Medicinal Drugs Research Articles

Bocconia frutescens L. induces neurological defects in rat offspring.

Nearly 80% of the world's population trusts traditional medicine and plant-based drug compounds to improve health, and more than 50% of women who participated in a study have used herbal remedies during pregnancy. Bocconia frutescens L. is a plant native to tropical America, where infusion of its leaves has been widely used for the treatment of several gastrointestinal disorders. We have already shown that orogastric consumption of B. frutescens L. during the organogenesis period at concentrations equivalent to human consumption produces teratogenic effects in rats, but effects on progeny development have not yet been studied. In this study, we aimed to investigate the possible association between the consumption of B. frutescens L. at a dose equivalent to that consumed by humans and the neurological development of rat progeny. Pregnant Wistar rats were administered lyophilized B. frutescens L. extract at 300 mg/kg/day or vehicle via the orogastric route during the organogenesis period (gestation days 7-13). The physical development and sensory and motor maturation of their offspring during lactation were analyzed with a battery of reflex and physical tests. B. frutescens L. produced a significant delay in physical development and sensorimotor maturation, compared to the control group. Proton nuclear magnetic resonance spectroscopy analysis showed signals for both flavonoids and alkaloids in the B. frutescens L. extract. We conclude that the delay in physical and neurological development could be interpreted as alterations in the maturation of some neuronal circuitries induced by B. frutescens L.

Enhancing C-S and C-N bond formation with ultrasound assistance: lipase-catalyzed synthesis of 2,4-disubstituted thiazole derivatives from arylethanones and thioamides.

The present study explores an innovative approach for the efficient synthesis of 2,4-disubstituted thiazole derivatives, a class of compounds with diverse biological and pharmaceutical significance. This research presents lipase as a highly effective and environmentally friendly catalyst for thiazole synthesis. Under mild circumstances, the condensation of aryl ethenone, KBrO3, and thioamide is aided by using ultrasonic energy. Moreover, we harness the power of ultrasound irradiation to accelerate the reaction, reducing reaction times and improving product yields. The lipase-catalyzed, ultrasound-assisted synthesis presented in this study represents a greener and more sustainable alternative to traditional synthetic pathways for these important compounds, offering promising potential for applications in medicinal chemistry and drug development. This approach holds the promise of advancing the field of thiazole synthesis, contributing to more sustainable and efficient chemical processes.

Recent advances in the transformation of maleimides via annulation.

Over the past five years, maleimide scaffolds have gained considerable attention in organic synthesis for their role in forming cyclized molecules through annulation and C-H activation. As versatile and reactive coupling agents, maleimides have enabled the efficient synthesis of various cyclized products, including annulation, benzannulation, cycloaddition, and spirocyclization, with applications in medicinal chemistry, drug discovery, and materials science. Despite the extensive study of maleimide chemistry, certain reactions-such as cycloaddition-based annulation, photoannulation, and electrochemical transformations-remain underexplored despite their promising potential in the pharmaceutical and chemical industries. Recent advancements, such as photocatalysis and electrochemical methods, have expanded the utility of maleimides, providing more sustainable and selective approaches for synthesizing complex molecules. This review compiles research published between 2019 and 2024, highlighting the substrate scope, reaction diversity, and industrial relevance of maleimide-based annulation strategies. Additionally, we discuss emerging trends and future directions in maleimide chemistry, exploring opportunities for novel reaction pathways and broader applications in synthetic biology and materials science.

Implementation of Omics Approaches in Unravelling the Potency of Cordyceps militaris in Drug Discovery

