchocarpum and berberine could serve for the treatment of diarrhea thereby supporting the traditional claim of the plant against diarrhea.
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    Antidiarrheal and Antibacterial Activity of 80% Methanol Leaf Extract of Gossypium Barbadense L. (Malvaceae) in Mice and on Selected Resistant Pathogenic Strains of Bacteria
    (Addis Ababa University, 2024-12-05) Oumer Mohammed; Zelalem Petros
    Antidiarrheal and antibacterial activity of 80% methanol leaf extract of Gossypium barbadense L. ( Malvaceae) in mice and on selected resistant pathogenic strains of bacteria
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    Antidiarrheal and Antispasmodic Activities of Stephania Abyssinica (Minspermaseae) Used In Ethiopian Traditional Medicine
    (Addis Ababa University, 2010-06) Deneke, Tatek; Engidawork, Ephrem(PhD)
    Diarrhea is a leading cause of morbidity and mortality in developing countries. Diarrhea may result from disturbance in bowel function in which case there is increased bowel transit, excessive intestinal secretion of water and electrolytes, decreased intestinal reabsorptions as well as more frequent defecations of loose, watery stool. Many plant preparations have claimed activities and traditional used as antidiarrhea and antispasmodic. S. abyssinica is traditionally used for treatment of diarrhea and stomachache in Ethiopia. The aim of this work was to evaluate the antidiarrheal and antispasmodic activities of the aqueous and methanol extract of the root and leaf of S. abyssinica. Antidiarrheal activities were studied in mice using castor oil-induced diarrhea at doses of 25, 50,100, and 200 mg/kg body weight. The extracts significantly prolonged the time of diarrheal induction, increased diarrhea free time, reduced the frequency of diarrhea episodes, decreased the weight of stool, and decreased general diarrheal score in a dose dependent way. With dose of 200 mg/kg the extracts produced higher in-vivo antidiarrheal index (ADI) than the reference loperamide. ADI of loperamide, SALM, SALA, SARM and SARA was 77.33, 88.79, 89.21, 91.08 and 82.23, respectively. In Entropooling test in mice the extract significantly (p < 0.01) inhibited intestinal fluid accumulations of mice in a dose dependent fashion; with dose of 100 mg/kg from1.03±0.093 ml of the control to 0.403±0.019ml, 0.210±0.018 ml, 0.494±0.012ml and 0.288±0.026ml by SALM, SARM, SALA and SARA respectively. The antispasmodic activity studies were performed as in vitro and in vivo models. The in-vitro antispasmodic activity studies were performed on isolated GPI. The methanol and aqueous extracts of the leaf showed significant and concentration dependent inhibition of acetylcholine induced contraction of isolated GPI. The extracts depressed Emax of Ach, and decreased PD2 value of the Ach. The Emax of Ach at conc of 10-3M is decreased (from100 for the control group) i viii by SALM with concentration of 200 and 100 ug/ml to 45.6±2.13 and 73.2±3.04 respectively, whereas by SALA with 200 and 100 ug/ml to 62.0±2.98 and 74.8±2.46 respectively. In the in vivo antispasmodic activity test, the extract significantly decreased the peristaltic index (PI). In normal transit test, the PI of SALM, SALA, SARM and SARA with dose of 200 mg/kg was all 0.00 (100% suppression of normal peristalsis). However in castor oil induced transit with dose of 200 mg/kg the peristaltic index (PI) of SALM, SALA, SARM and SARA was 26.67, 36.85, 22.00 and 40.65 respectively. The result of this study indicated that the plant extract possesses antidiarrheal and antispasmodic activities and proves the fact that this plant is used in traditional medicine for treatment of diarrhea, stomachache and abdominal cramp. Key words: S. abyssinica, antidiarrheal, antispasmodic, antienteropooling, aqueous and methanol extract, animal (mice or guinea pig)
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    Antihypertensive Activity of Aerial Parts of Satureja Punctata (Benth.) Briq. (Lamiaceae)
    (Addis Ababa University, 2015-02) Hika, Debabe; Hymete, Ariaya(PhD); Yonathan, Mariamawit(PhD); Mammo, Wendemagegn(Professor)
