Anticholinesterase and Antioxidant Activities of Spilanthes filicaulis Whole Plant Extracts for the Management of Alzheimer’s Disease
- Elufioye, Taiwo O., Unachukwu, Cynthia C., Oyedeji, Adebola O.
- Authors: Elufioye, Taiwo O. , Unachukwu, Cynthia C. , Oyedeji, Adebola O.
- Date: 2019
- Subjects: Alzheimer’s disease , Cholinesterase inhibitors , Antioxidants , Spilanthes , Flavonoids , Phenolic
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/11260/6534 , vital:46450 , xlink:href="https://10.2174/1573408015666190730113405"
- Description: Background: Spilanthes filicaulis is a tropical herb implicated as a memory enhancer in ethnomedicine. Objective: The study investigated acetyl/butyryl cholinesterase inhibitory and antioxidant activities of different extracts of S. filicaulis whole plant and correlated them to its phytochemical constituents. Methods: The powdered whole plant was successively extracted with n-hexane, ethyl acetate and methanol. Acetyl cholinesterase (AChE) and Butyryl cholinesterase (BuChE) inhibitory activity were evaluated by Ellman colorimetry assay. Antioxidant activity was tested using 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, ferric reducing power and nitric oxide scavenging assays. Total phenolic, flavonoid and tannin were estimated using standard methods. Correlation was determined using Quest Graph™ Regression Calculator. Results: Various extracts exhibited concentration-dependent AChE and BuChE inhibitory activity with ethyl acetate extract being the highest with IC50 of 0.77 μg/mL and 0.92 μg/mL for AChE and BuChE respectively. The ethyl acetate extract also showed the highest reducing power when compared with the other extracts. The methanol extract had slightly higher phenolic and flavonoid content and showed the highest DPPH radical scavenging effect. DPPH scavenging, AChE and BuChE inhibition had high correlation with the total flavonoid content with R2 values of 1.00, 0.800 and 0.992 respectively while nitric oxide scavenging had high correlation with phenolics and tannins with R2 = 0.942 and 0.806 respectively. Conclusion: These results show that the extracts of the whole plant of S. filicaulis possess significant AChE/BuChE inhibitory and antioxidant properties, mostly due to its flavonoid content, suggesting the possible use of the plant in neurodegenerative diseases such as AD.
- Full Text:
- Authors: Elufioye, Taiwo O. , Unachukwu, Cynthia C. , Oyedeji, Adebola O.
- Date: 2019
- Subjects: Alzheimer’s disease , Cholinesterase inhibitors , Antioxidants , Spilanthes , Flavonoids , Phenolic
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/11260/6534 , vital:46450 , xlink:href="https://10.2174/1573408015666190730113405"
- Description: Background: Spilanthes filicaulis is a tropical herb implicated as a memory enhancer in ethnomedicine. Objective: The study investigated acetyl/butyryl cholinesterase inhibitory and antioxidant activities of different extracts of S. filicaulis whole plant and correlated them to its phytochemical constituents. Methods: The powdered whole plant was successively extracted with n-hexane, ethyl acetate and methanol. Acetyl cholinesterase (AChE) and Butyryl cholinesterase (BuChE) inhibitory activity were evaluated by Ellman colorimetry assay. Antioxidant activity was tested using 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging, ferric reducing power and nitric oxide scavenging assays. Total phenolic, flavonoid and tannin were estimated using standard methods. Correlation was determined using Quest Graph™ Regression Calculator. Results: Various extracts exhibited concentration-dependent AChE and BuChE inhibitory activity with ethyl acetate extract being the highest with IC50 of 0.77 μg/mL and 0.92 μg/mL for AChE and BuChE respectively. The ethyl acetate extract also showed the highest reducing power when compared with the other extracts. The methanol extract had slightly higher phenolic and flavonoid content and showed the highest DPPH radical scavenging effect. DPPH scavenging, AChE and BuChE inhibition had high correlation with the total flavonoid content with R2 values of 1.00, 0.800 and 0.992 respectively while nitric oxide scavenging had high correlation with phenolics and tannins with R2 = 0.942 and 0.806 respectively. Conclusion: These results show that the extracts of the whole plant of S. filicaulis possess significant AChE/BuChE inhibitory and antioxidant properties, mostly due to its flavonoid content, suggesting the possible use of the plant in neurodegenerative diseases such as AD.