: Natural products have long garnered the interest of scientific communities as they have proven to be an effective therapeutic resource that paved the path for medicinal research and drug development. Among them, Cordyceps militaris is an entomopathogenic caterpillar fungus with a renowned history of being utilized as a medicinal remedy for centuries in Eastern civilizations. The number of pharmacological functions reported by this specific fungus resulted in continuous efforts to unravel new effective bioactive compounds and their corresponding mechanism of action. As time progresses, computational techniques become the forefront of genomic and proteomic analysis, besides acting as a platform for integrating various up-to-date multidisciplinary data sources. This review briefly introduces Cordyceps militaris alongside the latest known biologically active compounds and their respective therapeutic potential. The need to implement computational applications to cope with the continuous phytochemical evolution of Cordyceps militaris will be illustrated. Moreover, many databases, mathematical algorithms, or sourcing tools that could benefit data visualization, dissemination, and interpretation aligned to fungal-based research are enumerated, in addition to describing some of the broad discoveries relative to Cordyceps militaris in the past. In conclusion, using advanced computational technology may be the foundation to leverage natural product discovery about Cordyceps militaris and contribute to future mass production of this fungus for commercial purposes in the world pharmaceutical industry.

Research Progress on the Treatment of Allergic Rhinitis with Traditional Chinese Medicine and Topical Drugs

Research Progress on the Treatment of Allergic Rhinitis with Traditional Chinese Medicine and Topical Drugs

Research progress in the treatment of an immune system disease-type 1 diabetes-by regulating the intestinal flora with Chinese medicine and food homologous drugs.

Type 1 diabetes (T1D) is a specific autoimmune disease related to genetic and autoimmune factors. Recent studies have found that the intestinal flora is one of the important environmental factors in the development of T1D. The gut microbiota is the largest microbiota in the human body and has a significant impact on material and energy metabolism. Related studies have found that the intestinal floras of T1D patients are unbalanced. Compared with normal patients, the abundance of beneficial bacteria is reduced, and various pathogenic bacteria are significantly increased, affecting the occurrence and development of diabetes. Medicinal and food homologous traditional Chinese medicine (TCM) has a multicomponent, multitarget, and biphasic regulatory effect. Its chemical composition can increase the abundance of beneficial bacteria, improve the diversity of the intestinal flora, reduce blood sugar, and achieve the purpose of preventing and treating T1D by regulating the intestinal flora and its metabolites. Therefore, based on a review of T1D, intestinal flora, and TCM derived from medicine and food, this review describes the relationship between T1D and the intestinal flora, as well as the research progress of TCM interventions for T1D through regulation of the intestinal flora. Medicine and food homologous TCM has certain advantages in treating diabetes and regulating the intestinal flora. It can be seen that there is still great research space and broad development prospects for the treatment of diabetes by regulating the intestinal flora with drug and food homologous TCM.

Photocatalytic degradation of drugs and dyes using a maching learning approach.

The waste management industry uses an increasing number of mathematical prediction models to accurately forecast the behavior of organic pollutants during catalytic degradation. With the increasing quantity of waste generated, these models are critical for reinforcing the efficiency of wastewater treatment strategies. The application of machine-learning techniques in recent years has notably improved predictive models for waste management, which are essential for mitigating the impact of toxic commercial waste on global water supply. Organic contaminants, dyes, pesticides, surfactants, petroleum by-products, and prescription drugs pose risks to human health. Because traditional techniques face challenges in ensuring water quality, modern strategies are vital. Machine learning has emerged as a valuable tool for predicting the photocatalytic degradation of medicinal drugs and dyes, providing a promising avenue for addressing urgent demands in removing organic pollutants from wastewater. This research investigates the synergistic application of photocatalysis and machine learning for pollutant degradation, showcasing a sustainable solution with promising effects on environmental remediation and computational efficiency. This study contributes to green chemistry by providing a clever framework for addressing present-day water pollution challenges and achieving era-driven answers.

Применение секретома ММСК для стимуляции репаративного остеогенеза: экспериментальное исследование