    Satureja punctata Benth. Briq. (Lamiaceae) locally known as ‘‘Lomishet’’ is among the plants used in Ethiopian traditional medicine for the treatment of various diseases including hypertension. The current study aimed at evaluating the antihypertensive activity of the decoction of the aerial parts of this medicinal plant in guinea model of hypertension and its vasorelaxant effect on isolated aorta. Acute hypertension was induced by surgical procedures involving clamping of the left renal artery and blood pressure was recorded invasively by direct cannulation method from the right common carotid artery. Intravenous administration of the decoction at doses of 10, 20 and 30 mg/kg caused 13.66 ± 0.27, 34.35 ± 0.33, 45.78 ± 0.23% (n=6) fall in (p < 0.01) MABP, respectively, in normotensive guinea pig and a respective fall of 16.02 ± 0.28, 38.52 ± 0.50, 52.07 ± 0.42 % (n=6) (p < 0.01) MABP in renovascular hypertensive guinea pig. The decoction also caused a dose-dependent relaxation of aorta precontracted with KCl at a concentration of 2.5- 40 mg/ml, with a maximum relaxation of 98.19 % achieved at 40 mg/ml. Preparative reversed-phase HPLC analyses of the aerial part decoction of S. punctata resulted in isolation of two phenolic compounds, rosmarinic acid and linarin. The structures of these compounds were elucidated by utilization of spectroscopic techniques, i.e., MS, UV, IR, 1D, and 2D NMR. Further, rosmarinic acid showed significant (p<0.01) reduction of MABP by 8.14 ± 0.27, 15.79 ± 0.33 and 31.78 ± 0.64 % (n = 6) at doses of 0.75, 1.5 and 3 mg/kg, respectively, in normotensive guinea pig. The findings of this study suggest that the aerial parts of S. punctata have genuine antihypertensive activity.
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    Antimalarial activity of the root extract of Lobelia giberroa Hemsl. and its major constituent against Plasmodium berghei infection in mice.
    (Addis Abeba University, 2021-10) Tadege, Getnet; Prof. Hymete, Ariaya; Dr.Tadesse, Solomon
    Lobelia giberroa Hemsl. is an indigenous plant in Ethiopia. Ethiopian traditional healers use its different parts to treat malaria, bacterial and fungal infections, and cancer. For treatment of malaria, in particular, the traditional healers utilize the plant’s root parts. This study was carried out to investigate the antimalarial activity of L. giberroa. The roots of L. giberroa were extracted using 80% methanol and the hydroalcoholic extract was successively fractionated with hexane, ethyl acetate, methanol and water. Chromatographic and spectroscopic methods were used to isolate and identify the active compound from the methanol fraction. Acute oral toxicity study was conducted on the hydroalcoholic extract, solvent fractions, sub-fractions and the isolated compound. The hydroalcoholic extract and the isolated compound were evaluated for antimalarial activity using the standard four-day suppressive method, Rane’s and prophylactic tests in Plasmodium berghei infected albino mice. The solvent fractions and sub-fractions from column chromatography were evaluated for antimalarial activity using four-day suppressive method. The hydroalcoholic extract, solvent fractions, subfractions and the isolated compound were found to be safe at a dose of 2000 mg/kg. The hydroalcoholic extract of L. giberroa root and its methanol fraction exhibited the highest antimalarial activity and significantly increased the mean survival time of the treated mice. In fact, the hydroalcoholic extract exhibited 73.05%, 49.35% and 43.16% parasitemia suppression for four-day suppressive test, Rane's test and prophylactic test, respectively. The methanol fraction demonstrated 64.37% parasitemia suppression for four- day suppressive test. The isolated compound, characterized as lobetyolin, suppressed the level of parasitaemia by 39.96, 53.46 and 68.21% at a dose of 25, 50 and 100 mg/kg, in standard four-day suppressive test, respectively. Mice treated with 100 mg/kg/day lobetyolin survived longer (18.6 days) when compared with negative control group (6.8 days). In conclusion, the current study supports the traditional use of the plant for the treatment of malaria and identified the main active compound lobetyolin, the potential to be an antimalarial lead for further development. The active ingredient, lobetyolin, was also isolated for the first time from the root of Lobelia giberroa. To the best of our knowledge, this is the first report on the biological activity of L. giberroa.
