Universal Journal of Pharmaceutical Research
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VIRTUAL DESIGN OF NOVEL OF ORALLY BIOAVAILABLE PIPERAZINE INHIBITORS OF ENOYL-ACYL CARRIER PROTEIN REDUCTASE OF MYCOBACTERIUM TUBERCULOSIS WITH FAVORABLE PHARMACOKINETIC PROFILES
Get PDFBackground: Drug-resistant strains have been a real problem for anti-tuberculosis therapies in recent decades. Here we elaborated the virtual rational design and evaluation of a novel class of piperazine (PPZ) analogs as InhA-Mt inhibitors with a favorable pharmacokinetic profile.
Method: By in situ modification of the crystal structure of InhA-PPZ1 (Protein Data Bank (PDB) entry code: 1P44), which is the reference structure of a test set of 12 PPZs with their known inhibitory potencies experimental data (IC50exp), we prepared three-dimensional (3D) models of Inha-PPZx complexes. A structure activity relationship (SQR) model was built in the gas phase in the search for active conformations of PPZ 1-12 linearly correlating the calculated enthalpy of formation of the InhA-PPZ complex and thepIC50exp. Finally Lipinski's rule of 5 was used to filter the VCL which was subsequently screened by the pharmacophore model. The predicted activities of the new PPZ analogs obtained were evaluated with the initial QSAR and their pharmacokinetic profile was also evaluated.
Results: The virtual combinatorial library of more than 310,550 PPZ analogs was filtered by Lipinski's rule until it reached 19,044 analogs. Virtual screening by the pharmacophore made it possible to select 50 potential new analogues with predicted inhibitory potencies up to 100 times better than that of PPZ1 (IC50exp=160 nM). The predicted pharmacokinetic properties of the new analogues showed high cell membrane permeability, side effects and high human oral absorption compared to current anti-TB candidates.
Conclusions: The combined use of molecular modeling and PH4 in virtual screening makes it possible to propose new powerful anti-tuberculosis drugs with favorable pharmacokinetic profiles.
Peer Review History:
Received 21 July 2024; Reviewed 13 September 2024; Accepted 20 October; Available online 15 November 2024
Academic Editor: Dr. Asia Selman Abdullah, Pharmacy institute, University of Basrah, Iraq, [email protected]
Reviewers:
Antonio José de Jesus Evangelista, Federal University of Ceará, UFC, Brazil, [email protected]
Asmaa Ahmed Mohamed Ahmed Khalifa, Pharos University, Alexandria, Egypt, [email protected]
AMELOBLASTOMA IN POPULATION OF YEMEN: ANALYZING THE PREVALENCE AND CLINIC PATHOLOGIC FEATURES OF AMELOBLASTOMA IN A YEMENI POPULATION
Get PDFBackground and aims: Ameloblastoma is an uncommon tumor of odontogenic epithelium (ameloblasts, or the outer part of the teeth during development) that can be benign or malignant. It usually appears in the lower jaw rather than the upper jaw. The initial ameloblastoma is often treated with radical tumor resection. Analyzing the prevalence and clinic pathologic features of ameloblastoma in a Yemeni population was the goal.
Material and Methods: This retrospective cross-sectional study was carried out in all patients who were diagnosed with oral tumors at the targeted centers in Sana’a city (Al-Mamoon Center, Central Laboratory, and Al-Awlqy Laboratory Centers) in the period June 2020 to June 2022. This study is based on data taken from patients’s files that include age, gender, location, and histopathology. The study used descriptive statistics and SPSS version 26 for data analysis, describing quantitative non-parametric data using median and parametric data using mean and standard deviation.
Results: The ameloblastoma tumor prevalence was 8.8% of all oral tumors (330 cases). The mean age of the ameloblastoma patients was 31.10±11.4 (± SD) years and ranged from 11 to 80 years, with 1:1.2 males to females. The majority of ameloblastoma cases occurred in the lower jaw (93.1%; N=27), and the posterior part of the lower jaw was the main site for ameloblastoma tumors (79.3%; N=23), and 86.2%; N=23 of ameloblastoma was epithelial origin and 13.8%; N=4 was variegated origin. In terms of histological type, 65.5%; N=19 of the cases were not diagnosed, and the remaining cases showed a rate of 24.1%; N=7 for a multicystic tumor and 10.3%; N=3 for a unicystic tumor. 96.6%; N=28 of ameloblastoma cases were benign tumors, and only 3.4%; N=1 case was a malignant tumor.
Conclusions: The prevalence of ameloblastoma was significant, and these findings increase the awareness level of determent type of lesion for better diagnosis, management, and preventing measures.
