Pharmacognosy

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Quality Assessment of Common Antimalarials Marketed in Gambella National Regional State, South Western-Ethiopia.
(Addis Ababa University, 2023-06-15) Ahmed, Feruza; Ashenef, Ayenew
Over the past years, there has been a growing alarm that a considerable amount of antimalarial supply in the underdeveloped world particularly in the private sector, is of poor quality. According to a WHO research, poor quality antimalarials are common in malaria-endemic locations, with 1 in 10 drugs allegedly being either substandard or falsified and one-third of antimalarial drugs from these regions failing chemical content examination
Cytotoxicity of latex of Synadenium compactum var. rubrum S. Carter
(Addis Ababa University, 2023-02) Redae,Aynalem; Yeshak, Mariamawit Yonathan(PhD)
Cancer has become the second leading cause of death globally. While it was once predominately a disease affecting economically developed countries, it is now impacting developing nations more accounting for over half of all new cases worldwide. This has significant social and economic implications for countries like Ethiopia. One of the major drawbacks in treating cancer is the prevalence of drug resistance, along with the unbearable side effects and high costs associated with current treatments. Therefore, there is an urgent need to discover new, safe and effective drugs to combat this advancing disease. Natural products have proven to be a valuable source for the development of cancer drugs, as they make up over half of the currently used drugs. Traditional medicine attends to almost 80% of population’s primary health needs in Ethiopia. In this research, traditionally claimed cytotoxic latex and its fractions from Synadenium compactum var. rubrum S. Carter, a member of the Euphorbiaceae family, were evaluated for their cytotoxic activity. The latex and its ethyl acetate fraction showed potent cytotoxicity in an MTT assay against the ovarian cancer cell line A2780, with GI50 values as low as 1.98 ± 0.45 μl/ml and 0.911± 0.296 μl/ml, respectively. Additionally, the sub-fractions of the ethyl acetate fraction showed potent activity against histiocytic human lymphoma cell line U-937 in a Fluorometric microculture cytotoxicity assay (FMCA), with an SI value as low as 8% at a dose of 100 μl/ml. Through bioassay guided fractionation and preparative HPLC, a previously reported lathyrane diterpenoid known as 2-methylbutanoate tetraacetate synadenol was isolated from the most active ethyl acetate sub fraction. The structural elucidation of the compound was achieved using 1H NMR, 13C NMR, HMQC, HMBC and HRESIMS spectroscopic techniques. The finding of this study strongly supports the antitumor traditional claim of the latex of S. compactum.
In vitro Antileishmanial and Molecular Docking Studies of a Sesquiterpene Lactone from Cirsium dender Friis (Asteraceae)
(Addis Ababa University, 2023-10) Samuel,Aklilu; Tadesse,Solomon(PhD)
Leishmaniasis caused by genus of Leishmania has impact on the Africa and Asian countries due to high prevalence, resistance to current therapy and unavailability of standard medicine for the treatment. Asteraceae plants (a family widely used in folk medicine worldwide) are emerging as an interesting source for new leishmanicidal compounds and this study was aims to extract and isolate active metabolite from the root of Cirsium dender Friis (Asteraceae) to study molecular docking and to investigate in vitro antileishmanial activity against promastigote and amastigote forms of L. aethopica and L. donovani. Air dried roots of the plant was macerated with 80% methanol which resulted in 9.98% brown methanol extract. Phytochemical analysis was investigated by using thin layer and preparative chromatography which result in isolation of a white crystalline compound named AS01. Characterization of AS01 on the basis of APCI-MS, 13CNMR and 1HNMR spectral assignments and by comparing with reported data of the compound the AS01 was identified as dehydrocostus lactone. Antileishmanial activity of the extract and dehydrocostus lactone was studied on clinical isolates of L. aethopica and L. donovani and the IC50 of the dehydrocostus lactone was 24.33μ/mL, 12.35 μ/mL against promastigote and 12.54 μ/mL, 3.29 μ/mL against amastigote of L. aethopica and L. donovani respectively. The compound dehydrocostus lactone and the crystalline ii structure of pteridine reductase1 (PDB ID: 2XOX) extracted from L.donovani, which is a potential target for drug development against Leishmania, underwent a molecular docking study using the autodock vina and Pymol visualization tools. The result of the study discloses that the compound dehydrocostus lactone has antileishmanial activity and it has binding affinity to docking site of pteridine reductase1 enzyme.