The article is devoted to the study of the effect obtained by using a regenerative medicine drug (secretome of multipotent mesenchymal stromal cells) to stimulate reparative regeneration of a long tubular bone after a fracture. The presented materials are a fragment of comprehensive studies on the mechanisms of reparative regeneration of bone tissue under the conditions of the use of cellular products. The work was carried out on outbred white rats, in which the state of the bone regenerate was studied on the 30th and 120th days after injury. After the fracture, the animals were kept under normal conditions, without immobilization or restriction of motor activity. The work used methods of anatomical preparation and light microscopy. Studies have shown that the use of a secretome was accompanied by a more reliable consolidation of fragments behind the ossification of the callus, in the structure of which by the final period of the experiment lamellar bone tissue predominated, against which foci were observed reticulofibrous bone tissue and small fragments of cartilaginous tissue with signs of osteolysis and replacement with bone tissue. In the control group, the reparative process occurred more slowly, foci of cartilaginous tissue remained in the structure of the regenerate for a long time, and the bone tissue was represented mainly by reticulofibrous tissue. A significant amount of connective tissue was revealed between the fragments. All this indicates instability and unreliable consolidation of fragments. Apparently, the secretome of multipotent mesenchymal stromal cells stimulates the repair of bone tissue in fractures by improving the trophic supply in the healing area, against the background of which the formation and remodeling of callus is activated.

AmpClass: an Antimicrobial Peptide Predictor Based on Supervised Machine Learning.

In the last decades, antibiotic resistance has been considered a severe problem worldwide. Antimicrobial peptides (AMPs) are molecules that have shown potential for the development of new drugs against antibiotic-resistant bacteria. Nowadays, medicinal drug researchers use supervised learning methods to screen new peptides with antimicrobial potency to save time and resources. In this work, we consolidate a database with 15945 AMPs and 12535 non-AMPs taken as the base to train a pool of supervised learning models to recognize peptides with antimicrobial activity. Results show that the proposed tool (AmpClass) outperforms classical state-of-the-art prediction models and achieves similar results compared with deep learning models.

Monkey Pox: An Emerging Outbreak

Monkeypox is a viral disease, with very rare cases. It has gained attention because of its similarities to smallpox. It was diagnosed in 1958 for the first time in monkeys and then later this disease effected people of Africa who were living in the western and central parts of Africa. The virus is liable for monkeypox, an orthopoxvirus, and is generally transmitted to people through contact with animals such as rodents, monkeys, and different wildlife. Human-to-human transmission can occur, mainly in localized outbreaks. Although monkeypox is sporadic and typically considered a zoonotic disease, it has caused epidemics in Central and West Africa. These outbreaks are often connected to close touch with infected animals, especially in rural communities. Some common symptoms include rash, fever, and pustules. While the mortality rate of this disease is 1-10% which is less than small pox. Treatment includes addressing signs such as fever, pain, and skin lesions. Patients may also require hospitalization, especially if they develop extreme complications, and have to be isolated to prevent human-to-human transmission. Research into antiviral medicinal drugs and vaccines is ongoing; however, in September 2021, no licensed monkeypox-specific antiviral drugs or vaccines were available. Preventing monkeypox generally includes decreasing the risk of exposure to the virus. Key preventive measures include people in endemic regions reducing contact with animals that carry the virus, including rodents and monkeys. This review provides an overview of monkeypox, focusing on its epidemiology, treatment, and prevention strategies.

Quantification of THC levels in different varieties of Cannabis sativa

This literature review paper highlights and updates the THC quantification methods applied for the differentiation of Cannabis varieties and final Cannabis products as a part of the quality control measures. The quantification method also helps to differentiate between Medical Cannabis sativa (drug or marijuana) and Industrial Cannabis sativa L. (Hemp) since THC levels are different. Cannabis has been used for thousands of years for recreational, medicinal, or religious purposes and does not produce Δ9-tetrahydrocannabinol (THC). Tetrahydrocannabinolic acid (THCA) is produced by the cannabis plant as a precursor. The acidic residue of THCA undergo decarboxylation upon heating producing the psychoactive, Cannabinoid, Δ9-tetrahydrocannabinol (THC). A variety of analytical techniques have been developed for quantification and qualification of Cannabinoids and other compounds in Cannabis plant. The most common cannabinoid quantification techniques include color tests, testing gadgets, Cannabinoids direct ELISA Kit, thin layer chromatography (TLC), gas chromatography (GC) and high performance liquid chromatography (HPLC) followed by Fourier transform infrared spectroscopy (FTIR) and Nuclear magnetic resonance spectrometry (NMR). The lack of accurate reporting of THC potency can have impacts on medical patients controlling dosage, recreational consumers expecting an effect aligned with price, and trust in the industry as a whole. Therefore, quantification of final Cannabis product plays an important role in quality control measures. This literature review paper is developed as a part of Cannabis Science awareness programme since Cannabis with 2 different names (marijuana and hemp) is used as a medicine, food and psychotropic drug (THC).