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Correlation of Total Phenolic, Flavonoid and Tannin Content of Bryophyllum pinnatum (Lam.) (Crassulaceae) Extract with the Antioxidant and Anticholinesterase Activities
- Elufioye, Taiwo O, Olusola, Damilare M, Oyedeji, Adebola Omowunmi
- Authors: Elufioye, Taiwo O , Olusola, Damilare M , Oyedeji, Adebola Omowunmi
- Date: 2019
- Subjects: Cholinesterase inhibitors , Antioxidants , Bryophyllum pinnatum
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/11260/1536 , vital:37776 , https://doi.org/10.5530/pj.2019.11.158
- Description: Bryophyllum pinnatum is a perennial herb used in traditional medicine against varieties of ailments such as memory disorder. This study quantitatively estimated the total phenolic (TPC), total flavonoid (TFC) and total proautocyanidin (TPA) contents of extract and fractions of B. pinnatum and correlated them with its antioxidant and anticholinesterase activities. Methanolic extract of the dried leaves was partitioned into n-hexane, ethyl acetate and aqueous fractions. Total phenolic, flavonoids and proanthocyanidins content were estimated as gallic acid or quercetin equivalents. DPPH and nitric oxide scavenging activity as well as ferric reducing power assays were used to evaluate antioxidant activity, using 2,6-di-tert-butyl4-methylphenol (DDM) and ascorbic acid as standards. In vitro anticholinesterase activity was evaluated by Ellmann’s colorimetry assay with phsiostigmine (serine) and donepezil as positive control. The crude methanol extract had the highest phenolic, flavonoid and tannin content. The ethyl acetate fraction had the highest DPPH radical scavenging effect (IC50 0.004 mg/ml) while the aqueous fraction had the highest NO scavenging and ferric reducing effects with values of IC50 0.012 mg/ml and 0.007 mg/ml respectively. The ethyl acetate fraction had the best cholinesterase inhibitory effect (IC50 0.951 µg/ml AChE; 3.546 µg/ml BuChE). DPPH radical scavenging effect correlated strongly with total phenolic, flavonoids and proautocyanidins (r2 0.896, 0.651 and 0.619 respectively) while ferric reducing power showed weak correlation and NO scavenging as well as AChE inhibition had no correlation. The study shows DPPH radical scavenging could be due to the phenolic content while other class of compounds are responsible for the cholinesterase inhibition.
- Full Text:
- Authors: Elufioye, Taiwo O , Olusola, Damilare M , Oyedeji, Adebola Omowunmi
- Date: 2019
- Subjects: Cholinesterase inhibitors , Antioxidants , Bryophyllum pinnatum
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/11260/1536 , vital:37776 , https://doi.org/10.5530/pj.2019.11.158
- Description: Bryophyllum pinnatum is a perennial herb used in traditional medicine against varieties of ailments such as memory disorder. This study quantitatively estimated the total phenolic (TPC), total flavonoid (TFC) and total proautocyanidin (TPA) contents of extract and fractions of B. pinnatum and correlated them with its antioxidant and anticholinesterase activities. Methanolic extract of the dried leaves was partitioned into n-hexane, ethyl acetate and aqueous fractions. Total phenolic, flavonoids and proanthocyanidins content were estimated as gallic acid or quercetin equivalents. DPPH and nitric oxide scavenging activity as well as ferric reducing power assays were used to evaluate antioxidant activity, using 2,6-di-tert-butyl4-methylphenol (DDM) and ascorbic acid as standards. In vitro anticholinesterase activity was evaluated by Ellmann’s colorimetry assay with phsiostigmine (serine) and donepezil as positive control. The crude methanol extract had the highest phenolic, flavonoid and tannin content. The ethyl acetate fraction had the highest DPPH radical scavenging effect (IC50 0.004 mg/ml) while the aqueous fraction had the highest NO scavenging and ferric reducing effects with values of IC50 0.012 mg/ml and 0.007 mg/ml respectively. The ethyl acetate fraction had the best cholinesterase inhibitory effect (IC50 0.951 µg/ml AChE; 3.546 µg/ml BuChE). DPPH radical scavenging effect correlated strongly with total phenolic, flavonoids and proautocyanidins (r2 0.896, 0.651 and 0.619 respectively) while ferric reducing power showed weak correlation and NO scavenging as well as AChE inhibition had no correlation. The study shows DPPH radical scavenging could be due to the phenolic content while other class of compounds are responsible for the cholinesterase inhibition.