Peer Review History:
Received 20 July 2024; Reviewed 6 September 2024; Accepted 16 October; Available online 15 November 2024
Academic Editor: Dr. Amany Mohamed Alboghdadly, Ibn Sina National College for Medical Studies in Jeddah, Saudi Arabia, [email protected]
Reviewers:
Dr. Gülay B Anadolu, Anadolu University, Eskisehir, Turkey, [email protected]
Dr. Sheikh Abdul Khaliq, Department of Pharmacy Practice, Faculty of Pharmacy, Hamdard University, Karachi, Pakistan, [email protected]
QUANTUM BIOLOGY FROM THEORY TO THE FUTURE OF MEDICINE AND PHARMACY: A REVIEW ON A REVOLUTIONARY CHANGE IN OUR PERCEPTION OF LIFE
Get PDFQuantum biology is an innovative field that blends quantum mechanics and biology to explore how quantum phenomena influence biological processes. This review discusses the fundamental principles of quantum biology, its potential applications in medicine, materials science and energy production, as well as the ethical implications of its progress. By understanding the quantum intricacies of life, we can gain insights into disease mechanisms, develop innovative materials and harness sustainable energy sources. Quantum mechanics, essential for understanding atomic and subatomic behavior, underpins quantum biology, which examines processes like photosynthesis, olfaction and enzyme catalysis. Key principles include superposition, entanglement and tunneling, which may enhance biological efficiency, sensitivity and precision. Quantum biology’s potential spans various fields: in medicine and pharmacy, it could lead to new diagnostic tools and therapies; in materials science, it could inspire quantum materials for electronics, energy storage and sensing; in energy production, it could inform sustainable energy development through photosynthesis insights. However, ethical considerations are crucial. Quantum-enhanced medical technologies might widen healthcare disparities and advanced quantum materials could have mixed societal impacts. Open dialogue and ethical frameworks are necessary for responsible development. The future of quantum biology is promising, with ongoing research and interdisciplinary collaboration expected to yield innovative discoveries, fostering a sustainable and prosperous future.
Peer Review History:
Received 14 July 2024; Reviewed 19 September 2024; Accepted 16 October; Available online 15 November 2024
Academic Editor: Dr. Jennifer Audu-Peter, University of Jos, Nigeria, [email protected]
Reviewers:
Ahmad Najib, Universitas Muslim Indonesia, Makassar, Indonesia, [email protected]
Dr. Nazim Hussain, North East Frontier Technical University, Arunachal pradesh, India, [email protected]
DEVELOPMENT, CHARACTERIZATION, AND OPTIMIZATION OF REPAGLINIDE LOADED SPANLASTICS ALONG WITH INVESTIGATION OF DRUG SOLUBILITY IN VARIOUS MEDIA
Get PDFObjective: This study seeks to explore the solubility of an antidiabetic drug with poor water solubility, Repaglinide (RPG), in various media, and develop and optimize RPG-loaded spanlastic formulations.
Methods: A 72-hours solubility study was conducted for RPG in different media, followed by UV spectrum analysis. Spanlastics containing RPG were prepared through the thin-film hydration (TFH) method combined with ultrasonication, incorporating varying concentrations ofthe lipophilic, non-ionic surfactant agents, Span 60 and Tween 80. Characterization was performed To assess particle size (PS), polydispersity index (PDI), zeta potential (ZP), and entrapment efficiency (EE%). Optimization was achieved by analysing characterization results and using a mixture design of Design Expert software which predicted the optimized formula.
Results: RPG exhibited the highest solubility in phosphate buffer saline (PBS, pH 6.8) incorporating 0.5% Tween 20 (168.595 µg/mL), followed by PBS with 0.1% Tween 80 (80.355 µg/mL), PBS alone (56.163 µg/mL), and PBS with 0.1% sodium lauryl sulphate (SLS) (53.706 µg/mL). UV scanning in methanol revealed three characteristic absorption bands for RPG, with peak selection optimized for molar absorptivity in each medium. The RPG-loaded spanlastic formulations demonstrated nano-sized vesicles with uniform size distribution, high stability, and efficient drug encapsulation. Optimized spanlastics predicted a particle size 126.162 nm, PDI 0.416, ZP-43.258 mV, and EE% 77.753%.
Conclusions: This research emphasizes the potential of optimized RPG-loaded spanlastics, developed through the thin-film hydration method, as a promising approach for improving the solubility and stability of poorly water-soluble drugs. RPG showed the highest solubility in PBS (pH 6.8) containing 0.5% Tween 20, and the formulation achieved desirable nanosize, uniformity, and high encapsulation efficiency.