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    Antiprolif-erative Constituents of Roots of Podocarpus falcatus (Thunb.) R.Br. ex Mirb
    (Addis Ababa University, 2015-06) Mekuria, Ermias; Hymete, Ariaya(PhD); Yonathan, Mariamawit(PhD)
    Once thought of as the disease of the developed, cancer nowadays is becoming the prob-lem of every nation across the globe claiming millions of lives every year. Incidence, and thus prevalence, is increasing every year due to adoption of lifestyle factors that are known to be major cancer risk factors. Making things worse is the development of MDR to the known effective anticancer drugs. Moreover, the currently available drugs are cost-ly and are associated with severe side effects. Thus, discovering new anticancer drugs with new and safe modes of action is urgently needed. Natural products derived from medicinal plants are well-known contributors of clinically useful anticancer drugs; suffice to mention taxol, the Vinca alkaloids, podophyllotoxin and camptothecin and their de-rivatives. Relying on traditional medicines for most of their health needs, Ethiopians use various plants for prevention and treatment of cancer. For example, the roots of Podocar-pus falcatus are used as “anticancer” remedies in some parts of Ethiopia, which formed the basis of the present study to isolate the “responsible” “bioactive” compounds. Bioassay guided fractionation using the human colorectal adenocarcinoma (HT-29) cell line of the methanol extract of dried roots of P. falcatus (Podocarpaceae) led to the isola-tion of two new type C nagilactones, 16-hydroxy nagilactone F (PF-1) and 2β,16-dihydroxy nagilactone F (PF-3) and a new totarane-type bisditerpenoid 7β-hydroxy mac-rophyllic acid (PF-2), along with the seven known compounds: inumakinol D (28), mac- rophyllic acid (37), nagilactone D (41), ponasterone A (94), 2β-hydroxy nagilactone F (108), nagilactone I (109), and 15-hydroxy-nagilactone D (110). The structures of the new compounds were determined by 1D and 2D-NMR, HRESIMS and by comparison with the reported spectroscopic data of their congeners. The orientation of the hydroxyl group at C-2 of 108 and 109 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-hydroxy nagilactone F (PF-1) and 2β,16-dihydroxy nagilactone F (PF-3), were the most active (ED50 0.3–5.13 μM range) against the HT-29 cell line, whereas the bisditerpenoids (PF-2 and 37) and the other known compounds 28 and 94 were inactive. The presence of bioactive nagilactones in P. falcatus supports its traditional use.
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    Antiproliferative Activities of Alkaloids from Crinum abyscinicum Hochst. ExA. Rich Bulb Extract
    (Addis Abeba University, 2019-08) Abebe, Besufekad; Prof.Hymete, Ariaya; Dr.Bisrat, Daniel
    Cancers are group of diseases that are distinguished by increased division of cells caused by genetic changes. Globally, it accounted for 9.6 million deaths in 2015 and is increasing to be a public health burden. Yet the treatment of cancer is mainly through chemotherapy that possesses severe toxicities and facing multiple drug resistance. These problems have urged researchers to look for safe and effective chemotherapeutic agents from natural products, especially from plants. Thus, Crinum abyscinicum as one of such plants in Ethiopia that has been used traditionally for treatment of cancer was evaluated for its antiproliferative activity. In vitro antiproliferative activity of the bulb extract of C. abyscinicum was investigated using MTT and resazurine assays on ovarian carcinoma cell line (A2780) and leukemia cell line (MV4-11) respectively. It is noted that the bulb extract possesses antiproliferative activity with GI of 8.289 ± 0.33µg/ml and 20.77 ± 0.354µg/ml against leukemia cell line (MV4-11) and ovarian carcinoma cell line (A2780) respectively. 50 Further analysis of the bulb extract using preparative thin layer chromatography (PTLC) resulted in the isolation of two alkaloids. The structure of the alkaloids were characterized as 6hydroxycrinamine (BCA-1) and lycorine (BCA-2) using spectroscopic methods including HRTOF-MS, 1D-NMR ( 1 H, 13 C-NMR and DEPT) and 2D-NMR (HMBC) spectral data, and by comparison with reported spectroscopic data for the same compounds. Among the isolated compounds, lycorine displayed antiproliferative activity in a dose-dependent manner against MV4-11 and A2780 cell lines with GI of 3.372 ± 0.26733µg/ml and 2.849 ± 0.139µg/ml respectively. Likewise, 6-hydroxycrinamine exhibited activity with growth inhibition of 5.323 ± 0.455µg/ml and 2.925 ± 0.769µg/ml against MV4-11 and A2780 respectively. The activity observed for the bulb extract as well as isolated compounds of C. abyscinicum support the traditional use of the plant against cancer.