n vivo Antidiarrheal and Molecular Docking Studies of a Coumarin from the Root Extract of Impatiens ethiopica Grey-Wilson (Balsaminaceae)
(Addis Ababa University, 2023-11) Yimer,Sileshi; Bisrat,Daniel(PhD); Tadesse,Solomon(PhD)
Diarrhea continues to be a major health problem worldwide, particularly in developing countries like Ethiopia. In Ethiopia, as in many other developing nations, traditional medicine plays a significant role in healthcare, with people relying on the therapeutic properties of plants to treat various infectious diseases. One such plant is Impatiens ethiopica, a member of the Impatiens genus traditionally used for the treatment of diarrhea. Thus, the present study was aimed to investigate the potential antidiarrheal effects of 80% hydroalcoholic root extract of I. ethiopica and its major constituents using both in vivo models integrated with molecular docking studies. Three experimental models, such as intestinal transit, intestinal secretion and castor oil-induced mice models, were employed to determine the effects of the root extract, fractions, and the isolated compound. The findings of the study revealed that the root extract significantly reduced the frequency of defecation, the weight of feces, and the onset of diarrhea at 100 mg/kg, 200 mg/kg, and 400 mg/kg. Additionally, the root extract exhibited significant reduction in intestinal fluid accumulation and gastrointestinal (GI) motility. The active root extract was then divided into four fractions based on solubility-based fractionations, utilizing successively petroleum ether, chloroform, methanol, and water solubility as the basis for separation. Of these fractions, the methanol and water fractions demonstrated a dose-dependent antidiarrheal effect, with the methanol fraction exhibiting the highest activity at a dose of 400 mg/kg. Further fractionation of ii the active methanol fraction by normal-phase column chromatography led to the isolation a coumarin, coded as SY-1. The structure of SY-1 was identified as 7-hydroxy-6- methoxycoumarin (7-hydroxy-6-methoxy-2H-chromen-2-one), commonly known as scopoletin, on the basis of various spectroscopic techniques (ESI-MS, 1H-NMR, 13C-NMR and DEPT-135 spectral data). The antidiarrheal effects of scopoletin were also evaluated, demonstrating a significant reduction in intestinal fluid accumulation and gastrointestinal (GI) motility at the doses of 10 mg/kg, 20 mg/kg and 40 mg/kg. In this study, prostaglandin synthase (PGS) was chosen as a target for molecular docking analysis. Assessing scopoletin interaction with prostaglandin synthase (PGS) (COX-2; PDB ID: 4COX) revealed a promising docking score of −7.941 kcal/mol. Scopoletin demonstrated a strong binding affinity, engaging in hydrogen bonding with SER530 and pi-pi stacking interactions with TYR385 and TRP387, at specific COX-2 binding sites. These findings highlight that the antidiarrheal-like activity of I. ethiopica was partly attributed due to the presence of scopoletin. Overall, these results provide validation for the traditional use of I. ethiopica roots in the treatment of diarrhea and highlight the potential of scopoletin as antidiarrheal compound.
In vivo Antidiarrheal Activity of the Extracts and a Major Compound Isolated from the Roots of Sida ovata Forssk
(Addis Ababa University, 2024-02-15) Tesfa Begashaw; Kaleab Asres
In vivo Antidiarrheal Activity of the Extracts and a Major Compound Isolated from the Roots of Sida ovata Forssk
Synthesis, In vitro Antimicrobial and In silico Studies of Betti Base Derivatives of 2-Naphthol
(Addis Ababa University, 2024-02-11) Frehiwot Beyene; Daniel Bisrat
Synthesis, In vitro Antimicrobial and In silico Studies of Betti Base Derivatives of 2- Naphthol.