Peer Review History:
Received 12 July 2024; Reviewed 16 September 2024; Accepted 23 October; Available online 15 November 2024
Academic Editor: Dr. Asia Selman Abdullah, Pharmacy institute, University of Basrah, Iraq, [email protected]
Reviewers:
Antonio José de Jesus Evangelista, Federal University of Ceará, UFC, Brazil, [email protected]
Asmaa Ahmed Mohamed Ahmed Khalifa, Pharos University, Alexandria, Egypt, [email protected]
ACUTE TOXICITY AND HEPATO-RENAL PROTECTION OF LIME JUICE, HONEY AND THEIR FLAVONOID-RICH FRACTIONS IN HIGH FAT-DIET INDUCED OBESE RAT MODEL
Get PDFIntroduction: A major consideration for the use of alternative herbal medicine from natural compounds is the concern of safety due to possible toxicity. This study evaluated the safety and hepato-renal protection of fresh lime juice (FLJ), raw honey (RH) and their flavonoid-rich fractions in obese rat induced high fat-diet (HFD).
Methods: Oral acute toxicity (LD50) study involved 24 female Wistar rats, divided into 8 groups of 3 rats, administered 300 mg/kg and 2000 mg/kg of FLJ, RH, methanol flavonoid rich fraction of lime juice (MFLJ) and ethyl acetate flavonoid rich fraction of honey (EAFH) respectively, for 14 days. Simultaneously, for the anti-obesity study, 24 neonate Wistar rats of 21-days old, divided into 2 groups of 12 rats (for obesity induction phase-1, for two weeks), and regrouped into 4 groups of 4 rats (14 days treatment phase-2), were used.
Results: Result of LD50 on FLJ, RH, MFLJ, and EAFH showed no toxicity, no motility, and body weight of rats was not adversely affected evenup to 2000 mg/kg.The increased body weight of the HFD-obese rats was significantly (p<0.05)reduced compared to control. There was significant (p<0.05) decrease in activities of aspartate aminotransferase and alanine aminotransferase after MIX, MFLJ and EAFH administration, compared with control. Also, total protein and bilirubin concentrations was not significantly (p<0.05) different compared to control. Administration of EAFH significantly (p<0.05) reduced the concentrations of creatinine, urea, potassium, and chloride; while MIX and EAFH significantly (p<0.05) increased their concentrations compared to control.
Conclusion: It may be concluded that FLJ, RH, MFLJ, and EAFH are safe for consumption and also possess liver and renal protection.
Peer Review History:
Received: 2 October 2023; Revised: 9 November; Accepted: 27 December; Available online: 15 January 2024
Academic Editor: Dr. Asia Selman Abdullah, Pharmacy institute, University of Basrah, Iraq, [email protected]
Reviewers:
Ahmad Najib, Universitas Muslim Indonesia, Makassar, Indonesia, [email protected]
Dr. Sangeetha Arullappan, Universiti Tunku Abdul Rahman, Malaysia, [email protected]
Dr. Gehan Fawzy Abdel Raoof Kandeel, Pharmacognosy Department, National Research Centre, Dokki, 12622, Giza, Egypt, [email protected]
OUTCOME OF AZITHROMYCIN AND MONOSODIUM GLUTAMATE ON HISTOLOGIC AND BIOCHEMICAL ALTERATIONS IN RATS’ LIVER
Get PDFBackground: Monosodium glutamate (MSG), a commonly used flavouring, mediated hepatotoxic and pro-inflammatory responses. Azithromycin (AZT), an antibiotic with anti-inflammatory activity, may be co-consumed with MSG to present unknown outcomes on the liver, a major organ for the detoxification of xenobiotics.
Aim: This study evaluated the effect of AZT and MSG on histologic and biochemical changes in rats’ liver.
Methods: Thirty rats in five groups were for seven successive days orally exposed to groups 1, (distilled water 1 mL Kg−1), 2, (MSG 8000 mg/kg), 3, overdose AZT, OAZT (AZT 412.5 mg Kg−1), 4, therapeutic concentration AZT, TAZT, (AZT 82.5mg Kg−1), and 5, (TAZT 82.5 mg Kg−1 + MSG 8000 mg Kg−1). Liver function markers in therats’ serum and liver tissue, and changes in the liver histologic were assessed by acceptable protocols. The mean of numeric data were tested for significance at p value less than 0.05 by analysis of variance (ANOVA).
