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Cancer is a major public health concern, and is one of the leading causes of death globally. Surgical removal, chemotherapy or hormonal therapy, radiation therapy, or a combination of them are treatment for cancer, many of which are ineffective or have serious side effects. In view of this, there is a search for new, more effective alternatives for cancer prevention and treatment. One possible source of compounds are natural products; among them, terpenes, a large class of organic compounds, have shown promise due to their anti-inflammatory, anti-tumorigenic, and hypolipidemic properties, among others recorded in the literature.
The study aims to use a patent review to evaluate the development and use of terpenes, or formulations containing terpenes, in new therapeutic options for the treatment of various types of cancer.
This patent review was carried out using the specialized patent databases of WIPO and Espacenet. The selection of patents was based on the following inclusion criteria which included pre-clinical and/or clinical trials, and demonstrated anti-tumor effects.
Eight patents were identified, six from China, and two from Japan. In this review, all patents confirmed having good antitumor activity for many types of cancer cells. In addition, the inventors indicate more studies pre-clinical and clinical trials giving greater clarity and accurate reflection of the activity of the products studied.
Natural products are an important source of compounds for use in the fight against cancer that can act synergistically, and help in the treatment of cancer.
Natural products are an important source of compounds for use in the fight against cancer that can act synergistically, and help in the treatment of cancer.
Tuberculosis remains one of the most deadly infectious diseases worldwide due to the emergence of multi-drug resistance (MDR) and extensively drug resistance (XDR) strains of Mycobacterium tuberculosis (MTB).
Currently, available drugs are getting resistant and toxic. Hence, there is an urgent need for the development of potent molecules to treat tuberculosis.
Herein, the screening of a total of eight symmetrical 1,4-dihydropyridine (1,4- DHP) derivatives (4a-4h) was carried out for whole-cell anti-TB activity against the susceptible H37Rv and MDR strains of MTB.
Most of the compounds exhibited moderate to excellent activity against the susceptible H37Rv. Moreover, the most promising compound 4f (against H37Rv) having paratrifluoromethyl phenyl group at 4-position and bis para-methoxy benzyl ester group at 3- and 5- positions of 1,4-dihydropyridine pharmacophore, exhibited no toxicity, but demonstrated weak activity against MTB strains resistant to isoniazid and rifampicin. In light of the inhibitory profile of the title compounds, enoyl-acyl carrier protein reductase (InhA) appeared to be the appropriate molecular target. A docking study of these derivatives against InhA receptor revealed favorable binding interactions. Further, in silico predicted ADME properties of these compounds 4a-4h were found to be in the acceptable ranges, including satisfactory Lipinski's rule of five, thereby indicating their potential as drug-like molecules.
In particular, the 1,4-DHP derivative 4f can be considered an attractive lead molecule for further exploration and development of more potent anti-TB agents as InhA inhibitors.
In particular, the 1,4-DHP derivative 4f can be considered an attractive lead molecule for further exploration and development of more potent anti-TB agents as InhA inhibitors.Tuberculosis is a disease caused by Mycobacterium tuberculosis (Mtb), affecting millions of people worldwide. The emergence of drug resistance is a major problem in the successful treatment of tuberculosis. #link# Due to the commencement of MDR-TB (multi-drug resistance) and XDR-TB (extensively drug resistance), there is a crucial need for the development of novel anti-tubercular agents with improved characteristics such as low toxicity, enhanced inhibitory activity and short duration of treatment. In this direction, various heterocyclic compounds have been synthesized and screened against Mycobacterium tuberculosis. Among them, benzimidazole and imidazole containing derivatives have been found to have potential anti-tubercular activity. The present review focuses on various imidazole and benzimidazole derivatives (from 2015-2019) with their structure-activity relationships in the treatment of tuberculosis.
Mucopolysaccharidosis type II (Hunter syndrome, or MPS II) is an X-linked lysosomal disorder caused by the deficiency of iduronate-2-sulfatase, which leads to the accumulation of glycosaminoglycans (GAGs) in a variety of tissues, resulting in a multisystemic disease that can also impair the central nervous system (CNS).
This review focuses on providing the latest information and expert opinion about the therapies available and under development for MPS II.
We have comprehensively revised the latest studies about hematopoietic stem cell transplantation (HSCT), enzyme replacement therapy (ERT - intravenous, intrathecal, intracerebroventricular, and intravenous with fusion proteins), small molecules, gene therapy/genome editing, and supportive management.
Intravenous ERT is a well-established specific therapy, which ameliorates the somatic features but not the CNS manifestations. Intrathecal or intracerebroventricular ERT and intravenous ERT with fusion proteins, presently under development, seem to be ae of MPS II should be available.
Medical treatments are used either alone or in combination with assisted reproductive techniques for treatment of infertile patients with hypergonadotropic hypogonadism. A wide range of treatment options such as gonadotropins, aromatase inhibitors (AIs), selective estrogen receptor modulators (SERMs) and their combination are available as options.