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Evaluating the Prevention of Mother to Child Transmission (PMTCT) of HIV Services in the Eastern Cape: subtitle if needed. If no subtitle follow instructions in manual
- Authors: Sigovana, Khuthala
- Date: 2019
- Language: English
- Type: Masters theses , text
- Identifier: http://hdl.handle.net/11260/3176 , vital:43182
- Description: Abstract text To effectively reduce HIV transmission to newborns requires a reduction of HIV prevalence among pregnant women and a full understanding of its epidemiology. There is however, a literature gap: few recent HIV studies focus on women attending antenatal care in rural areas in South Africa. A Cross-sectional study of women attending antenatal care in four Primary Care facilities was conducted. An interviewer-administered questionnaire to collect information on socio-demographic characteristics and medical history was used. Binomial logistic regression analyses were used to determine factors associated with HIV and to estimate the prevalence ratio (PR). The 95% confidence interval (CI) is used for precision of estimates; p≤0.05 for statistical significance. A total of 343 participants were recruited. Most participants (n = 341 or 99.42%; CI: 97.91 – 99.93) knew their HIV status. The antenatal HIV prevalence was 38.19% (CI: 33.17 – 43.48). Participants older than 40 years were 3.99 and 3.81 times more likely to be HIV positive compared to teenagers (PR = 3.99; CI: 1.11 – 14.30; pstxvalue = 0.034) and those in the 20-29 age group (PR = 3.81; CI: 1.07 – 13.60; pstxvaluevalue = 0.039) respectively; and this was statistically significant. Unemployed participants were 34% (PR = 1.34; CI: 1.16 – 1.55; p-value less than 0.0001) and 41 percent (PR = 1.41; CI: 1.23 – 1.61; p-value less than 0.0001) more likely to be HIV positive when compared to tertiary students and self-employed individuals respectively. The antenatal HIV prevalence remains high and is increasing in this population. However, findings suggest a changing and maturing epidemic. , Thesis (MMED) -- Faculty of Health Sciences, 2019
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- Authors: Sigovana, Khuthala
- Date: 2019
- Language: English
- Type: Masters theses , text
- Identifier: http://hdl.handle.net/11260/3176 , vital:43182
- Description: Abstract text To effectively reduce HIV transmission to newborns requires a reduction of HIV prevalence among pregnant women and a full understanding of its epidemiology. There is however, a literature gap: few recent HIV studies focus on women attending antenatal care in rural areas in South Africa. A Cross-sectional study of women attending antenatal care in four Primary Care facilities was conducted. An interviewer-administered questionnaire to collect information on socio-demographic characteristics and medical history was used. Binomial logistic regression analyses were used to determine factors associated with HIV and to estimate the prevalence ratio (PR). The 95% confidence interval (CI) is used for precision of estimates; p≤0.05 for statistical significance. A total of 343 participants were recruited. Most participants (n = 341 or 99.42%; CI: 97.91 – 99.93) knew their HIV status. The antenatal HIV prevalence was 38.19% (CI: 33.17 – 43.48). Participants older than 40 years were 3.99 and 3.81 times more likely to be HIV positive compared to teenagers (PR = 3.99; CI: 1.11 – 14.30; pstxvalue = 0.034) and those in the 20-29 age group (PR = 3.81; CI: 1.07 – 13.60; pstxvaluevalue = 0.039) respectively; and this was statistically significant. Unemployed participants were 34% (PR = 1.34; CI: 1.16 – 1.55; p-value less than 0.0001) and 41 percent (PR = 1.41; CI: 1.23 – 1.61; p-value less than 0.0001) more likely to be HIV positive when compared to tertiary students and self-employed individuals respectively. The antenatal HIV prevalence remains high and is increasing in this population. However, findings suggest a changing and maturing epidemic. , Thesis (MMED) -- Faculty of Health Sciences, 2019
