Philip Uzor - Academia.edu (original) (raw)

Papers by Philip Uzor

Planta medica international open, Oct 1, 2017

Advances in bioscience and bioengineering, 2021

Pakistan Journal of Nutrition, Aug 15, 2019

Evidence-based Complementary and Alternative Medicine, Feb 12, 2020

Malaria is one of the major health problems in developing countries. e disease kills a large numb... more Malaria is one of the major health problems in developing countries. e disease kills a large number of people every year and also affects financial status of many countries. Resistance of the plasmodium parasite, the causative agent, to the existing drugs, including chloroquine, mefloquine, and artemisinin based combination therapy (ACT), is a serious global issue in malaria treatment and control. is warrants an urgent quest for novel compounds, particularly from natural sources such as medicinal plants. Alkaloids have over the years been recognized as important phytoconstituents with interesting biological properties. In fact, the first successful antimalarial drug was quinine, an alkaloid, which was extracted from Cinchona tree. In the present review work, the alkaloids isolated and reported recently (2013 till 2019) to possess antimalarial activity are presented. Several classes of alkaloids, including terpenoidal, indole, bisindole, quinolone, and isoquinoline alkaloids, were identified with a promising antimalarial activity. It is hoped that the reports of the review work will spur further research into the structural modification and/ or development of the interesting compounds as novel antimalarial drugs.

The root of Combretum dolichopetalum (Combreatacea) is used in ethnomedicine for the management o... more The root of Combretum dolichopetalum (Combreatacea) is used in ethnomedicine for the management of diabetes mellitus. Though some compounds have been isolated from it, the antidiabetic principles have not been identified. The present study was designed to evaluate the chemical constituents from the root of C. dolichopetalum with a view to identifying the antidiabetic principles. The constituents include the alkaloids, echinulin (1) and arestrictin B (2), the terpenoids, arjunolic acid (3) and 4'-dihydrophaseic acid (4) as well as the phenolic acids, ellagic acid (5) and 3, 4, 3'-triO -methylellagic acid (6). Twenty eight mice (in seven groups, n = 4) were made diabetic using alloxan monohydrate (i.p., 120 mg/kg) and treated orally with either the vehicle (control group), any of the constituents or glibenclamide (standard drug). The fasting blood glucose of the diabetic animals was monitored for nine hours. Results showed that all the chemical constituents (1-6) exhibited significant (p < 0.05) antidiabetic activity comparable to glibenclamide. The alkaloids exhibited the most profound antidiabetic activity. The present study has thus identified the antidiabetic principles of C. dolichopetalum root as echinulin, arestrictin B, arjunolic acid, 4'-dihydrophaseic acid, ellagic acid and 3, 4, 3'-triO -methylellagic acid. The study has further validated the ethnomedicinal use of the root of C. dolichopetalum in diabetes.

BMC Bioinformatics, Nov 8, 2022

Planta Medica, Nov 25, 2015

Planta Medica, Nov 25, 2015

Planta Medica, Dec 14, 2016

Scientific Research and Essays, Apr 15, 2014

The aim of this study was to investigate the anti-diabetic effects and biochemical parameters of ... more The aim of this study was to investigate the anti-diabetic effects and biochemical parameters of methanol root extract of Acalypha wilkesiana Mull Arg. (MEAW) in alloxan-induced diabetic rats. The effect of the extract (200 and 400 mg/kg, p.o.) on fasting blood glucose (FBG), total cholesterol (TC), triglycerides (TG), serum glutamate oxaloacetate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT) level and liver glycogen content were investigated in alloxan-induced diabetic rats after 14 days. An oral glucose tolerance test (OGTT) was also performed on the diabetic rats. Dose selection was made on the basis of acute oral toxicity study. Phytochemical analysis of the root extract was carried out following standard procedures. The most significant (p<0.05) reduction of FBG level of 74.06% was observed for 400 mg/kg in alloxan induced diabetic rats. A significant reduction (p<0.05) in serum TC and TG level of 50.43 and 58.05% respectively was also observed for the high dose of the extract. The SGOT and SGPT levels were significantly (p<0.05) reduced. The MEAW also showed improvement of body weight in diabetic rats. The animals showed no mortality at a dose of 5000 mg/kg while results of phytochemical analysis revealed the presence of mainly alkaloids, terpenoids, flavonoids, saponins, steroids and tannins. These results show that the root of Acalypha wilkesiana possesses antidiabetic, antihyperlipidemic and hepatoprotective effects.