The aim of this review was to evaluate treatment options for the infertile men with hypergonadotropic hypogonadism.
A literature search of MEDLINE (1980-2019) was conducted using the terms 'hypogonadism', 'male infertility', 'gonadotropins', 'SERMs' and 'AIs'. Pathologies leading to hypergonadotropic hypogonadism and treatment modalities such as gonadotropins, SERMs, AIs and surgical treatment were discussed.
FSH increases spontaneous pregnancy rates but level of evidence was proven to be low for live birth rates. AIs are valid treatment options for patients with low T/E2 ratio as they significantly increase sperm concentrations. SERMs are recommended for infertile males with a sperm concentration between 10-20 millions. Varicocele was reported to increase testosterone levels of hypogonadic infertile males.
Medical treatment modalities such as gonadotropins, SERMs, AIs and combination of these therapies has been showed to have some effect in improvement of fertility but is not mainstream of the treatment.
Medical treatment modalities such as gonadotropins, SERMs, AIs and combination of these therapies has been showed to have some effect in improvement of fertility but is not mainstream of the treatment.In light of the growing resistance toward current antiviral drugs, efforts to discover novel and effective antiviral therapeutic agents remain a pressing scientific effort. link2 Antiviral peptides (AVPs) represents promising therapeutic agents due to their extraordinary advantages in terms of potency, efficacy and pharmacokinetic properties. The growing volume of newly discovered peptide sequences in the post-genomic era requires computational approaches for timely and accurate identification of AVPs. Machine learning (ML) methods such as random forest and support vector machine represents robust learning algorithms that are instrumental in successful peptide-based drug discovery. Therefore, this review summarizes the current state-of-the-art on the application of ML methods for identifying AVPs directly from the sequence information. We compare the efficiency of these methods in terms of the underlying characteristics of the dataset used along with feature encoding methods, ML algorithms, cross-validation methods and prediction performance. Finally, guidelines for development of robust AVP models are also discussed. link3 It is anticipated that this review will be serve as a useful guide for the design and development of robust AVP and related therapeutic peptide predictors in the future.More than 70 years have passed since the first description of Klinefelter Syndrome (KS), the most frequent chromosome disorder causing male infertility and hypogonadism. KS is associated with increased cardiovascular (CV) mortality due to several comorbidities, including hypogonadism, as well as metabolic syndrome and type 2 diabetes, which are highly prevalent in these patients. Aside from selleck products , patients with KS suffer from both acquired and congenital CV abnormalities, cerebrovascular thromboembolic disease, subclinical atherosclerosis and endothelial dysfunction, which may all contribute to increased CV mortality. The mechanisms involved in this increased risk of CV morbidity and mortality are not entirely understood. More research is needed to better characterise the CV manifestations, elucidate the pathophysiological mechanisms and define the contribution of testosterone replacement to restoring CV health in KS patients. This review explores the complex association between KS, metabolic syndrome and CV risk in order to plan future studies and improve strategies to reduce mortality in this high-risk population.Cardiovascular diseases(CVD) are the leading cause of death worldwide. Evidence from observational and randomized controlled studies showing the potential benefits of green tea on lowering CVD risk has been emerging rapidly during the past few decades.These benefits include reduced risk for major cardiovascular events, lowering of blood pressure, decreased LDL cholesterollevels and weight loss.At the same time, the understanding of physiological mechamismsbehind these alterations is advancing.Consumption of green tea originates from China thousands of years ago, but has since expanded all over the world.Recent advances in understanding the role of tea polyphenols, mainly catechins,as mediators of tea's health benefits has caused an emergence of various types of green teaextracts(GTE) on the market. While drinking green tea is generally considered safe, there are concerns about thesafety of using tea extracts. The present article reviews the current evidence of green tea consumption leading to reducedCVD risk, the phenomenon's potential biological mechanisms and the safety of using GTE.Steroid-resistant nephrotic syndrome (SRNS) constitutes the second most frequent cause of chronic kidney disease in childhood. The etiology of SRNS remains largely unknown and no standardized treatment exists. Recent advances in genomics have helped to build understanding of the molecular mechanisms and pathogenesis of the disease. The genetic polymorphisms in genes encoding proteins which are involved in the pharmacokinetics and pharmacodynamics of glucocorticoids (GCs) partially account for the different responses between patients with nephrotic syndrome. More importantly, single-gene causation in podocytes-associated proteins was found in approximately 30% of SRNS patients. Some potential biomarkers have been tested for their abilities to discriminate against pediatric patients who are sensitive to GCs treatment and patients who are resistant to the same therapy. This article reviews the recent findings on genetic mechanisms, predictive biomarkers and current therapies for SRNS with the goal to improve the management of children with this syndrome.
Website: https://www.selleckchem.com/products/qnz-evp4593.html
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