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    Antiproliferative Activity of the Leaf Latex of Aloe secundiflora Engl. and its Major Constituents
    (Addis Ababa University, 2023-01) Berie,Yabibal; Tadesse,Solomon( PhD); Ayalew,Hiwot
    Globally, an estimated 19.3 million new cancer cases and almost 10.0 million cancer deaths occurred in 2020. The various methods of treatment of cancer that can be employed alone or in combination, depending upon different factors, are chemotherapy, radiotherapy and surgical interventions. The currently available chemotherapeutic agents have severe toxicities and face multiple drug resistance. This calls for researchers to look for safe and effective chemotherapeutic agents from natural products. Thus, the antiproliferative efficacy of Aloe secundiflora, a plant traditionally used to treat cancer, was evaluated. The antiproliferative activity of A. secundiflora leaf latex was investigated against four cancer cell lines, breast (MCF-7), lung (A427), urinary bladder (RT-4), and cervical (SiSo) using MTT assay. The latex possesses better antiproliferative activity with an IC50 value of 15.3 μg/mL against the A427 cell line over the other three cell lines. Phytochemical analysis of the latex using preparative thin layer chromatography resulted in the isolation of two glycosides and the structure of these two glycosides were characterized as Aloenin B and Aloeresin D using spectroscopic methods, and by comparison with reported spectroscopic data. Aloenin B and Aloeresin D displayed antiproliferative activity against A-427 cell lines with IC50 value of 3.2 and 5.5 μg/mL, respectively. The activity observed for the latex as well as isolated compounds of A. secundiflora support the traditional use of the plant against cancer
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    Antiprotozoal Activity of Extracts and a Major Compound from the Leaves of Ranunculus multifidus Forrsk.
    (Addis Abeba University, 2021-06) Sirak, Betelhem; Asres, Kaleab(Professor)
    Protozoal diseases caused by the genera Leishmania, Plasmodium and Trypanosoma have devastating impact mostly on the poorest countries of the world due to their prevalence, virulence and drug resistance ability. This calls for the development and discovery of new effective and safe chemotherapeutic agents from alternative sources such as medicinal plants. This study aimed at investigating the antiprotozoal activity of Ranunculus multifidus Forrsk. (Ranunculaceae), a medicinal plant used to treat leishmaniasis, malaria and trypanosomiasis in several African countries. Fresh leaves of R. multifidus were subjected to maceration using 80% methanol and hydrodistillation to obtain hydroalcoholic extract (RM-M) and hydrodistilled extract (RM-H), respectively. Antileishmanial activities of the extracts were studied on clinical isolates of the promastigote and amastigote forms of Leishmania aethiopica and Leishmania donovani, whilst 4-day-suppressive, Rane’s and prophylactic tests were employed to investigate in vivo antimalarial activity against chloroquine sensitive Plasmodium berghei infected mice. In vitro and in vivo antitrypanosomal effects of the extracts were also investigated against Trypanosoma congolense field isolate. Results of the study revealed that both extracts were active against the studied protozoans, although RM-H demonstrated superior activity (p < 0.001) compared the RM-M. The IC 50 values of RM-H were 0.490 and 0.984 μg/ml against promastigotes and 1.49 and 1.84 μg/ml against macrophage amastigotes of L. aethiopica and L. donovani, respectively. At a dose of 35.00 mg/kg/day, RM-H demonstrated a chemosuppression value of 70% in 4-day-suppressive test. Furthermore, at a concentration of 4 mg/ml, RM-H ceased motility of T. congolense within 20 min. Further phytochemical analysis of RM-H using preparative thin layer chromatography (PTLC) led to the isolation of an α,β-unsaturated dilactone characterized as anemonin on the basis of FT-IR, APCI-MS, 1D- and 2D-NMR spectral assignments and also by comparison with the reported spectroscopic data of the same compound. Anemonin displayed significant (p < 0.001) antileishmanial activity with IC 50 of 1.33 nM and 1.58 nM against promastigotes and 1.24 nM and 1.91 nM against amastigotes of L. aethiopica and L. donovani, respectively. Anemonin was found to be relatively less toxic to macrophage cells with selectivity indices (macrophage cytotoxic/antileishmanial ratios) of 22 and 14, respectively. In a 4-day suppressive, Rane’s and