Future Journal of Pharmaceutical Sciences

Background Combretum paniculatum (Combretaceae) Vent. is commonly used in traditional medicine to... more Background Combretum paniculatum (Combretaceae) Vent. is commonly used in traditional medicine to treat ulcers and gastrointestinal disorders, including distended spleens and the liver. This study investigated the gastroprotective effects of C. paniculatum leaf extract and its fractions on absolute ethanol-induced gastric ulcers in rats and explored their effects on endogenous antioxidant (SOD, MDA, GSH, and Catalase) levels. Butanol, n-hexane, and ethyl acetate extracts (100 and 200 mg/kg), omeprazole (20 mg/kg), and control (3% Tween 80) were administered orally. Results The methanolic extract and fractions of C. paniculatum exhibited varying degrees of ulcer protection. MECP exhibited significant (P < 0.05) ulcer protection (55.56%) at 200 mg/kg; at 100 and 200 mg/kg, HFCP induced considerable (P < 0.01 & 0.001) ulcer reduction (64.44% and 80.00%), respectively; EAFCP offered substantial (P < 0.05) ulcer reduction (57.78%) at 200 mg/kg, whereas BFCP produced significant ...

Evidence-Based Complementary and Alternative Medicine

In the present study, the antimalarial activity of the extracts and fractions of the leaves of Pe... more In the present study, the antimalarial activity of the extracts and fractions of the leaves of Persea americana and Dacryodes edulis as well as their phytochemical compositions were examined. Each of the extracts of the plants was successively fractionated to obtain hexane, ethyl acetate, methanol, and water fractions. The extracts and fractions were tested against Plasmodium berghei in both curative and suppressive antimalarial mouse models. Their major phytochemical composition was studied by the standard chemical tests and HPLC analysis. The extracts and fractions of P. americana and D. edulis demonstrated significant ( p < 0.05 ) maximal plasmodial inhibition as 52.16 ± 2.77% and 57.10 ± 1.98%, respectively, and chemosuppression of parasitemia as 64.01 ± 0.08% and 71.99 ± 0.06%, respectively. The major secondary metabolites identified in the plants include alkaloids, flavonoids, and saponins. It was concluded that P. americana and D. edulis possess promising antimalarial acti...

Background: In most parts of the world, especially in underdeveloped countries, Acquired Immunode... more Background: In most parts of the world, especially in underdeveloped countries, Acquired Immunodeficiency Syndrome (AIDS) still remains a major cause of death, disability and unfavorable economic outcomes. This has necessitated intensive research to develop effective therapeutic agents for the treatment of Human Immunodeficiency Virus (HIV) infection, which is responsible for AIDS. Peptide cleavage by HIV-1 protease is an essential step in the replication of HIV-1. Thus, correct and timely prediction of the cleavage site of HIV-1 protease can significantly speed up and optimize the drug discovery process of novel HIV-1 protease inhibitors. In this work, we built and compared the performance of selected machine learning models for the prediction of HIV-1 protease cleavage site utilizing a hybrid of octapeptide sequence information comprising bond composition, amino acid binary profile (AABP), and physicochemical properties as numerical descriptors serving as input variables for some ...

African Journal of Infectious Diseases

Background: The 2’-O-methyltransferase is responsible for the capping of SARS-CoV-2 mRNA and cons... more Background: The 2’-O-methyltransferase is responsible for the capping of SARS-CoV-2 mRNA and consequently the evasion of the host’s immune system. This study aims at identifying prospective natural inhibitors of the active site of SARS-CoV-2 2’O-methyltransferase (2’-OMT) through an in silico approach. Materials and methods: The target was docked against a library of natural compounds obtained from edible African plants using PyRx - virtual screening software. The antiviral agent, Dolutegravir which has a binding affinity score of -8.5 kcal mol−1 with the SARS-CoV-2 2’-OMT was used as a standard. Compounds were screened for bioavailability through the SWISSADME web server using their molecular descriptors. Screenings for pharmacokinetic properties and bioactivity were performed with PKCSM and Molinspiration web servers respectively. The PLIP and Fpocket webservers were used for the binding site analyses. The Galaxy webserver was used for simulating the time-resolved motions of the a...

