Drug Design, Discovery and Therapy
Lavandula Species as a Bioactive Phytomolecules and Medicinal Properties: A Review
The family Lamiaceae includes the genus Lavandula which is widely cultivated throughout the Mediterranean region including France Spain and Italy. The plant forms dense clumps that are roughly 40-60 cm tall. The reference genome for “Jingxun 2” an excellent cultivar of Lavender (Lavandula angustifolia) was developed by a research team in China. Lavandula which contains tannins phytosterols coumarins herniarins ursolic acid sugars valeric acid glycolic acid coumaric acid anthocyanins minerals and essential oils. Lavender oil can also help with many kinds of health problems because it has many bioactive ingredients such as linalool lavandulol anthocyanins geraniol ursolic acids linalyl acetate valeric acid 18-cineole borneol lavandulyl acetate terpinen-4-ol camphor phytosterols coumaric acid and glycolic acid. The genus Lavender exhibits various biological activities including antioxidants antiparasitic and neuroprotective properties. Recent studies have demonstrated the numerous biological activities of Lavandula but we still need to develop new medications that harness the components of this plant to treat a variety of illnesses. This study covers various recent advancements in the use of Lavender and its phytochemicals by using various search engines including Scopus PubMed Google Scholar and Web of Science.
Synthesis, Crystal Structure, Spectroscopic Characterization, In vitro and In silico Molecular Docking Studies of Benzyl Tetrazole-N-Isobutyl Acetamide Hybrid
Tetrazole-based compounds are of significant interest due to their potential pharmacological applications. The current study focuses on the synthesis and analysis of such a compound.
This research aims to synthesize the title compound N-(3-methyl-1-phenyl-2-(1H-tetrazol-1-yl) butyl) acetamide analyze its crystal structure perform computational studies and evaluate its potential pharmacological activities and it’s in silico and in vitro supports specifically antidiabetic and anti-inflammatory properties.
The title compound C14H19N5O was synthesized and its crystal structure was confirmed using single-crystal X-ray diffraction analysis by default parameters. Density Functional Theory (DFT) calculations were performed using the Gaussian 09W software package with the B3LYP/6-311++G (dp) method to optimize the compound's structure and calculate its HOMO-LUMO energy gap Molecular Electrostatic Potential (MEP) and Mulliken charge distribution. In vitro antidiabetic and anti-inflammatory activities were assessed and compared with standard drugs by using reported protocols. Additionally molecular docking studies were conducted with enzymes related to diabetes and inflammation with default parameters and Auto-Dock 4.2 software was used.
The X-ray diffraction analysis confirmed the crystal structure and the Density Functional Theory (DFT) calculations provided insights into the molecular properties of the compound. Molecular docking experiments with relevant enzymes further supported the significant antidiabetic and anti-inflammatory activities demonstrated in the in vitro tests.
The synthesized tetrazole-based compound exhibits promising antidiabetic and anti-inflammatory activities supported by both experimental and theoretical studies suggesting its potential for further pharmacological investigation.
Exploring Rheumatoid Arthritis: Unraveling Signaling Pathways, Advancing Management, and Charting Future Perspectives
Rheumatoid arthritis (RA) is a chronic autoimmune disorder in which inflammation occurs in the synovial joint and synovial membrane and in severe condition it leads to erosion of cartilage and bone. The etiology of RA is still indescribable; generally RA is a multifactorial disease wherein complex interactions between patients and different factors such as environmental genetic and epigenetic factors determine the overall risk of disease. RA is classified based on the stage of disease. Treatment for RA is still a challenge for doctors and researchers. Effective treatment for RA can be achieved by decreasing disease activity or reduction of RA to other patients using currently available treatment options. This article gives a comprehensive perspective of data regarding different signaling pathways involved in RA development factors affecting RA stages of RA and other treatments of RA. This article also suggests future research perspectives that would be helpful for the development of RA treatment (medicine) with more efficacy safety profiles and lower financial costs.
Neuropharmacological Evaluation of Betaine against Parkinson’s Disease Rat Model
This study aimed at evaluating the neuropharmacological impacts of betaine a natural compound known for its antioxidant properties in a rat model of Parkinson’s disease induced by rotenone.
Male Wistar rats were separated into various groups and administered betaine at two different doses (10 mg/kg and 20 mg/kg orally) in addition to rotenone (2 mg/kg subcutaneously) for 35 days.
Various parameters were analyzed to determine the effectiveness of betaine. After receiving rotenone the subjects displayed various behavioral alterations such as catalepsy delayed beam walk postural instability unusual movement patterns reduced weight altered rearing behavior impaired muscle coordination decreased locomotor activity and weakened grip strength. Interestingly these effects were notably alleviated when betaine was given alongside. Betaine demonstrated a reduction in rotenone-induced oxidative stress by lowering levels of thiobarbituric acid reactive substances (TBARS) and superoxide anion generation (SAG) while increasing levels of catalase (CAT) and glutathione (GSH) in the cerebrum and midbrain regions. Moreover betaine helped alleviate the reduction in dopamine (DA) levels caused by rotenone-induced neurodegeneration. In general the protective impact of betaine against rotenone-induced PD symptoms outperformed the typical treatment with Levodopa+Carbidopa (L+C) especially at the higher dosage of 20 mg/kg.