prophylactic antimalarial tests, anemonin showed median effective doses (ED 50 s) of 2.17, 2.78 and 2.70 μM, respectively. At a concentration of 4 mg/ml, anemonin completely immobilized trypanosomes within 5 min of incubation, while the standard dug diminazene diaceturate immobilized the parasites within 10 min. In the in vivo antitrypanosomal assay, anemonin eliminates parasites at all the tested doses (8.75, 17.00 and 35.00 mg/kg/day) and prevented relapse. Results of the present study provided evidence that the leaves of R. multifidus possess genuine antileishmanial, antiplasmodial and antitrypanosomal activities, which may be attributed to the presence of anemonin. Thus, use of the plant in traditional medicine for the treatment of protozoal diseases seems to be well founded. values
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    Antipsychotic Polypharmacy,Health-Related Quality of Life and Associated Factors among Patients with Schizophrenia: A Cross-Sectional Study at Ayder Comprehensive Specialized Hospital, Northern Et
    (Addis Ababa University, 2024-08-15) Elias Fitsum; Minyahil Alebachew
    Antipsychotic Polypharmacy,Health-Related Quality of Life and Associated Factors among Patients with Schizophrenia: A Cross-Sectional Study at AyderComprehensive SpecializedHospital, Northern Et
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    Appropriateness of Type 2 diabetes mellitus drug therapy: A case of Tikur Anbessa Specialized Hospital Diabetes Clinic
    (Addis Ababa University, 2014-03) Ayele, Alemseged; Engidawork, Epherm(PhD); Yifter, Helen(PhD)
    Background: Diabetes mellitus (DM) is a metabolic problem involving chronically high blood glucose levels or hyperglycemia, which is thought to arise from insulin deficiency. This insulin deficiency can be decrease in amount or a complete absence in body. In the long run high blood glucose level could lead to various complications. Beside altered glucose metabolism carbohydrate, protein, and lipids metabolisms are also affected in diabetes mellitus. Objective: To assess appropriateness of Type 2 diabetes mellitus drug therapy (T2DM) and investigate association between fasting blood glucose (FBG) and the patients’ clinical and demographic characteristics at the diabetes clinic of Tikur Anbessa specialized hospital (TASH). Methods: The study was a cross sectional hospital based survey and used both quantitative and qualitative methods. T2DM patients who came for their follow up treatment at the diabetes clinic of TASH over a one month period (April 2013) were used as research participants. Plus key informant interview with the help of semi-structured open ended questioner was used focusing on the experience and practice physicians within the diabetes clinic regarding medication choice and guidelines they use. Results: A total of 103 patients enrolled in the survey and the proportion of females (59.2%) was higher than males (40.8%). The mean age was 52.2 years and most of them live in Addis Ababa. When it comes to clinical characteristics mean FBG was 155.99 ± 44.32 mg/dl, the difference in FBG between male and female was insignificant (P=0.325). Body mass index (BMI) had a mean value of 26.4± 3.05 kg/m2 and 51.45% of the patients were overweight. Medication wise NPH (56.3%), metformin plus glibenclamide (19.4%) and metformin (10.7%) were the most prescribed drug therapies. And 3.88% of patients were only on glibenclamide. The association of gender, age, BMI and medication used with the FBG levels of patients was not significant with a p value of 0.6, 0.803, 0.97 and 0.081 respectively. The key informants point out that patient load, physician rotation, lack of guide-line and devices as a reason for inadequacy of treatment. Conclusions: The treatment of T2DM is appropriate with existing problems. Metformin was the first choice oral medication, while most patients were on NPH. And no single factor was associated with influencing the FBG of patients. Key Words: Type 2 diabetes mellitus, Drug therapy Acknowledgments
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    Assessment of Drug Therapy Problems and Contributing Factors among Adults Admitted to Tirunesh Beijing General Hospital, Addis Ababa, Ethiopia
    (Addis Abeba univerisity, 2021-11) Ababiya, Tsegaye; Mekuanint, Solomon
