Current topics in medicinal chemistry最新文献

Ethnopharmacological relevance: Due to the high prevalence of cancer, researchers for the past decades have made considerable efforts for its management and treatment. Medicinal plants have always been exploited to discover novel anticancer agents. Oman's huge biodiversity has created a rich source of traditional medicine.

Objective: The current survey has aimed to document the traditionally used medicinal plants of Oman and their therapeutic role in the treatment of cancer.

Material method: This study comprises of literature-based survey through different databases, including Google, Scopus, Google Scholar, Web of Science, Science Direct, Springer Link, BioMed Central and PubMed.

Results: The current review revealed a total of 57 plant species that belong to 35 families that are used in the treatment of cancer in Oman. Most documented plants belong to Solanaceae (6 sp.), Apocyanaceae (5 sp.) and Lamiaceae (4 sp.). The literature reveals that the residents of the area mostly use leaves (38.5%) and prepare their recipes in the form of decoction (40.3%). Moreover, herbs are the most dominant life form (43.85%). Among all forms of cancer in Oman, breast (47%), wound (26), and lung cancer (0.5%) were found dominantly. A literature study confirmed that the medicinal plants used for cancer in Oman are rich in phytochemicals such as quercetin, allicin, coumarin, alliin, kaempferol, solamargine, rutin, lupeol, ursolic acid and luteolin that have shown significant biological activities including anti-cancer potential. It reflects the efficacy of these plants to be used as a medicine in clinical trials. Among all, Boswellia sacra Flueck. is of key importance due to the presence Boswellic acid being used for the treatment of different types of cancer.

Conclusion: The residents of Oman have great knowledge about the traditional use of medicinal plants for the treatment of various diseases like cancer. The therapeutic potential and physiological efficacy of Omani medicinal plants should be further explored at a molecular level via in vivo and in vitro experiments.

Background: Diabetes Mellitus (DM) is known to have an impact on the health of the male reproductive system. It is linked to low sperm quality, increased oxidative stress, and an increased generation of reactive oxygen species in the seminal fluid. Pomegranate extract has phenolic compounds and significant protective properties against oxidative stress, male sex hormone disruptions, and sperm abnormalities.

Objective: The current study aimed to evaluate the effectiveness of Pomegranate Peel Extract Nanoparticles (PPENPs) on male fertility in diabetic rats.

Methods: DM was induced in rats by intraperitoneal injection of streptozotocin (60 mg/kg). Twenty-four rats were divided into four groups, 6 rats in each group: control, DM, DM+empty NPs (60 mg/kg, orally), and DM+PPENPs (60 mg/kg, orally).

Results: Administration of PPENPs increased the levels of insulin, FSH, LH, testosterone, catalase, glutathione reduced, and semen fructose. PPENPs also improved sperm quality, as seen by improvements in sperm morphology, motility, count, and the ability of metabolically active spermatozoa to convert blue resazurin dye to pink resorufin. However, PPENPs decreased levels of glucose, malonaldehyde, nitric oxide, and sperm abnormalities. Also, histological investigation of the PPENPs showed improvement in testis tissue architecture and increased the diameter size of seminiferous tubules and germinative layer thickness.

Conclusion: Our investigation proved that the treatment of PPENPs has a protective effect on the reproductive system of male diabetic rats, improving fertility parameters, healthy sperm profiles, and the antioxidant system.

Aim: Our goal was to investigate the use of Cyclodextrin in creating an aqueous extract of Cinnamon with a high content of its bioactive ingredients, validated by cell-based assays.

Background: Due to their safety and cost-effectiveness, natural compounds have garnered attention for cancer therapy, which often faces challenges related to drug toxicity and resistance. Cinnamon (Cinnamomum verum; also known as Ceylon Cinnamon) is a commonly used spice with a history in folk medicine for treating various ailments. However, its active ingredients suffer from poor solubility, stability, and bioavailability, which limits its use and benefits.

Objective: We prepared γCyclodextrin (γCD)-assisted aqueous extract of Cinnamon (CD-CIN) and compared its activity with the DMSO extract (DM-CIN).

Methods: The cells were exposed to CD-CIN and DM-CIN extracts under normal and stressed (oxidative, metal, and hypoxic) conditions and then analyzed for stress and cancerous phenotypes using various molecular assays.

Results: We found that CD-CIN possesses considerable anticancer activity that involves the activation of tumor suppressor proteins and DNA damage response. Low, non-toxic concentrations of DM-CIN and CD-CIN caused comparable inhibition of migration and invasion capability of cells, supported by molecular marker analyses. Furthermore, protection against oxidative, metal, and hypoxia stress, as well as induction of differentiation, was recorded in both DM-CIN and CD-CIN treated cells, as compared to the control.

Conclusion: We report CD-CIN as a new economic and easy Cinnamon-derived resource that possesses considerable anticancer and antistress activities and hence warrants further chemical, in vitro, and in vivo studies.

Diabetes mellitus (DM) manifests as a complex and chronic metabolic disorder, posing a significant threat to global public health and contributing substantially to mortality rates. It is characterized by elevated blood glucose levels or hyperglycemia and requires effective preventive and therapeutic strategies. One promising approach involves targeting the inhibition of α- glucosidase and α-amylase, key enzymes responsible for carbohydrate hydrolysis. Inhibiting these enzymes proves beneficial in reducing postprandial glucose levels and mitigating postprandial hyperglycemia. However, existing antidiabetic medications are associated with undesirable side effects, highlighting the need to develop new molecules with increased efficacy and reduced side effects. Traditional methods for designing such molecules are often lengthy and costly. To address this, computer-based molecular modeling tools offer a promising approach to evaluate the antidiabetic activities of chemical compounds. This review aims to compile information on chemical compounds assessed for their anti-diabetic activities through molecular modeling, with a particular focus on the period from 2020 to 2023.