Comparative in Vitro Availability of Some Locally Manufactured and Imported Bcs Class II Drug Products Against their Innovator/Counter Reference Products
(Addis Ababa University, 2024-05-05) Habtamu Bulbula; Tsige Gebre
According to the Biopharmaceutical classification system (BCS), active pharmaceutical ingredients (APIs) are classified into four (BCS Class I-IV) based on aqueous solubility and intestinal permeability. BCS Class II drug products are medicines which have low solubility in body fluids and high permeability through membranes and they are among the drug products that require documented evidence of bioequivalence study. In addition to the solubility problems, there may be differences between generic and innovator products in terms of the type, source, and quantity of ingredients, manufacturing methods and processes, and machineries used in the production, and these factors can bring major differences in dissolution and bioavailability. The objective of this study is therefore to compare in vitro availability of four types of locally manufactured and imported BCS Class II drug products namely two types of macrolide antibiotics, Azithromycin (AZM) 500mg and clarithromycin (CLM) 500mg tablets, atorvastatin (ATO) 40mg tablets (anti-hyperlipidemia) and glibenclamide (GLB) 5mg tablets (oral hypoglycaemic agent) against their innovator/counter comparator products. A total of 21 selected drug products and their comparator counter products were collected from different drug retail outlets in Addis Ababa. For each drug product, quality control parameters such as thickness, and diameter, were determined in house pre-determined standards (Manufacturer’s specifications), and the hardness, weight variation, friability and disintegration time were determined according to USP monograph using appropriate analytical equipment. The assay and dissolution profile of each drug product were also determined as per their respective procedures in the official monograph using high-performance liquid chromatogram (HPLC) and UV/Vis spectrophotometer. All quality control parameters were assessed by a one-way analysis of variance (ANOVA). Statistically, a significant difference was considered when
Synthesis, in vitro Antimicrobial Activity and in silico Studies of Schiff Base Derivatives of Isonicotinic Acid Hydrazide
(Addis Ababa University, 2024-02-16) Mulugeta Ayele; Daniel Bisrat
Synthesis, In vitro Antimicrobial Activity and In silico Studies of Schiff Base Derivatives of Isonicotinic Acid Hydrazide
Investigation of in vivo Analgesic and Anti-inflammatory Activities of 80% Methanol Extract of Grewia feruginea Bark, Identifying its Essential Oil Chemical Composition and In Silico Analysis of the Major Constituent
(Addis Ababa University, 2024-02-15) Yared Yibeltal; Solomon Tadesse
Investigation of In vivo Analgesic and Anti-inflammatory Activities of 80% Methanol Extract of Grewia feruginea Bark, Identifying its Essential Oil Chemical Composition and In Silico Analysis of the Major Constituent
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.
Isolation and Characterization of a Pregnane Steroid from the Antiproliferative Active Extract of Caralluma speciosa (N.E.Br.) N.E.Br. Stem Latex
(Addis Ababa University, 2024-05) Derese,Kalkidan; Asres,Kaleab(PhD); Bisrat,Daniel(PhD)
Cancer is a broad term for a large diverse group of diseases that can affect any body part, standing as one of the leading global causes of death. In response to the challenges posed by cancers, researchers are actively investigating natural alternatives, specifically plant-derived compounds, seeking safer and more effective chemotherapeutic options to address the limitations of current treatments. In the traditional medical practices of Ethiopia, the stem latex of Caralluma speciosa (N.E.Br.) N.E.Br. stands for its traditional use in treating cancer. Thus, this study aimed at evaluating the antiproliferative activity of the latex and isolating its constituents. In vitro crystal violet cell proliferation assay was used to determine the antiproliferative/cytotoxic activity of the 80% methanolic extract of C. speciosa against four cancer cell lines. The latex extract exhibited cytotoxic effects against breast cancer cell line (MCF-7) and normal cervical cancer cell line (SiSoN) with Treated versus Control corrected percentage [(T/C)corr. (%)] values of -1.07 and - 0.95, respectively. Additionally, the latex demonstrated antiproliferative effects on lung cancer cell line (A427) and cervical cancer cells resistant to cisplatin (SiSoR) with (T/C)corr. (%) values of 0.43 and 1.07, respectively. Subsequently, a pregnane glycoside was isolated from the 80% methanol extract of the latex using chromatographic techniques including HPLC. The structure was tentatively identified as 20-O-benzoyl-12-O-acetyl-14-hydroxy-20-pregn-5-ene-3-O- -D- cymaropyranosyl-(1→4)- -D-canaropyranosyl-(1→4)- -D-glucopyranoside through 1D and 2D NMR spectral data. Although the antiproliferative activity of the isolated compound was not determined, considering the reported anticancer activity of pregnane glycosides, it was evident that the isolated compound could have contributed to the antiproliferative/cytotoxic activity of latex of C. speciosa. The present findings also support the traditional use of the plant for the treatment of cancer.