These results indicate that betaine shows potential as a therapeutic option for PD because of its antioxidant properties.
Cinnamomum tamala (Buch.-Ham.) Th. G. G. Nees Leaves Extract Protects against an Experimental Murine Model of Diabetic Cardiomyopathy
Diabetic cardiomyopathy (DCM) is a critical complication involving oxidative stress and inflammation that is not amenable to current therapeutic strategies. Herbal remedies are increasingly being used as an alternative to current treatment options.
In this research we evaluated the effects of Cinnamomum tamala (Buch.-Ham.) Th. G. G. Nees leaves the extract in DCM and its scope as an adjunct or alternative therapy along with existing standard treatment.
The ethanolic extract was prepared using the Soxhlet apparatus and rotary evaporator. Streptozotocin (1st day) and isoproterenol (12th and 13th day) were given to induce DCM in rats. Oral treatment with ethanolic extract of C. tamala leaves (250 and 500 mg/kg) or glibenclamide (10 mg/kg) was given from the 3rd to the 14th day.
C. tamala extract or glibenclamide attenuated streptozotocin-induced hyperglycemia in rats. C. tamala extract or glibenclamide (10 mg/kg) inhibited serum dyslipidemia lactate dehydrogenase and creatine kinase MB activities. The body weight total heart protein and heart weight were ameliorated by C. tamala extract or glibenclamide (10 mg/kg). Furthermore DCM culminated in cardiac oxidative stress and inflammation and these biochemical parameters were ameliorated by C. tamala extract or glibenclamide (10 mg/kg) treatment. The combination of C. tamala extract (500 mg/kg) and glibenclamide (5 mg/kg low dose) significantly attenuated DCM relative to separate treatments.
C. tamala can be a useful alternative or adjunct therapy in DCM therapeutics. The combinatorial treatment approach with C. tamala might reduce the dose of therapeutic molecules used in the current clinical practice of DCM.
Phytochemical and Pharmacological Profile of Plants from Genus Buxus: A Review
Buxus is an evergreen shrub of the Buxaceae family. A comprehensive survey of the literature has been conducted revealing that alkaloids are the predominant metabolites characterized by their noteworthy biological activities. Of particular interest are the alkaloids that have exhibited significant cytotoxic activity against various cell lines including HL-60 SMMC-7721 A549 MCF-7 SW480 ES2 and A2780 cell lines. CVB-D buxbodine B and buxmicrophyllines F can inhibit the growth of tumor cells and induce tumor cell apoptosis. This paper reviews the chemical constituents antitumor effect and mechanism of Buxus alkaloids in recent years so as to provide a reference for its further development and utilization of medicinal plants of the genus Buxus.
Therapeutic Potential of Alkaloids to Combat Breast Cancer: A Mechanistic Overview
Breast cancer remains a major global health concern ranking among the leading causes of illness and mortality in women worldwide. Despite the effectiveness of conventional treatments such as surgery chemotherapy (CT) endocrine therapy (ET) radiation therapy (RT) and targeted therapies these approaches often fall short in providing a cure for advanced-stage patients and frequently result in adverse side effects. This limitation drives the ongoing search for therapeutic natural compounds with minimal or no side effects. Alkaloids in particular have garnered attention for their broad spectrum of therapeutic properties against various malignancies including breast cancer. The objective of this review is to systematically evaluate the therapeutic potential of 14 selected alkaloids that have been tested in in vitro and some in vivo models of breast cancer along by focusing on their mechanistic actions targeting key molecular signaling pathways involved in breast cancer progression. Majorly the capability of alkaloids to induce cell cycle arrest pro-apoptotic mechanisms via modulating various molecular signaling pathways were discussed. Notably pathways such as the intrinsic and extrinsic mitochondrial apoptotic pathways PI3K/AKT/mTOR RAS/RAF/MEK/MAPK Wnt/β-catenin and NF-κB cascades were highlighted. Insights into conclusion the isoquinoline and indole derivatives particularly berberine piperine capsaicin matrine and harmine have demonstrated significant potential effects and these compounds also exhibited the ability to overcome drug resistance and shown synergistic effects with conventional therapies. Finally this comprehensive review could provide an overall insight into the application of these alkaloid compounds towards the prevention of breast cancer and a foundation for future studies aimed at improving their clinical effectiveness offering valuable prospects.
Nature's Arsenal: Exploring the Anticancer Properties of Bioactive Compounds from Natural Sources
Considering that cancer is a disease that affects people all over the world there has been a movement in the focus of scientific and research efforts towards substances that are acquired from natural sources. It has been demonstrated that the identification of pharmaceuticals originating from plants has proven to be particularly beneficial in the process of producing anticancer therapies such as vincristine vinblastine paclitaxel and irinotecan. Additionally marine sources have provided substances such as cytarabine and aplidine and microbes have developed important drugs such as dactinomycin doxorubicin and bleomycin with their anticancer qualities. The purpose of this review is to highlight the fact that active components derived from natural sources present significant opportunities for the discovery of not only completely new categories of anticancer medicines but also novel precursor chemical compounds. The purpose of this article is to review naturally isolated anticancer medications from a wide range of agents that can be derived from a wide range of natural resources such as bacteria marine organisms and plants.