Journal of Biomolecular Structure and Dynamics

Dolichyl-phosphate N-acetylglucosaminephosphotransferase (dpagt1) inhibition is reported to kill ... more Dolichyl-phosphate N-acetylglucosaminephosphotransferase (dpagt1) inhibition is reported to kill tumor cells whose growth progression requires increased branching of N-linked glycans. Available dpagt1 inhibitors are grossly limited and are faced with problems of heamolytic effect and aqueous solubility thereby necessitating the search for new, safe and effective dpagt1 inhibitors. We employed computational methods to screen a dataset of ∼1300 FDA approved drugs in order to obtain theoretical dpagt1 inhibitors which could be repurposed as chemotherapeutic drugs. Top six better performing drugs, binding affinity for dpagt1 at the range of -17.63 to -20.40 kcal/mol, than the reference ligand (tunicamycin; -14.86 kcal/mol) were obtained at the end of structure-based-pharmacophore- and virtual-screening and 'induced fit' docking calculations. Analysis of their binding poses identified essential pharmacophores involved in target-ligand complexation that could be targeted in chemical modification to develop more effective and safe dpagt1 inhibitors.Communicated by Ramaswamy H. Sarma.

Green Sustainable Process for Chemical and Environmental Engineering and Science

Indian Journal of Traditional Knowledge (IJTK), Mar 11, 2021

65th International Congress and Annual Meeting of the Society for Medicinal Plant and Natural Product Research (GA 2017), 2017

Tropical Journal of Pharmaceutical Research, 2018

Purpose: To evaluate the effects of Loranthus micranthus leaf extracts from three host plants on ... more Purpose: To evaluate the effects of Loranthus micranthus leaf extracts from three host plants on the blood glucose, lipid profile and other biochemical indices of diabetic rats. Methods: The extracts of L. micranthus from Persea americana, Irvingia gabonensis and Cola acuminata were administered (orally at 200 mg/kg for 14 days) to alloxan-induced diabetic rats with glibenclamide serving as the standard drug. The fasting blood glucose (FBG), lipid profile, hematological indices and liver enzyme functions of the rats were determined. Phytochemical analysis of the extracts was carried out by standard methods. Results: The extracts reduced (p < 0.05) the FBG, low density lipoprotein (LDL), triglycerides and increased (p < 0.05) high density lipoprotein (HDL) and hematological parameters of the rats. However, there was no increase (p > 0.05) in liver enzymes. Phytochemical screening showed abundance of flavonoids, alkaloids, tannins and terpenoids. Conclusion: The study revealed that L. micranthus extracts from the three host plants possess antidiabetic, hypolipidemic and anti-anemic activities.

Planta medica international open, Oct 1, 2017

Advances in bioscience and bioengineering, 2021

Pakistan Journal of Nutrition, Aug 15, 2019

Evidence-based Complementary and Alternative Medicine, Feb 12, 2020

Malaria is one of the major health problems in developing countries. e disease kills a large numb... more Malaria is one of the major health problems in developing countries. e disease kills a large number of people every year and also affects financial status of many countries. Resistance of the plasmodium parasite, the causative agent, to the existing drugs, including chloroquine, mefloquine, and artemisinin based combination therapy (ACT), is a serious global issue in malaria treatment and control. is warrants an urgent quest for novel compounds, particularly from natural sources such as medicinal plants. Alkaloids have over the years been recognized as important phytoconstituents with interesting biological properties. In fact, the first successful antimalarial drug was quinine, an alkaloid, which was extracted from Cinchona tree. In the present review work, the alkaloids isolated and reported recently (2013 till 2019) to possess antimalarial activity are presented. Several classes of alkaloids, including terpenoidal, indole, bisindole, quinolone, and isoquinoline alkaloids, were identified with a promising antimalarial activity. It is hoped that the reports of the review work will spur further research into the structural modification and/ or development of the interesting compounds as novel antimalarial drugs.

The root of Combretum dolichopetalum (Combreatacea) is used in ethnomedicine for the management o... more The root of Combretum dolichopetalum (Combreatacea) is used in ethnomedicine for the management of diabetes mellitus. Though some compounds have been isolated from it, the antidiabetic principles have not been identified. The present study was designed to evaluate the chemical constituents from the root of C. dolichopetalum with a view to identifying the antidiabetic principles. The constituents include the alkaloids, echinulin (1) and arestrictin B (2), the terpenoids, arjunolic acid (3) and 4'-dihydrophaseic acid (4) as well as the phenolic acids, ellagic acid (5) and 3, 4, 3'-triO -methylellagic acid (6). Twenty eight mice (in seven groups, n = 4) were made diabetic using alloxan monohydrate (i.p., 120 mg/kg) and treated orally with either the vehicle (control group), any of the constituents or glibenclamide (standard drug). The fasting blood glucose of the diabetic animals was monitored for nine hours. Results showed that all the chemical constituents (1-6) exhibited significant (p < 0.05) antidiabetic activity comparable to glibenclamide. The alkaloids exhibited the most profound antidiabetic activity. The present study has thus identified the antidiabetic principles of C. dolichopetalum root as echinulin, arestrictin B, arjunolic acid, 4'-dihydrophaseic acid, ellagic acid and 3, 4, 3'-triO -methylellagic acid. The study has further validated the ethnomedicinal use of the root of C. dolichopetalum in diabetes.

