Pharmaceutical and Biomedical Research
Volume:8 Issue: 4, Dec 2022

The use of pharmacological agents to synergistically target key enzymes associated with carbohydrate digestion (α-glucosidase) and the hypertension-related angiotensin-converting enzyme (ACE) are critical strategies for the management of type 2 diabetes (T2D) and its end-stage complications. Furthermore, aside from their blood pressure-lowering effect, ACE inhibitors (ACEIs) are important therapeutic agents for preventing diabetic complications, highlighting their synergistic renoprotective and antihypertensive effects in diabetic patients who are normotensive and hypertensive.

We reviewed the safety and potent activity of phytochemicals discovered based on molecular docking and dynamics in recent years that could be used to treat T2D.

We surveyed recently in silico drug discovery findings on α-glucosidase and ACE retrieved from the PubMed database. Computational in silico ADMET meta-analysis was performed on 57 compounds that could potentially inhibit α-glucosidase or ACE.

The review highlighted the fact that most hit compounds of α-glucosidase and ACE involving the use of molecular docking and molecular dynamics techniques are competitive and peptide inhibitors, respectively. Moreover, we found that most authors do not consider absorption distribution metabolism excretion toxicity (ADMET) studies on drug candidates, which is important in determining the safety profile of potent leads. Hence, we performed in silico ADMET meta-analysis of the reported compounds and found some inhibitors with an excellent pharmacological profile.

We propose that further studies be conducted on these promising leads to demonstrate their efficacy and safety in the treatment of T2D.

Traditional medicines have a wide range of pharmacological properties.

This work was done to investigate the antimicrobial effect of Thymus vulgaris, Matricaria chamomilla, Melissa officinalis, and Rhus coriaria extracts against clinical isolates of Pseudomonas aeruginosa.

A total of 180 P. aeruginosa clinical isolates were examined. Using the disc diffusion method, MIC and MBC of the methanol and alcohol herbal extracts were measured. Furthermore, microtiter plate assay evaluated biofilm development in the P. aeruginosa isolates. The free radical scavenging activity of the plant extracts against 2,2-diphenyl-1-picrylhydrazyl (DPPH) was determined.

Results showed that P. aeruginosa strains were resistant to more than three different classes of antibiotics. Our results demonstrated that the MBC value of ethanol and methanol extracts of thyme was 43.75 mg/mL, and 31.25 mg/mL, respectively. The highest MIC and MBC values were observed for the thyme and Lemon balm had the lowest MIC and MBC values. Our study showed that thyme extract was the most efficient plant extract against P. aeruginosa. The Mean±SD scavenging activity of thyme, chamomile, sumac, and lemon balm was 91.05±1.10, 89.55±0.70, 64.65±1.95, and 80.1±0.30%, respectively

These findings may help in reducing our dependence on antibiotics and handling infections of opportunistic pathogens more efficiently. Further studies are required to distinguish the most important phytochemical compounds and estimate their antibiofilm activities and their mechanisms of action.

Uncontrolled diabetes can lead to a high rate of complications. Diabetic foot ulcer (DFU) leads to significant morbidity. However, DFU can be prevented and managed through foot care education for patients.

The current study aimed to evaluate the knowledge and practice routines of patients with type 2 diabetes (T2DM) regarding foot care.

A questionnaire was designed to obtain patients’ demographic data, evaluate their risk for a foot ulcer, and assess their level of knowledge and practice about daily foot care. After confirming the validity and reliability of the questionnaire, 200 T2DM patients were interviewed.

The mean age was 61.1±11.7 years, and 64% were males. Forty-five percent of patients were previously educated regarding foot care. More than 50% of patients answered questions correctly. Calculations demonstrated the mean score of knowledge and practice as 6.3±2 (out of 11) and 14.2±3.4 (out of 20), respectively. There was no correlation between the patient’s age, gender, or history of previous DFU and their knowledge and practice level. However, patients’ higher level of education or employment status was associated with a higher level of knowledge and practice than their other respective groups.

In this study, patients had a medium to low level of foot care knowledge and a medium to a high level of daily foot care practice. However, these results also emphasize the importance of the need for organized and structured educational programs for diabetic patients regarding diabetic foot care.

Acute and subacute toxicity screenings of medicinal plants are the fastest way to evaluate the toxicological profiles of medicinal plants. It helps to have a quick idea of the harm or safety potency of drugs. This study aims to conduct an acute and subacute oral toxicity study on the Cyperus Papyrus (CP) ash in Wistar albino rats. CP is traditionally used for managing painful spasms, eye diseases, ulcers, fever, diarrhea, and inflammations. Further study is required to reflect the safety profile of this plant ash.