In vivo Antidiarrheal Activity of the Extracts and a Major Compound Isolated from the Roots of Sida ovata Forssk
(Addis Ababa University, 2024-02) Begashaw,Tesfa; Asres, Kaleab (Prof.); Bisrat, Daniel (PhD)
Diarrhea is a common health issue often dealt with traditional remedies, especially in developing countries, where medicinal plants are frequently used. Sida ovata Forssk (Malvaceae) is a medicinal plant used in Nigerian folkloric medicine for the treatment of diarrhea, and in Ethiopia it is employed for managing various disorders including inflammation, wound and skin infection. However, despite its traditional uses, there is a lack of scientific evaluation regarding its claimed activities. This study aimed to assess the antidiarrheal activities of the 80% MeOH extract of S. ovata root and its major constituent using mice models. The hydroalcoholic extract was obtained by macerating the roots of S. ovata in 80% MeOH. The extract was subjected to solvent fractionation and isolation, which led to the isolation of a sterol tentatively identified as stigmasterol. Structural elucidation of the isolated compound was carried out by spectroscopic techniques (1H- and 13C-NMR). The antidiarrheal activity of the total extract, solvent fractions, and the isolated compound was assessed using castor oil-induced diarrhea, castor oil-induced enteropooling, and castor oil-induced gastrointestinal motility tests. Acute toxicity test results of this study indicated that the 80% MeOH root extract of S. ovata was safe by oral route up to a dose of 2000 mg/kg. Oral dose levels of 100, 200, and 400 mg/kg were used for the crude extract and solvent fractions, whilst doses of 25, 50, and 100 mg/kg were employed for the isolated compound. Similarly, the isolated compound appeared to be safe at the maximum dose tested (100 mg/kg). In vivo antidiarrheal index of the 80% MeOH extract and solvent fractions of S. ovata roots increased in a dose dependent manner. The highest antidiarrheal index was observed at the maximum dose of the test substances. Among the solvent fractions, the MeOH fraction showed the highest antidiarrheal index at all dose levels, although these values are less than that of the 80% MeOH extract. Stigmasterol produced dose-dependent antidiarrheal indices with the maximum effect at 100 mg/kg. In conclusion, the present study provided evidence that the roots of S. ovata possess genuine antidiarrheal activity supporting the folkloric assertion of the plant.
Chemotherapy-Induced Toxicities, Clinical Outcomes and Associated Factors among Patients with Gastrointestinal Cancer in two Tertiary Care Hospitals, Addis Ababa, Ethiopia
(Addis Ababa University, 2025-02-23) Samson Fisseha; Minyahil Alebachew
Gastrointestinal tract cancers are the leading cause of cancer-related death worldwide. Chemotherapy remains a cornerstone of treatment, and it is often associated with various toxicities. However, there is a lack of data that shows the prevalence of chemotherapy-induced toxicity, clinical outcomes, and associated factors among patients with gastrointestinal tract cancer in Addis Ababa, Ethiopia
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
Nematicidal Activity of the 80% Methanol Extract and Major Compounds Isolated from the Unripe Fruits of Peponium vogelii (Hook. f.) Engl.