The Potential of Phytotherapy In Managing Dyspepsia: A Narrative Review

Dyspepsia, commonly known as indigestion, is delineated as suffering the manifestations of epigastric pain, nausea, burning, or after-meal fullness. The common therapy for dyspepsia, e.g., proton pump inhibitors or histamine-H2 receptor antagonists, has shown some adverse effects, thus, phytotherapy is currently becoming the drug of interest. Phytotherapy, additionally known as herbal medicine or botanical medicinal drug, includes the use of plant-derived compounds to prevent, alleviate, or therapy for diverse ailments. Most medications commonly used in Chinese traditional medicine or Asian folklore drugs contain mixtures of several plant extracts. Twelve clinical trials reported the effect and safety of phytotherapy on gastrointestinal disorders. Taken together, phytotherapy may be considered safe for the management of dyspepsia with close monitoring of the dose and duration of therapy.

Efficacy and safety of oral traditional Chinese medicine combined with conventional anti-osteoporosis drugs for osteoporosis and fractures: A meta-analysis of randomized controlled trials.

To evaluate the efficacy and safety of oral traditional Chinese medicine combined with conventional anti-osteoporosis drugs in the treatment of osteoporosis and fractures. The database of China national knowledge infrastructure, China Science and Technology Journal Database, Wangfang (WANGFANG DATA), ChineseBioMedicalLiteratureDatabase, PubMed, Embase, and Cochrane Library databases were searched from inception to June 1st, 2023 for randomized controlled trials on oral Chinese medicine combined with conventional anti-osteoporosis drugs for the treatment of osteoporosis and fractures. Quality assessment was performed using the Cochrane Handbook for Systematic Reviews of Interventions version 5.1.0. STATA 15.0 software was used for meta-analysis. Outcome measures included overall response rate, adverse events, T-score, bone mineral density, Oswestry Disability Index score, fracture healing time, and visual analog scale score. A total of 72 studies were included, involving 7847 participants. Different treatment options showed different advantages in the adjuvant treatment of osteoporosis and fractures. The total response rate, complication reduction, Oswestry Disability Index and visual analog scale score reduction, bone mineral density improvement and fracture healing time were all superior to drug therapy alone. The differences were statistically significant, but the improvement in T-score was not significant. The combination of oral traditional Chinese medicine and conventional anti-osteoporosis drugs is more effective and safer than Western medicine alone in the treatment of osteoporosis and fractures, which indicated that the treatment of integrated Chinese and western medicine can promote the healing of osteoporosis and fracture. This approach had a promising clinical application prospect. Due to the limitations of included studies, the ranking results should be interpreted with caution. In the next step, we will further conduct subgroup data based on factors, such as conventional Western medicine treatment regimens, whether surgical treatment was performed, fracture locations.

The Potential of a Stratified Approach to Drug Repurposing in Alzheimer's Disease.

Alzheimer's disease (AD) is a complex neurodegenerative condition that is characterized by the build-up of amyloid-beta plaques and neurofibrillary tangles. While multiple theories explaining the aetiology of the disease have been suggested, the underlying cause of the disease is still unknown. Despite this, several modifiable and non-modifiable factors that increase the risk of developing AD have been identified. To date, only eight AD drugs have ever gained regulatory approval, including six symptomatic and two disease-modifying drugs. However, not all are available in all countries and high costs associated with new disease-modifying biologics prevent large proportions of the patient population from accessing them. With the current patient population expected to triple by 2050, it is imperative that new, effective, and affordable drugs become available to patients. Traditional drug development strategies have a 99% failure rate in AD, which is far higher than in other disease areas. Even when a drug does reach the market, additional barriers such as high cost and lack of accessibility prevent patients from benefiting from them. In this review, we discuss how a stratified medicine drug repurposing approach may address some of the limitations and barriers that traditional strategies face in relation to drug development in AD. We believe that novel, stratified drug repurposing studies may expedite the discovery of alternative, effective, and more affordable treatment options for a rapidly expanding patient population in comparison with traditional drug development methods.

