Notes

Adverse Effects involving Immunosuppression: Nephrotoxicity, High blood pressure levels, along with Metabolism Condition.
Cornin is a commonly used herb in cardiology for its cardioprotective effect. The effect of herbs on the activity of cytochrome P450 enzymes (CYP450s) can induce adverse drug-drug interaction even treatment failure. Therefore, it is necessary to investigate the effect of cornin on the activity of CYP450s, which can provide more guidance for the clinical application of cornin.

Cornin (100 μM) was incubated with eight isoforms of CYP450s, including CYP1A2, 2A6, 3A4, 2C8, 2C9, 2C19, 2D6, and 2E1, in pooled human liver microsomes. The inhibition model and corresponding parameters were also investigated.

Cornin exerted significant inhibitory effect on the activity of CYP3A4, 2C9, and 2E1 in a dose-dependent manner with the IC
values of 9.20, 22.91, and 14.28 μM, respectively (p < 0.05). Cornin inhibited the activity of CYP3A4 non-competitively with the Ki value of 4.69 μM, while the inhibition of CYP2C9 and 2E1 by cornin was competitive with the Ki value of 11.31 and 6.54 μM, respectively. PF-543 in vitro Additionally, the inhibition of CYP3A4 by cornin was found to be time-dependent with the K
K
value of 6.40/0.055 min
·μM
.

The inhibitory effect of cornin on the activity of CYP3A4, 2C9, and 2E1 indicated the potential drug-drug interaction between cornin and drugs metabolized by these CYP450s, which needs further investigation and validation.
The inhibitory effect of cornin on the activity of CYP3A4, 2C9, and 2E1 indicated the potential drug-drug interaction between cornin and drugs metabolized by these CYP450s, which needs further investigation and validation.
The design of anti-cancer therapies with high anti-tumour efficacy and reduced toxicity continues to be challenging. Anti-cancer prodrug and antibody-drug-conjugate (ADC) strategies that can specifically and efficiently deliver cytotoxic compounds to cancer cells have been used to overcome some of the challenges. Key to the success of many of these strategies is a self-immolative linker, which after activation can release the drug payload. link2 Various types of triggerable self-immolative linkers are used in prodrugs and ADCs to improve their efficacy and safety.

Numerous patents have reported the significance of self-immolative linkers in prodrugs and ADCs in cancer treatment. Based on the recent patent literature, we summarise methods for designing the site-specific activation of non-toxic prodrugs and ADCs in order to improve selectivity for killing cancer cells.

In this review, an integrated view of the potential use of prodrugs and ADCs in cancer treatment are provided. This review presents recent patenng results in therapeutic applications.
Radiotherapy represents one of the main therapeutic modalities for localized prostate cancer. In the last two decades, emerging data regarding the radiobiology of prostate cancer suggests a very low α/β value which has led the scientific community to evaluate the potential advantage of hypofractionation.

The aim of this manuscript is to present the rationale of prostate radiobiology and the medical evidence of moderate hypofractionation for prostate cancer.

Existing literature was reviewed, including data from prospective clinical trials dealing with the efficacy and toxicity of hypofractionated radiotherapy. Fifteen prospective phase II studies, nine randomized phase III studies, and ten meta-analyses were selected. For every study included, the equivalent dose was calculated for both biochemical control and late toxicity.

The efficacy of hypofractionated radiotherapy, compared to conventional radiotherapy, regarding biochemical control, was evaluated in five superiority and four non-inferiority randomized phase III studies. The majority of participants in these studies were patients with low- and intermediate-risk prostate cancer. Even though the superiority criterion of the hypofractionation was not met in all studies, the non-inferiority criterion was. Prospective phase II studies of hypofractionation reported a low rate of acute and late toxicity. In randomized phase III studies, acute and late toxicity grade 3 and higher for the bowel and bladder were comparable between hypofractionated and conventional radiotherapy. The included meta-analyses showed no difference in efficacy and toxicity.

Moderate hypofractionation is feasible and safe and may be considered an alternative option in low- and intermediate-risk prostate cancer patients.
Moderate hypofractionation is feasible and safe and may be considered an alternative option in low- and intermediate-risk prostate cancer patients.
Greater saphenous vein (GSV) courses within saphenous compartment, an adipose-filled space bound by fasciae provides structural support. Ultrasound shear-wave elastography (SWE) provides objective and quantitative data on tissue shear elasticity modulus.

This study aims to analyze possible associations between early stage GSV insufficiency and saphenous intracompartmental SWE measurements.

Two-hundred consecutive patients, ages 22 to 81 (mean=44.3) years, with venous insufficiency symptoms underwent Doppler and SWE examinations. Patients had no visible or palpable sign of venous disease or had telangiectasia and reticular veins only. Analyses regarding patient age, gender, presence of venous insufficiency of GSV proper and intracompartmental connective tissue elasticity were performed.