(Addis Ababa University, 2022-04-12) Mohamed Israel; Asres Kaleab
Helminthiasis remain a major public health problem affecting an estimated 1.45 billion individuals worldwide, particularly in tropical developing countries. The aim of this study was to investigate the nematicidal activity of 80% methanol extract of unripe fruits of Peponium vogelii Hook. f. Engli. (Cucurbitaceae), a medicinal plant used to treat intestinal parasite infection in Southwest Ethiopia, and determine the compounds responsible for activity using bioassay-guided fractionation. 80% methanol extract of unripe fruit of P. vogelii was first fractionated by using solvents of different polarity followed by a silica gel column chromatography and reverse phase HPLC, while nematicidal assay was followed throughout on Caenorhabditis (C.) elegans as a model organism. Results of the study revealed that the 80% methanol extract of the unripe fruits of P. vogelii was active against C. elegans (p < 0.001) with an IC50 value of 23.5 μg/ml. Bioassay-guided fractionation led to the isolation of five active components designated PVMF2-4, PVMF2-5, PVMF2-7, PVMF2-8, and PVMF2-9, which exhibited percentage inhibition of 84%, 96%, 97%, 89% and 41%, respectively. Based on spectroscopic data (1H and 13C NMR and ESI-MS), PVMF2-8 and PVMF2-8 which were active and major components from active fraction were identified as linoleic acid and palmitic acid respectively. The results support the use of P. vogelii unripe fruits for the treatment of intestinal parasite infection by traditional healers in Southwest Ethiopia.
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
Post-marketing Quality Surveillance of Selected Antibacterial Agents Marketed in Setit Humera and west Gondar Zones, North West Ethiopia.
(Addis Ababa University, 2023) Denekew,Tewodros; Ashenef,Ayenew(Ass.Prof.); Eticha,Tadele(Ass.Prof.)
Background: The presence of low-quality medicines is becoming increasingly problematic in many parts of the world, particularly in developing countries. Antibiotics are among the most common anti-infective medicines that are falsified. Objective: The purpose of this study was to assess the quality of selected antibacterials that are marketed in Setit Humera and west Gondar Zones, North West Ethiopia. Methods: Seventy-one samples of the antibacterials were collected from six sites in Setit Humera and west Gondar Zones, North West Ethiopia. A mystery shopper collection system was used for sample collection. Visual inspection and confirmation of the registration status were carried out using the WHO/FIP/USP checklist and the EFDA's MRIS database, respectively. Then Pharmacopeial methods (USP, BP) were employed to assess the physicochemical parameters. Results: From 71 samples, 25.35% (18/71) were not registered and 15.49% (11/71) were registered but the license period was expired i.e not in line with the EFDA’s specification. Some (74.65% (53/71) observed samples) did not meet the visual inspection criteria outlined in the joint WHO/FIP/USP checklists. The physicochemical evaluation showed that all the samples studied met the quality specification with respect to the identification and hardness test. From 71 samples tested with regard to assay, dissolution, uniformity of dosage units, disintegration and friability tests, 27.49% (23/71), 16.9%, and 14.08% (10/71), 2.82% (2/71) and 8.57% (3/35) of samples were found to be substandard respectively. Overall, 56.33 % (40/71) of the samples tested were of poor-quality. Conclusion: The results indicated that some (56.33 %) antibacterial medicines circulating in the market did not meet the required quality. Therefore, the regulatory body (EFDA) should focus on enforcing the necessary measures to ensure that antibacterial drugs on the market meet the required mandatory standards
Quality Assessment of Antimicrobial Drugs: Amoxicillin Capsules, Amoxicillin + Clavulanate, Ciprofloxacin and Norfloxacin Tablets from Drug Retail Outlets of Selected Cities in Eastern Ethiopia.
(Addis Ababa University, 2023) Anjulo,Hailu; Ashenef,Ayenew (Assist. Prof.); Hymete,Ariaya(Prof.)