Interpretation through literature review of the properties of the neem tree (azadirachta indica) applicable in veterinary medicine

This study focuses on a bibliographic review of the properties of the Neem tree (Azadirachta indica) and its applications in veterinary medicine. Through a narrative and qualitative review of scientific articles and updated books, 72 relevant documents were identified, of which 30 met the inclusion criteria. Neem exhibits multiple therapeutic properties, including anti-inflammatory, antibacterial, antiviral, antiparasitic, and anticancer effects. Its use extends to various veterinary applications, such as reducing gastrointestinal parasite loads in goats and poultry, controlling ticks in cattle, and improving performance in broiler chickens. Additionally, studies demonstrate the low toxicity of Neem when administered orally. These findings highlight Neem's potential as a natural alternative to synthetic drugs in veterinary medicine, thus promoting more sustainable and healthier practices in the animal industry

A rapid and large volume synthesis of mono-, di-, tri-, and tetra-substituted imidazole derivatives via ultrasonic radiation-driven technique

Sonochemistry under controlled conditions has proven effective in medicinal chemistry and drug development. It can substantially shorten reaction timelines from days or hours to minutes. A convenient one-pot synthesis of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives catalyzed by PTSA and benzenesulfonic acid in ethanol as solvent, under ultrasonic irradiation and without ultrasound irradiation at 50° C has been achieved successfully. These 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives synthesis were also accomplished using different solvents viz., Methanol, Ethanol, DCM, DMF, Acetonitrile and THF and PTSA as the catalyst. This method yielded the highest % synthesis of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives with PTSA as the catalyst in solvent ethanol. These reactions were also optimized for % of PTSA catalyst required to obtain the maximum yield of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives with and without ultrasound irradiation at 50° C. Synthesis of 2,4,5-trisubstituted Imidazole derivatives reaction follows first-order rate kinetics while that of 1,2,4,5-tetrasubstituted Imidazole derivatives reaction follows the second-order rate kinetics. Furthermore, sonochemistry has higher yields, lower cost, easier workups, and higher purity than conventional thermal organic synthesis, which has lower yields, tedious workups, longer reaction periods, lower purity, and numerous byproducts.

Biological Activity of Hexaazaisowurtzitane Derivatives.

Biologically active compounds of natural or synthetic origin have a complex structure and generally contain various structural groups among which polycyclic cage amines are found. Hexaazaisowurtzitanes are representatives of these amines and studies on their biological activity began less than two decades ago, starting with research on the environmental impact of CL-20. This research helped to evaluate the risks of potential pollution in the habitat environments of living organisms and determine whether the chemical compounds in question could be utilized in pesticides, herbicides, fungicides, or medicinal drugs. The nomenclature of hexaazaisowurtzitane compounds has recently been expanded significantly, and some of them have demonstrated promise in the design of medicinal drugs. This paper review studies the pharmacological activity of the acyl derivatives of hexaazaisowurtzitane. Most of the compounds have been found to possess a high analgesic activity, providing a solution to the pressing issue of pain management in current pharmacology. Analgesic drugs currently used in the clinical practice do not meet all of the efficacy and safety requirements (gastro-, nephro-, hepato-, haematotoxicity, etc.). The material presented in the seven sections of this paper highlights information about hexaazaisowurtzitane derivatives. Furthermore, they have been observed to exhibit anti-inflammatory, anticonvulsant, antihypoxic, and antimetastatic activities, which render them highly promising for evaluation in various fields of medicinal practice.

Reconstructing the phylodynamic history and geographic spread of the CRF01_AE-predominant HIV-1 epidemic in the Philippines from PR/RT sequences sampled from 2008 to 2018.