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Exploring Teacher Assessment Practices in The General Education and Training Level in Junior Secondary Schools in Mthatha Education District
- Authors: Novukela, Cawe Sandys
- Date: 2019
- Language: English
- Type: Masters theses , text
- Identifier: http://hdl.handle.net/11260/3460 , vital:43409
- Description: Diabetes mellitus is one of the largest and most important public health emergencies of our time that has resulted in human suffering and huge financial implications for organisations, governments and individuals (IDF Atlas, 2015). Furthermore there is growing evidence that a number of employees are overstretched in their work environments and this has resulted in stress and burnout (McCormack and Cotter, 2013). This study investigated the effects of diabetes mellitus on burnout among WSU employees as well as the prevalence of diabetes mellitus and burnout. A mixed method research design using quantitative and qualitative approaches was employed in order to explore the effects of diabetes on burnout as well as the prevalence of diabetes and burnout at WSU. A cross-sectional survey was used to gather quantitative data and semi-structured interviews were used for the qualitative data collection. A total number of 169 participants were involved in this study. This included 154 participants and 15 participants who were selected for the quantitative and qualitative respectively using random sampling technique and purposive sampling method. The quantitative data was analysed using Stata version 13. The study findings indicated that the prevalence of diabetes at WSU was 16% and 57% participants were burned out. It was further found that the majority of participants (58%) who were diabetic also suffered from burnout. The relationship between diabetes and burnout was found to be significant. Qualitative data analysis involved coding data and analysing the emerging themes to form the basis of the findings. The results of the study found an emerging problem of high level of burnout and also a significant number of employees who were diabetic. A combination of these two conditions poses a challenge to the continued uninterrupted functioning of WSU. It is recommended that the university should educate its employees about diabetes and burnout as well as create an environment that promotes healthy lifestyle. A model has been developed that could help deal with diabetes and burnout. , Thesis - Faculty of Health Sciences, 2019
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- Authors: Novukela, Cawe Sandys
- Date: 2019
- Language: English
- Type: Masters theses , text
- Identifier: http://hdl.handle.net/11260/3460 , vital:43409
- Description: Diabetes mellitus is one of the largest and most important public health emergencies of our time that has resulted in human suffering and huge financial implications for organisations, governments and individuals (IDF Atlas, 2015). Furthermore there is growing evidence that a number of employees are overstretched in their work environments and this has resulted in stress and burnout (McCormack and Cotter, 2013). This study investigated the effects of diabetes mellitus on burnout among WSU employees as well as the prevalence of diabetes mellitus and burnout. A mixed method research design using quantitative and qualitative approaches was employed in order to explore the effects of diabetes on burnout as well as the prevalence of diabetes and burnout at WSU. A cross-sectional survey was used to gather quantitative data and semi-structured interviews were used for the qualitative data collection. A total number of 169 participants were involved in this study. This included 154 participants and 15 participants who were selected for the quantitative and qualitative respectively using random sampling technique and purposive sampling method. The quantitative data was analysed using Stata version 13. The study findings indicated that the prevalence of diabetes at WSU was 16% and 57% participants were burned out. It was further