BMC Bioinformatics, Nov 8, 2022

Planta Medica, Nov 25, 2015

Planta Medica, Nov 25, 2015

Planta Medica, Dec 14, 2016

Scientific Research and Essays, Apr 15, 2014

The aim of this study was to investigate the anti-diabetic effects and biochemical parameters of ... more The aim of this study was to investigate the anti-diabetic effects and biochemical parameters of methanol root extract of Acalypha wilkesiana Mull Arg. (MEAW) in alloxan-induced diabetic rats. The effect of the extract (200 and 400 mg/kg, p.o.) on fasting blood glucose (FBG), total cholesterol (TC), triglycerides (TG), serum glutamate oxaloacetate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT) level and liver glycogen content were investigated in alloxan-induced diabetic rats after 14 days. An oral glucose tolerance test (OGTT) was also performed on the diabetic rats. Dose selection was made on the basis of acute oral toxicity study. Phytochemical analysis of the root extract was carried out following standard procedures. The most significant (p<0.05) reduction of FBG level of 74.06% was observed for 400 mg/kg in alloxan induced diabetic rats. A significant reduction (p<0.05) in serum TC and TG level of 50.43 and 58.05% respectively was also observed for the high dose of the extract. The SGOT and SGPT levels were significantly (p<0.05) reduced. The MEAW also showed improvement of body weight in diabetic rats. The animals showed no mortality at a dose of 5000 mg/kg while results of phytochemical analysis revealed the presence of mainly alkaloids, terpenoids, flavonoids, saponins, steroids and tannins. These results show that the root of Acalypha wilkesiana possesses antidiabetic, antihyperlipidemic and hepatoprotective effects.

Future Journal of Pharmaceutical Sciences

Background Combretum paniculatum (Combretaceae) Vent. is commonly used in traditional medicine to... more Background Combretum paniculatum (Combretaceae) Vent. is commonly used in traditional medicine to treat ulcers and gastrointestinal disorders, including distended spleens and the liver. This study investigated the gastroprotective effects of C. paniculatum leaf extract and its fractions on absolute ethanol-induced gastric ulcers in rats and explored their effects on endogenous antioxidant (SOD, MDA, GSH, and Catalase) levels. Butanol, n-hexane, and ethyl acetate extracts (100 and 200 mg/kg), omeprazole (20 mg/kg), and control (3% Tween 80) were administered orally. Results The methanolic extract and fractions of C. paniculatum exhibited varying degrees of ulcer protection. MECP exhibited significant (P < 0.05) ulcer protection (55.56%) at 200 mg/kg; at 100 and 200 mg/kg, HFCP induced considerable (P < 0.01 & 0.001) ulcer reduction (64.44% and 80.00%), respectively; EAFCP offered substantial (P < 0.05) ulcer reduction (57.78%) at 200 mg/kg, whereas BFCP produced significant ...

Evidence-Based Complementary and Alternative Medicine

In the present study, the antimalarial activity of the extracts and fractions of the leaves of Pe... more In the present study, the antimalarial activity of the extracts and fractions of the leaves of Persea americana and Dacryodes edulis as well as their phytochemical compositions were examined. Each of the extracts of the plants was successively fractionated to obtain hexane, ethyl acetate, methanol, and water fractions. The extracts and fractions were tested against Plasmodium berghei in both curative and suppressive antimalarial mouse models. Their major phytochemical composition was studied by the standard chemical tests and HPLC analysis. The extracts and fractions of P. americana and D. edulis demonstrated significant ( p < 0.05 ) maximal plasmodial inhibition as 52.16 ± 2.77% and 57.10 ± 1.98%, respectively, and chemosuppression of parasitemia as 64.01 ± 0.08% and 71.99 ± 0.06%, respectively. The major secondary metabolites identified in the plants include alkaloids, flavonoids, and saponins. It was concluded that P. americana and D. edulis possess promising antimalarial acti...