    The philosophy of pharmaceutical care (PC) is the sum of responsibilities of the pharmacist to meet all of the patient’s drug-therapy needs through direct patient care and cooperation with other facets of the health care. It is important to avoid drug therapy problems (DTPs) as they may cause morbidity and mortality, reduce quality of life and increase health expenses for the patient and for society. This study aimed to assess DTPs and associated factors among adults admitted to Tirunesh Beijing General Hospital. A prospective cross-sectional study was conducted on 220 adults admitted to medical ward of TBGH. Cippole`s DTPs classification system was used for identification, intervention and documentation of DTPs. Thirty-eight percent of patients encountered at least one DTP and 298 DTPs were identified in 177 patients (104 males and 73 females) with prevalence of 80%. Out of 1467 drugs prescribed, 62 drugs were significantly associated with the occurrence of DTPs. ‘‘Needs additional drug therapy” (36.9%), was the most frequently identified DTPs followed by ‘‘inappropriate dose’’ (19.8%) and “noncompliance” (19.5%). Hospital stay more than seven days (AOR=3, 95% CI:1.394-5.843; p=0.004) and polypharmacy (AOR=2, 95% CI: 1.168-5.287; p=0.019) were potential risk factors for the occurrence of DTPs. In conclusion, there is high prevalence of DTPs, with the most frequent one being needs additional drug therapy followed by inappropriate drug therapy and noncompliance. Polypharmacy and number of hospital stay were potential risk factors for the occurrence of DTPs. In recommendation, all stake holders should work in collaboration to combat drug therapy problems as it poses harm and poor quality life to patients and great attention should be given for those drugs which are associated with the occurrence of DTPs.
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    Assessment of Knowledge, Attitude and Practices on Adverse Drug Reaction Reporting among Pharmacy Personnel Working at Community Pharmacy, Addis Ababa, Ethiopia
    (Addis Ababa University, 2015-05) Goshime, Alaynesh; Gedif, Teferi (PhD)
    Assessment of Knowledge, Attitude and Practice on Adverse Drug Reaction Reporting among Pharmacy Personnel Working at Community Pharmacy, Addis Ababa, Ethiopia Alaynesh Goshime Addis Ababa University, 2015 Modern medicines have changed the way in which diseases are managed and controlled. However, despite all their benefits, evidence continues to mount that adverse drug reactions (ADRs) are common cause of illness, disability and even death. Knowledge, attitude and practices of health professionals towards ADR reporting are known to have crucial contribution in the detection and reporting of the reactions. A cross sectional study was conducted on a sample of 379 pharmacy personnel working at randomly selected community pharmacies of Addis Ababa to assess their knowledge, attitude and practice towards ADR reporting. Data was collected using self administered questionnaire. Majority of the respondents were male (57.5%) and in the age group 26-30 (55.1%). Over half (70.7%) of the respondents had poor knowledge. One hundred seventy three (45.6%) participants encountered ADRs in the past 12 months but none of them reported to the relevant authority. The majority of respondents (82.8%) had a positive attitude towards ADRs reporting. The study revealed that majority of pharmacy personnel at community pharmacy in Addis Ababa had poor knowledge, positive attitudes and very limited practices towards ADR reporting. The Ethiopian Food, Medicine and Health Care Administration and Control Authority should create awareness iv on the existence of ADR monitoring system and the purpose and importance of ADR reporting and should also conduct continuous trainings and seminars about ADR reporting with community pharmacies dispensers and finally ADR reporting forms should be made available at community pharmacies. Keywords: Pharmacovigilance , ADR reporting, Community Pharmacy Personnel, Knowledge, Attitude, Practice
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    Assessment of Microbial and Food Safety Knowledge, Attitude and Practice among Food Handlers in Hotels / Restaurants in Woldia Town, North Wollo, Ethiopia
    (Addis Ababa University, 2025-02-23) Mekuriaw Melesse; Ashagrie Zewudu
    Insufficient knowledge, attitude and practices with respect to food safety can contribute to the outbreaks of food borne illness. Most foods, to include meat, legume and vegetable based sauces, could be vulnerable to food borne pathogens. More specifically, there is an association of inadequate Knowledge, negative attitudes and poor practices on food hygiene, with hygienically unsuitable condition, and unfit food handling practices