The Philippines has had a rapidly growing human immunodeficiency virus (HIV) epidemic with a shift in the prevalent subtype from B to CRF01_AE. However, the phylodynamic history of CRF01_AE in the Philippines has yet to be reconstructed. We conducted a descriptive retrospective study reconstructing the history of HIV-1 CRF01_AE transmissions in the Philippines through molecular epidemiology. Partial polymerase sequences (n = 1144) collected between 2008 and 2018 from three island groups were collated from the Research Institute for Tropical Medicine drug resistance genotyping database. Estimation of the time to the most recent common ancestor (tMRCA), effective reproductive number (Re), effective viral population size (Ne), relative migration rates, and geographic spread of CRF01_AE was performed with BEAST. Re and Ne were compared between CRF01_AE and B. Most CRF01_AE sequences formed a single clade with a tMRCA of June 1996 [95 per cent highest posterior density (HPD): December 1991, October 1999]. An increasing CRF01_AE Ne was observed from the tMRCA to 2013. The CRF01_AE Re reached peaks of 2.46 [95 per cent HPD: 1.76, 3.27] in 2007 and 2.52 [95 per cent HPD: 1.83, 3.34] in 2015. A decrease of CRF01_AE Re occurred in the intervening years of 2007 to 2011, reaching as low as 1.43 [95 per cent HPD: 1.06, 1.90] in 2011, followed by a rebound. The CRF01_AE epidemic most likely started in Luzon and then spread to the other island groups of the country. Both CRF01_AE and Subtype B exhibited similar patterns of Re fluctuation over time. These results characterize the subtype-specific phylodynamic history of the largest CRF01_AE cluster in the Philippines, which contextualizes and may inform past, present, and future public health measures toward controlling the HIV epidemic in the Philippines.

Application of artificial intelligence approaches to predict the metabolism of xenobiotic molecules by human gut microbiome.

A highly complex, diverse, and dense community of more than 1,000 different gut bacterial species constitutes the human gut microbiome that harbours vast metabolic capabilities encoded by more than 300,000 bacterial enzymes to metabolise complex polysaccharides, orally administered drugs/xenobiotics, nutraceuticals, or prebiotics. One of the implications of gut microbiome mediated biotransformation is the metabolism of xenobiotics such as medicinal drugs, which lead to alteration in their pharmacological properties, loss of drug efficacy, bioavailability, may generate toxic byproducts and sometimes also help in conversion of a prodrug into its active metabolite. Given the diversity of gut microbiome and the complex interplay of the metabolic enzymes and their diverse substrates, the traditional experimental methods have limited ability to identify the gut bacterial species involved in such biotransformation, and to study the bacterial species-metabolite interactions in gut. In this scenario, computational approaches such as machine learning-based tools presents unprecedented opportunities and ability to predict the gut bacteria and enzymes that can potentially metabolise a candidate drug. Here, we have reviewed the need to identify the gut microbiome-based metabolism of xenobiotics and have provided comprehensive information on the available methods, tools, and databases to address it along with their scope and limitations.

Analysis of the therapeutic effect and application of anticoagulant drugs

As the global population ages, the incidence of cardiovascular disease, stroke, and other diseases associated with thrombosis is also increasing, resulting in a great need for effective anticoagulant treatments. The purpose of this research is to summarize the development of anticoagulant drugs to date, including their drug types, version iterations, mechanisms of action, as well as current challenges and future development directions of anticoagulant drugs. The research will first review traditional anticoagulants, such as vitamin K antagonists and heparins, and discuss in detail their effects, advantages, and limitations. Next, it will give a detailed description of new anticoagulants, such as direct acting oral anticoagulants (DOACs), and analyse their advantages over traditional anticoagulants in terms of safety and efficacy. Finally, it will propose the strategy of individualized therapy for specific population and the combination therapy of anticoagulant therapy and other drugs, and look forward to the development of new anticoagulant drugs in the future. The application of anticoagulant drugs in medicine has a wide range of clinical significance. With the continuous deepening of research, new therapeutic strategies and drugs are constantly being developed and improved, aiming at providing more safe and effective anticoagulant therapy.