There are many different applications of heterocyclic molecules in the pharmaceutical and materials science fields, which make them an important family of compounds. Among these heterocyclic compounds, nitrogen-containing heterocyclic (N-heterocyclic) compounds have attracted a lot of interest among researchers due to their various applications across a wide variety of fields. Many studies have been performed over the past few years to study the synthesis of N-heterocycles under different reaction conditions, such as solvent-free, catalytic, reactants immobilized on a solid support, one-pot synthesis, and microwave irradiation. It has been demonstrated by our research group that microwaves can be utilized for rapid and efficient synthesis of biologically active compounds. In this review, we provide an overview of the microwave-assisted non-catalytic and catalytic preparation of nitrogen-containing heterocycles, mostly polycyclic N-heterocycles, five-membered N-heterocycles, six-membered N-heterocycles, and fused N-heterocycles. Mostly in this article, we explore the microwave-assisted preparation of biologically important compounds, such as pyrimidines, thiazoles, imines, tetrazoles, steroidal derivatives, quinolines, indolizine, triazoles, beta-lactams, pyrroles and quinoxalines.

Bicyclic quinazolinone constitutes an important class of organic framework enveloping numerous biological properties which enthused organic and medicinal chemists to explore green synthetic strategies for the construction of quinazolinone hybrids with significantly improved pharmacodynamics and pharmacokinetic profiles. In this perspective, the present review summarizes the most recent green synthetic strategies, biological properties, structure-activity relationship, and molecular docking studies of the 4-quinazolinone-based scaffold. This review provides deeper insight into the hit-to-lead synthesis of quinazolinone derivatives in the development of clinically important therapeutic candidates.

This review explores the transformative impact of AI on drug development and delivery in pharmaceutical sciences, spanning formulation design, real-time monitoring, targeted delivery, and future prospects. The rational design of smart drug carriers, such as AI-optimized liposomes for cancer therapy, optimizes formulations for individual patient needs. AI-driven sensors, exemplified by glucose-monitoring biosensors for diabetics, enable adaptive drug administration, enhancing precision. Despite promises, challenges like biocompatibility, regulations, and ethics persist. Interdisciplinary collaboration and transparent communication are crucial for responsible AI adoption. Anticipated trends include personalized dosage optimization and intelligent nanocarriers. The review underscores AI's potential in reshaping pharmaceuticals for patient-centric care while addressing challenges for widespread adoption.

Growth factors and their receptor tyrosine kinases play a central role in regulating vital cellular processes such as proliferation, differentiation, division, and cell survival, and they are closely associated with the development of various types of cancer, particularly in the context of angiogenesis. Although several small chemical compounds targeting tyrosine kinase receptors have been approved by the FDA for cancer treatment by inhibiting angiogenesis, there is still a need for more effective medications. in silico studies are now crucial tools for the design of new drugs, offering considerable advantages such as cost and time reduction. In this review, we examined recent in silico research carried out between 2022 and 2024, focusing on new drug candidates synthesized to fight cancer, in particular by targeting tyrosine kinase receptors involved in the process of angiogenesis.

Synthetic routes of chromene are an area of thrust research due to its wide application as pigments, agrochemicals, cosmetics, and an important nucleus scaffold for various pharmaco-logically active drugs. The chromene nucleus is an important moiety for the discovery of new drug candidates owing to its broad range of pharmacological actions like antitumor, anti-inflammatory, antiviral, and many others. However, traditional synthesis techniques frequently use unsafe reagents and produce hazardous waste, presenting environmental issues. The eco-friendly production of chromene derivatives utilizes sustainable raw materials, non-toxic cata-lysts, and gentle reaction conditions to reduce ecological consequences. Innovative methods like microwave irradiation, ultrasound synthesis, the use of environmentally friendly solvents, a cata-lyst-based approach with minimal environmental impact, and mechanochemistry-mediated syn-thesis are implemented. These approaches provide benefits in scalability, cost-effectiveness, and ease of purification. This review compiles and presents various recently reported green synthetic strategies of chromene and its derivatives and gives the reader a clear idea of the detailed and crit-ical aspects of various synthetic protocols described.

Cancer stands as a prominent global cause of mortality, with chemotherapy using synthetic drugs being the predominant treatment method. Despite its high success rate, this approach is constrained by substantial side effects. Herbal medicines, known for their diverse bioactive components, exhibit promising anticancer attributes. The drug delivery systems can improve the precision of delivering these herbal compounds, enhancing efficacy while minimizing potential side effects. Various platforms, such as nanoparticle-based carriers, liposomes, and polymeric micelles, are investigated for encapsulating and delivering herbal components to cancer cells. These systems not only enhance the bioavailability of herbal compounds but also facilitate controlled release, sustained drug circulation, and improved cellular uptake. This comprehensive review focuses on the recent advancement in the field of drug delivery systems employed in the delivery of plant-derived anticancer compounds. It categorizes carriers into organic and inorganic nanoparticles, addressing their application in enhancing the safety and efficacy of plant-derived anticancer compounds alongside associated challenges. The review concludes by outlining recent investigations into drug delivery systems aimed at increasing the efficacy of plant-derived anticancer compounds. Future research in this field should emphasize experiments in animal models and potential clinical translation.