Rising incidence of substandard and falsified antimicrobial drugs is an increasing concern in developing nations. The beta-lactams and fluoroquinolones are among the broad-spectrum antimicrobial agents that are most frequently prescribed, inexpensive, and readily available in Ethiopia, for the treatment of infectious diseases. The consumption of substandard and/or falsified antimicrobial drugs has the potential to result in treatment failure, emergence and development of Antimicrobial resistance (AMR), and ultimately patient mortality. The objective of this study is to assess the quality of four commonly used antimicrobials (ciprofloxacin, norfloxacin, and amoxicillin and its combination with clavulanic acid) marketed in Dire Dawa and Jijiga cities, and Togo-Wuchale town with high potential for illegal drug trade in Ethiopia due to porous border through Somaliland. A total of 54 different brands/products of amoxicillin, amoxicillin plus clavulanic acid, ciprofloxacin, and norfloxacin formulations were collected covertly from 43 facilities using a convenience sampling strategy from March 16 to March 29, 2022, from the selected locations. The samples were first screened using GPHF-minilab protocol and then analyzed with references to USP and BP methods. The quality evaluation showed that 14.28% (6/42) of all samples failed the GPHF-minilab screening test quantitatively, 27.27% (6/22) of amoxicillin samples failed weight variation test, and 22.73% (5/22) of amoxicillin and 40% (2/5) of amoxicillin/clavulanate products failed to meet the assay test. Furthermore, 12.96% of the samples failed the dissolution test. Overall, 22.22% of the products analyzed did not meet pharmacopoeial specifications. Additionally, 56.25% of amoxicillin samples, 60% of amoxicillin/clavulanate, 20% of ciprofloxacin, and 54.54% of norfloxacin samples were found to be pharmaceutically inequivalent with their respective comparator products in relation to dissolution profile studies. The study had shown that the quality of essential antimicrobial medicines in eastern Ethiopia is substandard. This affirms the need for regular post-market surveillance to inform on the situation of antibiotic quality in eastern Ethiopia. Based on the accumulated evidence regulatory actions and mechanisms had to be also in place to circumvent the challenge
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
Synthesis, Antibacterial Activity and Insilco Studies of 1-(2- ethyl acetate)-2-styryl 5-nitroimidazole Derivatives.
(Addia Ababa University, 2023-05) Aragaw,Misgana; Tadesse,Solomon(PhD); Bisrat,Daniel(PhD); Abebayehu,Mekonnen(PhD)
The proliferation of drug-resistant microorganisms that have acquired new resistance mechanisms contributes to the development of antimicrobial resistance. For more than 60 years, metronidazole (2) has served as an antibacterial and antiprotozoal agent. However, its prolonged usage has resulted in drug-resistance and associated with adverse effects. Metronidazole is usually not effective on Gram-negative and Gram- positive facultative anaerobic bacteria, which are considered as the most life- threatening pathogens. However, there are reports of metronidazole analogues with potent activity against the facultative anaerobic bacteria indicate that there is a different mode of action of metronidazole. As a result, it is important to synthesize new metronidazole analogs with unique mode of action in order to enhance the antibacterial efficacy of metronidazole while reducing toxicity. Recent studies have shown that the enzyme FabH (β-ketoacyl-acyl carrier protein synthase III), responsible for the first step of fatty acid biosynthesis (FAB), is a promising target for nitroimidazole derivatives that can be used as an effective anti-infective. In this study, we synthesized four 2-styryl 5-nitroimidazoles derivatives, via condensation of metronidazole with respective benzaldehydes and subsequent acetylation reactions. The chemical structures of the synthesized compounds were determined through 1H and 13C-NMR spectroscopy. We evaluated the antimicrobial activity of the synthesized compounds against six bacterial strains, three Gram- positive bacterial strains (S. aureus, S. epidermidus and S. agalactiae) and three Gram-negative bacterial strains (E. coli, P. aeruginosa and K. pneumoniae) using a two-fold serial dilution MTT assay. Of all the synthesized compounds, compound 33, ((E)-2-(5-nitro-2-styryl-1H-imidazol-1- yl)ethyl acetate) and 36, ((E)-2-(2-(4-(dimethylamino)styryl)-5-nitro-1H-imidazol-1- yl)ethyl acetate) equally demonstrated the most potent antibacterial activity against S. agalactiae (MIC = 1.56 μg/mL), P. aeruginosa (3.13 μg/mL), respectively. Additionally, compound 33 and 36 also exhibited potent activity against K. pneumonia, with an MIC value of 6.25 μg/mL and 12.5 μg/mL, respectively. Molecular docking studies revealed that both compounds have favorable hydrophobic and electrostatic interactions with conserved residues in the binding site of E. coli FabH -CoA complex (1HNJ.pdb). Overall acetylation of 2-styryl-5-nitroimidazoles improved both their biological activity and binding interaction with the target protein.

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