found that the majority of participants (58%) who were diabetic also suffered from burnout. The relationship between diabetes and burnout was found to be significant. Qualitative data analysis involved coding data and analysing the emerging themes to form the basis of the findings. The results of the study found an emerging problem of high level of burnout and also a significant number of employees who were diabetic. A combination of these two conditions poses a challenge to the continued uninterrupted functioning of WSU. It is recommended that the university should educate its employees about diabetes and burnout as well as create an environment that promotes healthy lifestyle. A model has been developed that could help deal with diabetes and burnout. , Thesis - Faculty of Health Sciences, 2019
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On-site evaluation of smoking, alcohol consumption and physical inactivity among commercial taxi drivers in Buffalo City Metropolitan Municipality, South Africa
- Adedokun, Aanuoluwa Odunayo, Ter Goon, Daniel, Owolabi, Eyitayo Omolara, Adeniyi, Oladele Vincent, Ajayi, Anthony Idowu
- Authors: Adedokun, Aanuoluwa Odunayo , Ter Goon, Daniel , Owolabi, Eyitayo Omolara , Adeniyi, Oladele Vincent , Ajayi, Anthony Idowu
- Date: 2019
- Subjects: Alcohol use , Substance use , Commercial drivers
- Language: English
- Type: article , text
- Identifier: http://hdl.handle.net/11260/5086 , vital:44345 , https://doi.org/10.5539/gjhs.v11n2p110
- Description: Commercial drivers have been identified as eliciting behaviours that promote non- communicable diseases and road traffic accidents. The aim of the study is to determine the prevalence and pattern of alcohol use, smoking and physical inactivity among commercial taxi drivers in Buffalo City Metropolitan Municipality, South Africa. A cross-sectional study was conducted among 403 commercial drivers using the face-to-face interviews method. The WHO STEPwise questionnaire was used to obtain the demographic data, self-reported rate of alcohol consumption, tobacco use and physical inactivity. The participants’ mean age was 43.3 ± 12.5 years. About 30% of the participants were daily smokers, 37% consumed alcohol regularly and only 18% were physically active, whilst 82% were physically inactive. The prevalence of alcohol use, smoking and physical inactivity is high among commercial drivers in East London. Workplace health education on the health effects of these lifestyles’ risky behaviours on individuals and the general public should be given to the drivers.
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- Authors: Adedokun, Aanuoluwa Odunayo , Ter Goon, Daniel , Owolabi, Eyitayo Omolara , Adeniyi, Oladele Vincent , Ajayi, Anthony Idowu
- Date: 2019
- Subjects: Alcohol use , Substance use , Commercial drivers
- Language: English
- Type: article , text
- Identifier: http://hdl.handle.net/11260/5086 , vital:44345 , https://doi.org/10.5539/gjhs.v11n2p110
- Description: Commercial drivers have been identified as eliciting behaviours that promote non- communicable diseases and road traffic accidents. The aim of the study is to determine the prevalence and pattern of alcohol use, smoking and physical inactivity among commercial taxi drivers in Buffalo City Metropolitan Municipality, South Africa. A cross-sectional study was conducted among 403 commercial drivers using the face-to-face interviews method. The WHO STEPwise questionnaire was used to obtain the demographic data, self-reported rate of alcohol consumption, tobacco use and physical inactivity. The participants’ mean age was 43.3 ± 12.5 years. About 30% of the participants were daily smokers, 37% consumed alcohol regularly and only 18% were physically active, whilst 82% were physically inactive. The prevalence of alcohol use, smoking and physical inactivity is high among commercial drivers in East London. Workplace health education on the health effects of these lifestyles’ risky behaviours on individuals and the general public should be given to the drivers.