Results: MSG treatment significantly (p<0.05) increased hepatic and serum alanine aminotransferase activity (ALT), aspartate aminotransferase activity (AST), alkaline phosphatase activity (ALP), total bilirubin concentration (T-BIL), and direct bilirubin concentration (D-BIL) but decreased albumin concentration (ALB) compared to control and others. TAZT treatment caused a significant (p<0.05) decrease in these effects unlike MSG and OATZ treatments while TAZT + MSG co-treatment significantly (p<0.05) reversed these effects compared to MSG-treated rats. Rats’ liver sections for rats in groups 2 and 3 showed severe hepatocellular degeneration and necrosis compared to others while those in group 4 (TAZT) showed the normal hepatic histo-architecture comparable to those in group 1 (control). Those in group 5 showed marked cellular swelling and leukocytic infiltration in only the centrilobular areas, suggesting active restorative responses.
Conclusion: Thus, TAZT significantly mitigated the compromised histologic and biochemical integrities of liver function due to MSG treatment in rats via probable normalization of their enzymatic and non-enzymatic indicators of liver function. This suggests that TAZT could be useful in managing histologic and biochemical malfunction of rats’ liver due to MSG assault.
Peer Review History:
Received: 4 October 2023; Revised: 9 November; Accepted: 21 December; Available online: 15 January 2024
Academic Editor: Dr. Marwa A. A. Fayed, University of Sadat City, Egypt, [email protected]
Reviewers:
Idoko Alexander, Caritas University, Enugu, Nigeria, [email protected]
Dr. Dennis Amaechi, MrsFoluBabade Mini Estate, Flat 5 by Old Soldiers Quarter, Sabongari/Bwari, Abuja- Federal Capital Territory, Nigeria. [email protected]
THE EFFECT OF ULTRASONICATION TIME ON PARTICLE SIZE, POLYDISPERSITY INDEX AND STABILITY EVALUATION OF ANTHOCYANIN LIPOSOMES
Get PDFBackground: One of the drug delivery systems that acts as a targeting system is liposomes which have good characteristics so they can encapsulate and deliver drug compounds. One of the characteristics that need to be considered in liposomes is the particle size and polydispersity index. Several methods can be used to control these two characteristics, including the extrusion and the ultrasonication method.
Objectives: This research aims to see stability evaluation and effect of ultrasonication time and extrusion on particle size and polydispersity index (PDI) of Anthocyanin liposomes.
Methods: The liposome formula was prepared using Anthocyanin: DSPC: cholesterol: DSPE-PEG2000 in a ratio of 1: 1.85: 1: 0.15 using the ethanol injection method. Anthocyanin liposome was divided into 3 treatments of varying ultrasonication times i.e. 5 minutes (L1), 15 minutes (L2), and 30 minutes (L3), and extrusion method as control (L0). All methods of anthocyanin liposomes size and PDI were done the stability evaluation based on storage temperature i.e 4oC and 25oC for 6 weeks
Results: The results of liposome characterization using particle size analyzer (PSA) showed that L0, L1, L2, and L3 had particle sizes of 152.1 nm, 150, 6 nm, 156.2 nm, 169.7 nm with the average PDI 0.379, 0.368, 0.450, 0.366 respectively. The statistical data (T-test) showed that there was no real influence on the particle size and PDI of Anthocyanin liposomes. However, Liposome treatment (L1) produced using the ultrasonication method for 5 minutes produces better particle size and PDI than other time variables. Moreover, the stability evaluation of anthocyanin liposomes size and PDI described the extrusion (control) and sonication method particularly 5 minutes of ultrasonication time were more stable than others due to no change size and PDI significantly at 4oC and 25oC for 6 weeks.
Conclusion: Both methods can reduce the particle size of anthocyanin liposomes and have a homogeneous particle distribution, particularly the ultrasonication treatment time of 5 minutes which is the same as the extrusion method and and also more stable at storage temperatures of 4oC and 25oC for 6 weeks.
Peer Review History:
Received 8 December 2023; Revised 26 January 2024; Accepted 29 February; Available online 15 March 2024
Academic Editor: Dr. DANIYAN Oluwatoyin Michael, Obafemi Awolowo University, ILE-IFE, Nigeria, [email protected]
Reviewers:
Dr. Md. Shahidul Islam, USTC, Chittagong, Bangladesh, [email protected]
Dr. Mohammad Tauseef, Department of Pharmaceutical Sciences, College of Pharmacy, Chicago State University, [email protected]
DENTAL CARIES AND TREATMENT NEEDS AMONG CHILDREN WITH PHYSICAL DISABILITIES IN DHAMAR CITY, YEMEN: A COMPARATIVE STUDY
Get PDFBackground and objective: A child with disability is a child who, for any reason, has a problem with learning, communication, or using their physical, and social activities. There are a lot of people with different disabilities around world which forms an important section of the community. The Objective of this study was to compare the prevalence of dental caries and treatment needs among children with and without physical disabilities in Dhamar City, Yemen.