Background: In most parts of the world, especially in underdeveloped countries, Acquired Immunode... more Background: In most parts of the world, especially in underdeveloped countries, Acquired Immunodeficiency Syndrome (AIDS) still remains a major cause of death, disability and unfavorable economic outcomes. This has necessitated intensive research to develop effective therapeutic agents for the treatment of Human Immunodeficiency Virus (HIV) infection, which is responsible for AIDS. Peptide cleavage by HIV-1 protease is an essential step in the replication of HIV-1. Thus, correct and timely prediction of the cleavage site of HIV-1 protease can significantly speed up and optimize the drug discovery process of novel HIV-1 protease inhibitors. In this work, we built and compared the performance of selected machine learning models for the prediction of HIV-1 protease cleavage site utilizing a hybrid of octapeptide sequence information comprising bond composition, amino acid binary profile (AABP), and physicochemical properties as numerical descriptors serving as input variables for some ...

African Journal of Infectious Diseases

Background: The 2’-O-methyltransferase is responsible for the capping of SARS-CoV-2 mRNA and cons... more Background: The 2’-O-methyltransferase is responsible for the capping of SARS-CoV-2 mRNA and consequently the evasion of the host’s immune system. This study aims at identifying prospective natural inhibitors of the active site of SARS-CoV-2 2’O-methyltransferase (2’-OMT) through an in silico approach. Materials and methods: The target was docked against a library of natural compounds obtained from edible African plants using PyRx - virtual screening software. The antiviral agent, Dolutegravir which has a binding affinity score of -8.5 kcal mol−1 with the SARS-CoV-2 2’-OMT was used as a standard. Compounds were screened for bioavailability through the SWISSADME web server using their molecular descriptors. Screenings for pharmacokinetic properties and bioactivity were performed with PKCSM and Molinspiration web servers respectively. The PLIP and Fpocket webservers were used for the binding site analyses. The Galaxy webserver was used for simulating the time-resolved motions of the a...

Journal of Biomolecular Structure and Dynamics

Dolichyl-phosphate N-acetylglucosaminephosphotransferase (dpagt1) inhibition is reported to kill ... more Dolichyl-phosphate N-acetylglucosaminephosphotransferase (dpagt1) inhibition is reported to kill tumor cells whose growth progression requires increased branching of N-linked glycans. Available dpagt1 inhibitors are grossly limited and are faced with problems of heamolytic effect and aqueous solubility thereby necessitating the search for new, safe and effective dpagt1 inhibitors. We employed computational methods to screen a dataset of ∼1300 FDA approved drugs in order to obtain theoretical dpagt1 inhibitors which could be repurposed as chemotherapeutic drugs. Top six better performing drugs, binding affinity for dpagt1 at the range of -17.63 to -20.40 kcal/mol, than the reference ligand (tunicamycin; -14.86 kcal/mol) were obtained at the end of structure-based-pharmacophore- and virtual-screening and 'induced fit' docking calculations. Analysis of their binding poses identified essential pharmacophores involved in target-ligand complexation that could be targeted in chemical modification to develop more effective and safe dpagt1 inhibitors.Communicated by Ramaswamy H. Sarma.

Green Sustainable Process for Chemical and Environmental Engineering and Science

Indian Journal of Traditional Knowledge (IJTK), Mar 11, 2021

65th International Congress and Annual Meeting of the Society for Medicinal Plant and Natural Product Research (GA 2017), 2017

Tropical Journal of Pharmaceutical Research, 2018

Purpose: To evaluate the effects of Loranthus micranthus leaf extracts from three host plants on ... more Purpose: To evaluate the effects of Loranthus micranthus leaf extracts from three host plants on the blood glucose, lipid profile and other biochemical indices of diabetic rats. Methods: The extracts of L. micranthus from Persea americana, Irvingia gabonensis and Cola acuminata were administered (orally at 200 mg/kg for 14 days) to alloxan-induced diabetic rats with glibenclamide serving as the standard drug. The fasting blood glucose (FBG), lipid profile, hematological indices and liver enzyme functions of the rats were determined. Phytochemical analysis of the extracts was carried out by standard methods. Results: The extracts reduced (p < 0.05) the FBG, low density lipoprotein (LDL), triglycerides and increased (p < 0.05) high density lipoprotein (HDL) and hematological parameters of the rats. However, there was no increase (p > 0.05) in liver enzymes. Phytochemical screening showed abundance of flavonoids, alkaloids, tannins and terpenoids. Conclusion: The study revealed that L. micranthus extracts from the three host plants possess antidiabetic, hypolipidemic and anti-anemic activities.