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Prevalence and molecular analysis of multidrug-resistant Acinetobacter baumannii in the extra-hospital environment in Mthatha, South Africa
- Adjei, Anane Yaw, Apalata, Teke, Vasaikar, Sandeep, Okuthe, Grace Emily, Songca, Sandile
- Authors: Adjei, Anane Yaw , Apalata, Teke , Vasaikar, Sandeep , Okuthe, Grace Emily , Songca, Sandile
- Date: 2019
- Subjects: Acinetobacter baumannii , Carbapenemase-encoding genes , Multidrug-resistance , ISAba1 , intI1
- Language: English
- Type: article , text
- Identifier: http://hdl.handle.net/11260/2409 , vital:41457 , https://doi.org/10.1016/j.bjid.2019.09.004
- Description: The presence of Acinetobacter baumannii outside hospitals remains unclear. This study aimed to determine the prevalence of multidrug-resistance (MDR) A. baumannii in the extra-hospital environment in Mthatha, South Africa and to investigate the frequency of carbapenemase-encoding genes. Material and Methods: From August 2016 to July 2017 a total of 598 abattoir samples and 689 aquatic samples were collected and analyzed presumptively by cultural methods for the presence of A. baumannii using CHROMagarTM Acinetobacter medium. Species identification was performed by autoSCAN-4 (Dade Behring Inc., IL) and confirmed by the detection of their intrinsic blaOXA-51 gene. Confirmed MDR A. baumannii isolates were screened for the presence of carbapenemase-encoding genes, ISAba1 insertion sequence and integrase intI1. Results: In total, 248 (19.3%) Acinetobacter species were isolated. Acinetobacter. baumannii was detected in 183 (73.8%) of which 85 (46.4%) and 98 (53.6%) were recovered from abattoir and aquatic respectively. MDR A. baumannii was detected in 56.5% (48/85) abattoir isolates and 53.1% (52/98) aquatic isolates. Isolates showed high resistance to antimicrobials most frequently used to treat Acinetobacter infections such as piperacillin/tazobactam; abattoir (98% of isolates resistant), aquatic (94% of isolates resistant), ceftazidime (84%, 83%), ciprofloxacin (71%, 70%), amikacin (41%, 42%), imipenem (75%, 73%), and meropenem (74%, 71%). All the isolates were susceptible to tigecycline and colistin. All the isolates carried blaOXA-51-like. The blaOXA-23 was detected in 32 (66.7%) abattoir isolates and 11 (21.2%) aquatic isolates. The blaOXA-58-like was positive in 7 (14.6%) and 4 (7.7%) abattoir and aquatic isolates, respectively. Both groups of isolates lacked blaOXA-24-like, blaIMP-type, blaVIM-type, blaNDM-1, blaSIM, blaAmpC, ISAba1 and inI1. Isolates showed high level of Multiple Antibiotic Resistance Index (MARI) ranging from 0.20-0.52. Conclusion: Extra-hospital sources such as abattoir and aquatic environments may be a vehicle of spread of MDR A. baumannii strains in the community and hospital settings.
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- Authors: Adjei, Anane Yaw , Apalata, Teke , Vasaikar, Sandeep , Okuthe, Grace Emily , Songca, Sandile
- Date: 2019
- Subjects: Acinetobacter baumannii , Carbapenemase-encoding genes , Multidrug-resistance , ISAba1 , intI1
- Language: English
- Type: article , text
- Identifier: http://hdl.handle.net/11260/2409 , vital:41457 , https://doi.org/10.1016/j.bjid.2019.09.004
- Description: The presence of Acinetobacter baumannii outside hospitals remains unclear. This study aimed to determine the prevalence of multidrug-resistance (MDR) A. baumannii in the extra-hospital environment in Mthatha, South Africa and to investigate the frequency of carbapenemase-encoding genes. Material and Methods: From August 2016 to July 2017 a total of 598 abattoir samples and 689 aquatic samples were collected and analyzed presumptively by cultural methods for the presence of A. baumannii using CHROMagarTM Acinetobacter medium. Species identification was performed by autoSCAN-4 (Dade Behring Inc., IL) and confirmed by the detection of their intrinsic blaOXA-51 gene. Confirmed MDR A. baumannii isolates were screened for the presence of carbapenemase-encoding genes, ISAba1 insertion sequence and integrase intI1. Results: In total, 248 (19.3%) Acinetobacter species were isolated. Acinetobacter. baumannii was detected in 183 (73.8%) of which 85 (46.4%) and 98 (53.6%) were recovered from abattoir and aquatic respectively. MDR A. baumannii was detected in 56.5% (48/85) abattoir isolates and 53.1% (52/98) aquatic isolates. Isolates showed high resistance to antimicrobials most frequently used to treat Acinetobacter infections such as piperacillin/tazobactam; abattoir (98% of isolates resistant), aquatic (94% of isolates resistant), ceftazidime (84%, 83%), ciprofloxacin (71%, 70%), amikacin (41%, 42%), imipenem (75%, 73%), and meropenem (74%, 71%). All the isolates were susceptible to tigecycline and colistin. All the isolates carried blaOXA-51-like. The blaOXA-23 was detected in 32 (66.7%) abattoir isolates and 11 (21.2%) aquatic isolates. The blaOXA-58-like was positive in 7 (14.6%) and 4 (7.7%) abattoir and aquatic isolates, respectively. Both groups of isolates lacked blaOXA-24-like, blaIMP-type, blaVIM-type, blaNDM-1, blaSIM, blaAmpC, ISAba1 and inI1. Isolates showed high level of Multiple Antibiotic Resistance Index (MARI) ranging from 0.20-0.52. Conclusion: Extra-hospital sources such as abattoir and aquatic environments may be a vehicle of spread of MDR A. baumannii strains in the community and hospital settings.