Study design: A comparative cross-sectional study was conducted among physical disability children (n=101) and control children (n=101), their age ranged from 6 to 12 years old in Dhamar City, Yemen. WHO Oral Health Assessment Form for children, 2013 was used for assessment of dental caries and treatment needs.
Results: The findings of this study indicate a statistically significant difference in dt (decayed teeth) between children with physical disabilities and the control group (p=0.013). Among children with physical disabilities, 55.4% exhibited decay in their primary teeth, whereas the prevalence was 72.3% among the control children. The highest mean dmft scores were observed in the 6-7 years age group. Additionally, a significant difference in dmft values was found in the control children (p=0.001). It is essential to highlight that only 14.4% of the children evaluated in this study had no treatment needs identified.
Conclusions: In conclusion, the prevalence of dental caries was lower among physical disability children than control. Control children have a significantly higher dental caries in primary teeth than physical disability children. Additionally, both groups exhibit a considerable proportion of unmet treatment needs.
Peer Review History:
Received 5 February 2024; Revised 13 March 2024; Accepted 24 April; Available online 15 May 2024
Academic Editor: Dr. Marwa A. A. Fayed, University of Sadat City, Egypt, [email protected]
Reviewers:
Dr. George Zhu, Tehran University of Medical Sciences, Tehran, Iran, [email protected]
Prof. Hassan A.H. Al-Shamahy, Sana'a University, Yemen, [email protected]
EVALUATION OF THE PHYTOCHEMICAL COMPOSITION, ANTIOXIDANT PROPERTIES, AND IN VIVO ANTIHYPERGLYCEMIC EFFECT OF COCCINIA GRANDIS LEAF EXTRACT IN MICE
Get PDFBackground: Diabetes mellitus (DM) is a disease described as a high level of blood glucose level and caused by Insulin Deficiency called (Type I). Abnormal metabolism of carbohydrates in connection with insufficient insulin production is called Type II (insulin resistance). As synthetic drugs are generated for the management of different types of DM in injectable and oral dosage forms undesired side effects are being recorded.
Objective: The research side moves nowadays to the safer chemical components with hypoglycemic effects. Using natural remedies, particularly those derived from medicinal plants, to treat diabetes has emerged as a promising alternative treatment.Methods: This study investigated the phytochemicals constituents, and anti-hyperglycemic and anti-oxidant activities of Coccinia grandis leaves extract. Where the leaves of Coccinia grandis were collected and the extract containing ethanol was made. The initial phytochemical screening concerning the plant powder was done using standard procedures. Sixteen mice were divided into four groups, group (1) received normal saline, group (2) received standard oral hypoglycemic agent (glimepiride), group (3) received Glucose 50%, and group (4) received ethanolic extract. Extract doses were calculated according to the mice's body weight.
Results: Antioxidant activity for the plant extract was found to be (62 ± 0.03 %) The Anti-hyperglycemic effect was determined by calculating the reduction in glucose levels as a function of time.
Conclusion: The outcomes showed that the pharmacological impact of C. grandis’s extract reduces the blood glucose levels than the normal metabolic process and when compared to the standard oral hypoglycemic agent.
Peer Review History:
Received 2 February 2024; Revised 11 March 2024; Accepted 23 April; Available online 15 May 2024
Academic Editor: Dr. Gehan Fawzy Abdel Raoof Kandeel, Pharmacognosy Department, National Research Centre, Dokki, 12622, Giza, Egypt, [email protected]
Reviewers:
Ahmad Najib, Universitas Muslim Indonesia, Makassar, Indonesia, [email protected]
Prof. Ali Gamal Ahmed Al-kaf, Sana'a university, Yemen, [email protected]
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Get PDFIn reality, UJPR is currently acknowledged as an international journal that is indexed in different locations. In the near future, I believe our journal will attain an impact factor and become a member of Scopus journals. With its highly experienced editorial board, excellent submissions, and excellent manuscript reviewers, UJPR will be able to advance and establish a solid reputation around the world.
Using this as an occasion, I will urge all authors to ensure that their submissions are prepared in precise accordance with journal guidelines. This will help to prevent unwarranted delays in the editorial processing of their work and the disappointment of rejection.
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Finally, I hope that in upcoming yrs UJPR will be indexed with Scopus, we will continuously publish quality articles for which we invite additional original articles to be submitted and for you to cite relevant works published in this journal in your future publications