Acute oral toxicity study of the CP ash was evaluated by using a dose of 2000 mg/kg body weight on rats according to the Organization for Economic Co-operation and Development (OECD) guidelines using the Aot425 software. Subacute oral toxicity was carried out on 4 groups of 6 rats, at doses of 175 mg/kg, 550 mg/kg, 1750 mg/kg, and 1750 mg/kg. The recovery group (control group) received water according to OECD 407 guidelines for consecutive 28 days. At the end of the experiments (day 29), all rats were weighed and sacrificed except the rats of the recovery group which were continued without ash administration for extra 14 days and then weighed and sacrificed. Subsequently, the hematological parameters, plasma biochemical parameters, and histopathological examination were carried out. 

Upon completion of the acute toxicity, no deaths or signs of acute oral toxicity were observed. Hematologic observations after oral subacute toxicity included a decrease in hematocrit percentage, mean corpuscular volume, and lymphocyte percentage, while there was a slight increase in the mean corpuscular hemoglobin concentration, however, it returned to the normal range in the recovery group. Biochemical tests showed a mild increase in the serum creatine and aspartate aminotransferase levels but they also returned to their normal range in the recovery group. No morphological changes in the kidney, liver, lung, spleen, heart or small intestine were observed after the histopathological examinations.

Dried ash of CP is considered to be safe and non-toxic at acute exposure and as the lethal dose 50% value exceeds 2000 mg/kg body weight, it has a mild reversible effect on some hematological and biochemical parameters while no morphological changes of vital organ histopathology occur.

The effects of Pb-induced neurotoxicity have been largely established; however, the need for proper neuroprotective agents to mitigate the effects of Pb-induced neurotoxicity remains vague.

This study aimed at investigating the neuroprotective effects of pre-treatment with vitexin and C. cajan extract against Pb-induced neurotoxicity in Wistar rats.

Twenty-four male Wistar rats were randomly assigned into four groups (n=6). The control group was administered 0.5 mL of distilled water, Pb group received Pb acetate (200 mg/kg), vitexin+Pb group received Vitexin (50 mg/kg) an hour before Pb acetate (200 mg/kg), and C. cajan+Pb group received C. cajan (50 mg/kg) an hour before Pb acetate (200 mg/kg). All treatments were done within 28 days. Barnes maze test and novel object recognition (NOR) test were done to ascertain working memory, while the levels of oxidative stress markers (MDA, SOD, and GPx) were also tested. In addition, prefrontal cortical sections were stained with H&E stain, and the immunoreactivity of Iba1 and Nrf2 was examined.

There was a significant decline in working memory in the Pb group, but good working memory was maintained in vitexin and C. cajan pretreated groups. In vitexin and C. cajan pretreated groups, oxidative stress, neuronal damage, and expression of Iba1 were significantly low compared to the Pb group. Also, Nrf2 expression in the Pb group was significantly low compared to other groups.

Pretreatment with vitexin and C. cajan offers neuroprotection against Pb toxicity via antioxidant and anti-inflammation actions. Although both vitexin and C. cajan extract showed neuroprotective abilities, vitexin exhibited better results.

Emerging multidrug resistance amongst pathogens is making the choice of antibiotics for the management of infections extremely difficult and threatens the return of the pre-antibiotic era in healthcare settings. To tackle this menace, there is a growing need for exploring bioactive compounds derived from herbal extracts, which could be incorporated as alternative therapeutic agents in the antimicrobial therapy of such infections.

We evaluated the antibacterial activity of ethanolic extracts of Neem leaves against standard ATCC strains and the pathogens isolated from clinical specimens.

This cross-sectional study was undertaken to assess in vitro antibacterial activity of different concentrations of ethanolic Neem extract against three ATCC (American-type culture collection) strains and 63 clinical isolates using the disk diffusion method. The minimum inhibitory concentration (MIC) of the extract against test isolates was determined by the Broth dilution method.

Neem extract exhibited the highest antimicrobial activity toward Escherichia coli ATCC-25922 followed by Staphylococcus aureus ATCC-25923 and Pseudomonas  aeruginosa ATCC-27853 strains. Amongst the Gram-positive isolates, the extract exhibited significantly high antibacterial activity against S. aureus and Enterococcus spp. Amongst the Gram-negative isolates, high antibacterial activity was seen against E. coli followed by Klebsiella pneumoniae and Proteus mirabilis. In this study, the lowest MIC values were observed against E. coli followed by S.aureus, P. mirabilis, and K. pneumoniae. The highest MIC values of the extract were observed against non-fermenters, like P. aeruginosa and Acinetobacter spp. isolates.