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Ursolic Acid and its derivatives as bioactive agents
- Mlala, Sithenkosi, Oyedeji, Adebola Omowunmi, Gondwe, Mavuto, Oyedeji, Opeoluwa Oyehan
- Authors: Mlala, Sithenkosi , Oyedeji, Adebola Omowunmi , Gondwe, Mavuto , Oyedeji, Opeoluwa Oyehan
- Date: 2019
- Subjects: Noncommunicable diseases , Pentacyclic triterpenoids , Ursolic acid , Clinical trials
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/11260/1576 , vital:37793 , https://doi.org/10.3390/molecules24152751
- Description: Non-communicable diseases (NCDs) such as cancer, diabetes, and chronic respiratory and cardiovascular diseases continue to be threatening and deadly to human kind. Resistance to and side effects of known drugs for treatment further increase the threat, while at the same time leaving scientists to search for alternative sources from nature, especially from plants. Pentacyclic triterpenoids (PT) from medicinal plants have been identified as one class of secondary metabolites that could play a critical role in the treatment and management of several NCDs. One of such PT is ursolic acid (UA, 3 β-hydroxy-urs-12-en-28-oic acid), which possesses important biological effects, including anti-inflammatory, anticancer, antidiabetic, antioxidant and antibacterial effects, but its bioavailability and solubility limits its clinical application. Mimusops caffra, Ilex paraguarieni, and Glechoma hederacea, have been reported as major sources of UA. The chemistry of UA has been studied extensively based on the literature, with modifications mostly having been made at positions C-3 (hydroxyl), C12-C13 (double bonds) and C-28 (carboxylic acid), leading to several UA derivatives (esters, amides, oxadiazole quinolone, etc.) with enhanced potency, bioavailability and water solubility. This article comprehensively reviews the information that has become available over the last decade with respect to the sources, chemistry, biological potency and clinical trials of UA and its derivatives as potential therapeutic agents, with a focus on addressing NCD.
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- Authors: Mlala, Sithenkosi , Oyedeji, Adebola Omowunmi , Gondwe, Mavuto , Oyedeji, Opeoluwa Oyehan
- Date: 2019
- Subjects: Noncommunicable diseases , Pentacyclic triterpenoids , Ursolic acid , Clinical trials
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/11260/1576 , vital:37793 , https://doi.org/10.3390/molecules24152751
- Description: Non-communicable diseases (NCDs) such as cancer, diabetes, and chronic respiratory and cardiovascular diseases continue to be threatening and deadly to human kind. Resistance to and side effects of known drugs for treatment further increase the threat, while at the same time leaving scientists to search for alternative sources from nature, especially from plants. Pentacyclic triterpenoids (PT) from medicinal plants have been identified as one class of secondary metabolites that could play a critical role in the treatment and management of several NCDs. One of such PT is ursolic acid (UA, 3 β-hydroxy-urs-12-en-28-oic acid), which possesses important biological effects, including anti-inflammatory, anticancer, antidiabetic, antioxidant and antibacterial effects, but its bioavailability and solubility limits its clinical application. Mimusops caffra, Ilex paraguarieni, and Glechoma hederacea, have been reported as major sources of UA. The chemistry of UA has been studied extensively based on the literature, with modifications mostly having been made at positions C-3 (hydroxyl), C12-C13 (double bonds) and C-28 (carboxylic acid), leading to several UA derivatives (esters, amides, oxadiazole quinolone, etc.) with enhanced potency, bioavailability and water solubility. This article comprehensively reviews the information that has become available over the last decade with respect to the sources, chemistry, biological potency and clinical trials of UA and its derivatives as potential therapeutic agents, with a focus on addressing NCD.
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