Ninety-six patients had Doppler evidence for either bilateral or unilateral insufficiency of GSV proper at mid-thigh level. Intracompartmental elasticity of patients with venous insufficiency (mean=4.36±2.24 kilopascalsve tissue elastography measurements; thus, cut-off values obtained from specific populations have limited generalizability. Nevertheless, statistically significant intrapatient differences of intracompartmental elasticity among diseased and normal saphenous veins indicate that lack of elastic support from surrounding connective tissues contributes to venous insufficiency in early stages.
In healthcare settings with limited resources, it is crucial to make a plan to prioritize hospital admission for patients affected by COVID-19. So, we tried to develop a novel approach for triaging COVID-19 patients and deciding the priority for hospital admission using Lung Ultrasound. In this study, we aimed to evaluate the efficacy of lung ultrasound in triaging suspected COVID-19 patients and assessment of the severity of COVID-19 pneumonia and its comparison with CT chest as the gold standard.

This was a multicenter cross-sectional study enrolled on 243 COVID-19 confirmed patients presented to the emergency department in three major University hospitals in Egypt. Lung ultrasound was done by an experienced emergency physician or chest physician according to the local protocol of each hospital. Demographic, clinical, and laboratory data were collected from each patient. Each patient was subjected to CT chest and lung ultrasound.

A total of 243 confirmed COVID-19 patients were enrolled in this study, ital admission for patients affected by COVID-19 in healthcare settings with limited resources.
Lung Ultrasound with Oxygen saturation is a very efficient tool for decision-making to prioritize hospital admission for patients affected by COVID-19 in healthcare settings with limited resources.Pyrazolopyrimidines are a privileged class of 5-6 bicyclic systems with three or four nitrogen atoms, including four possible isomeric structures. The significance of this class of compounds is that they can be applied in medical and pharmaceutical fields due to their unlimited biological aptitude; hence it is the basic skeleton of several synthetic drugs. The current review aimed to highlight all the synthetic routes that have been applied to construct the pyrazolo[1,5-a]pyrimidine ring systems up to date. The sections in this study included the synthesis of pyrazolo[1,5-a]pyrimidines by condensation reactions of 5-aminopyrazoles with each of β-diketones, 1,5-diketones, β-ketoaldehydes, α-cyanoaldehydes, β-enaminones, enamines, enaminonitriles, ethers, with unsaturated ketones, unsaturated thiones, unsaturated esters, unsaturated dienones "1,2-allenic", unsaturated aldehydes, unsaturated imines, and unsaturated nitriles. The synthesis of this class of hetereocycles was extended for ring construction from acyclic reagents and multicomponent reactions under catalytic or catalyst-free conditions.Type 2 diabetes (adult onset diabetes) is the most common type of diabetes, accounting for around 90% of all diabetes cases with insulin resistance and insulin secretion defect. The key goal of anti-diabetic therapy is to increase the development of insulin, immunity and/or decrease the amount of blood glucose. While many synthetic compounds have been produced as anti-diabetic agents, due to their side effects and limited effectiveness, their usefulness has been hindered. This systematic review investigated the bioactive compounds reported to possess activities against type 2 diabetes. Three (3) databases, PubMed, ScienceDirect, and Google Scholar, were searched for research articles published between January 2010 and October 2020. A total of 6464 articles were identified, out of which 84 articles were identified to be eligible for the study. From the data extracted, it was found that quercetin, Kaempferol, Rosmarinic acid, Cyanidin, Rutin, Catechin, Luteolin, and Ellagic acid were the most cited bioactive compounds, which all falls within the class of polyphenolic compounds. link3 The major sources of these bioactive compounds include citrus fruits, grapes, onions, berries, cherries, broccoli, honey, apples, green tea, Ginkgo biloba, St. John's wort, green beans, cucumber, spinach, tea, Rosmarinus officinalis, Aloe vera, Moringa oleifera, tomatoes, potatoes, oregano, lemon balm, thyme, peppermint, Ocimum basilicum, red cabbage, peas, olive oil, and walnut. In conclusion, the data collected in our study indicates that consumption of polyphenolic/flavonoids rich food and vegetables as a routine diet could considerably reduce the risk of T2DM and also benefits insulin sensitivity and other chronic inflammations.The coronavirus pandemic has hit the world lately and caused acute respiratory syndrome in humans. The causative agent of the disease was soon brought to focus by scientists as SARS-CoV-2 and later called a novel coronavirus by the general public. Due to the severity and rapid spread of the disease, WHO classifies the COVID-19 pandemic as the 6th public health emergency even after taking efforts like worldwide quarantine and restrictions. Since only symptomatic treatment is available, the best way to control the spread of the virus is by taking preventive measures. Various types of antigen/antibody detection kits and diagnostic methods are available for the diagnosis of COVID-19 patients. In recent years, various phytochemicals and repurposing drugs are showing a broad range of anti-viral activities with different modes of action have been identified. Repurposing drugs such as arbidol, hydroxychloroquine, chloroquine, lopinavir, favipiravir, remdesivir, hexamethylene amiloride, and dexamethasone, tocilizumab, interferon-β, neutralizing antibodies exhibit in vitro anti-coronaviral properties by inhibiting multiple processes in the virus life cycle. Various research groups are involved in drug trials and vaccine development. Plant-based anti-viral compounds such as baicalin, calanolides, curcumin, oxymatrine, matrine, and resveratrol exhibit different modes of action against a wide range of positive/negative sense-RNA/DNA virus, and future researches need to be conducted to ascertain their role, use in managing SARS-CoV-2. Thus, this article is an attempt to review the current understanding of COVID-19 acute respiratory disease and summarize its clinical features with their prospective control and various aspects of the therapeutic approach.
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