This study strongly depicts that the ethanolic extract of Neem leaves exhibits significant antibacterial activity not only against the standard ATCC strains but also against various clinical isolates

Plasma protein binding is a key component in drug therapy as it affects the pharmacokinetics and pharmacodynamics of drugs.

This study aimed to predict the fraction of plasma protein binding.

A quantitative structure-activity relationship, convolutional neural network, and feed-forward neural network (QSAR-CNN-FFNN) methodology was used. CNN was used for feature selection, which is known as a difficult task in QSAR studies. The values of the descriptors acquired without the preprocessing procedures were rearranged into matrices, and features from a deep fully connected layer of a pre-trained CNN (ALEXNET) were extracted. Then, the latest features learned from the CNN layers were flattened out and passed through an FFNN to make predictions.

The external accuracy of the validation set (Q2=0.945, RMSE=0.085) showed the performance of this methodology. Another extremely favorable circumstance of this method is that it does not take a lot of time (only a few minutes) compared to the QSAR-Wrapper-FFNN method (days of hard work and concentration) and it automatically gives us the characteristics that are the best representations of our input.

We can say that this model can be used to predict the fraction of human plasma protein binding for drugs that have not been tested to avoid chemical synthesis and reduce expansive laboratory tests.

Ischemic stroke is a common disease that affects the blood vessels in the brain. This disease is considered one of the most dangerous ailments that affect the nervous system all over the world.

The aim of this study was to evaluate some hematological and biochemical parameters in men with ischemic disease in Touggourt (Algeria) region. 

The study was done on 40 voluntary individuals divided into healthy men reserved as control with Mean±SD age of 56.13±3.32 years and ischemic stroke man (patients) with Mean±SD age of 57.75±4.01 years; their origin covered the whole Touggourt (Algeria) region. Some hematological and biochemical parameters were analyzed, Sensitivity and specificity of oxidative stress biomarkers in serum, erythrocytes, and leucocytes were estimated using a receiver operating characteristics curve (ROC) design. 

The results suggest that when compared to the controls, blood glucose levels significantly increased (P>0.05) while serum sodium, potassium, and chloride concentrations and serum alkaline phosphatase activity significantly decreased (P<0.05) in stroke patients. Red blood cell, hemoglobin, glutathione (GSH), and total thiol levels significantly decreased (P<0.05) while white blood cell, neutrophile, platelets, malondialdehyde (MDA), superoxide dismutase (SOD), total antioxidant capacity (TAC) and vitamine C levels significantly increased (P<0.05) in ischemic stroke patients compared to the controls with high sensitivity and specificity values of oxidative stress markers. 

The results indicate that change in electrolytes, hematological, alkaline phosphatase, and oxidative stress markers contributes to the development or complications of ischemic stroke. Investigations on oxidative stress markers can early identify predictors of stroke disease.

The novel coronavirus disease (caused by SARS-CoV-2) has become a disaster all over the world. Based on available evidence, the main organ infected by this virus is the respiratory system; however, various other vital systems can also be affected by potential outcomes. One of the critical affected organs is the kidney.

This study aimed to report and reviewed Risk of Renal Stones in Patients With COVID-19 Infection.

In the present study, we reviewed literature about the renal stone in patients with COVID-19 in six databases, including PubMed, Scopus, Web of Science, Springer, Ovid, and Google Scholar. Then, we reported six adult COVID-19 patients with no history of kidney disease and new-onset renal stones. 

The rate of complicated ureteral stone disease significantly increased during the COVID-19 period. A few studies were available about renal stones, and mostly they were about the management of renal stones in patients infected with the coronavirus. However, in six patients, after being infected with COVID-19, the renal stone was recognized in patients. All the reported patients did not have a history of renal disease or other risk factors for renal stone formation.

Kidney injury is a possible complication of coronavirus, but based on our search, renal stone without history was not reported. However, observed cases highlighted the possible effects of COVID-19 infection on kidney function changes. On the other hand, although supplementation with vitamins C and D may be beneficial for the management of COVID-19, is associated with risks. These molecules should be used with caution, particularly in prior stone formers. Physicians should be responsible for understanding the impact of potential treatments for COVID-19 on common pathologies within their scope of practice.