A Brief Review-An Update on 1,3,4-Oxadiazole
The 134-oxadiazole nucleus is a biologically necessary scaffold that exhibits a wide range of pharmacological activities. The broad and strong activity of 134-oxadiazole and their derivatives has established them as significant pharmacological scaffolds particularly in the treatment of cancer disease. A number of di- tri- aromatic and heterocyclic substituted 134-oxadiazole derivatives have been reported to possess potent biological activities; these substituted 134-oxadiazoles had different mechanisms of action and contributed to the development of biologically active drugs. This review is intended to supplement previous reviews by reviewing the literature on the different activities of 134-oxadiazole derivatives from the last fifteen years. 134-oxadiazole can be produced in a number of ways and has a wide range of possible pharmacological uses. As a result scientists have created novel procedures for the production of 134-oxadiazole derivatives and their use in medicine presently. Anticancer antibacterial anti-inflammatory anti-HIV anti-tubercular anti-diabetic antifungal and other properties are among the activities. In this review we discussed various research works based on 134-oxadiazole derivatives synthetic procedure and assessment of different biological activities. Many researchers may find the material on this page helpful which could lead to the discovery of new medicinal species for society.
Botanical Bounty: Exploring Aphrodisiac Drug Discovery and Development from Nature's Pharmacy
Ayurveda Siddha and Unani are some important traditional healing systems of India having long back evidence-based rejuvenation therapies addressing various infertility and reproductive disorders. Surprisingly the United Nations has revealed data on infertility that show that it affects around one in every six individuals highlighting the utmost importance of actively questioning and confronting the misunderstanding and lack of discussion related to infertility. Even though allopathic drugs like Clomiphene citrate Anastrozole Letrozole Human Chronic Gonadotropin (hCG) and Human Menopausal Gonadotropin (hPG) are available on the market there are a range of traditional and indigenous medical techniques that have been used for millennia to promote and cure health including Ayurveda Siddha and Unani to deliver safe and potent drugs having reproductive rejuvenation with proven evidence. Various botanicals are proven to heal both male and female infertility issues with clinical evidence due to the presence of various potent phytochemicals. Hence this review critically assesses the evidence-based literature focused on the mapping of botanical sources phytochemicals reproductive pharmacology and their clinical evidence.
An Overview of the Phytochemical and Therapeutic Potential of Wrightia tinctoria
Several natural phytomedicines derived from Chinese herbs demonstrate a wide range of pharmacological effects. Wrightia tinctoria (WT) is a small deciduous tree known as sweet indrajao. It belongs to the Apocynaceae family. Many diseases have been treated with this plant's phytoconstituents such as skin disorders dysenteric diarrhea and hair treatments. In addition the therapeutic elements of WT demonstrate significant anti-inflammatory and anti-dandruff properties. However there is a difference between this plant's preclinical and clinical significance. The purpose of this study is to collect and evaluate the various chemical medicinal and pharmacological characteristics of WT in relation to multiple disorders using preclinical evidence. This will serve as a valuable foundation for researchers to explore its effectiveness in clinical trials further.
A comprehensive search was conducted across several databases including PubMed Web of Science Scopus Academic Journals Embase Google Scholar and Science Direct. The search utilized specific keywords such as “Wrightia tinctoria” as well as terms like “Traditional Chinese Medicine” “Pharmacological activities” “Anti-cancer” “Anti-viral” “Anti-microbial” “Anti-psoriatic” “Anti-Inflammatory” “Quercetin” and their combinations mainly from 1993 to 2024.
The pharmacological and therapeutic potential of WT is gathered and summarized based on existing research reports. WT substances consist of various phytoconstituents including flavonoids steroids alkaloids volatile oils esters and others. These components are primarily responsible for the various pharmacological effects of WT such as anti-oxidant anti-bacterial anti-fungal anti-diabetic anti-cancer anti-microbial anti-inflammatory and anti-ulcer effects.
This review focuses on current research findings regarding WT's therapeutic potential and pharmacological activities. Additionally it addresses the major safety and toxicity issues related to WT.
Exploring the Therapeutic Potential of Bixa orellana L. Phytochemicals in Oxidative Stress and Complications using Network Pharmacology
This study explores the therapeutic potential of Bixa orellana (B. orellana) focusing on its bioactive compounds and antioxidant effects. Phytochemical analysis combined with network pharmacology was employed to investigate its multi-targeted therapeutic potential against oxidative stress.
The antioxidant activity of B. orellana flower extract was determined using DPPH assays. High-performance thin-layer chromatography (HPTLC) and liquid chromatography-mass spectrometry (LC-MS) were performed to profile key bioactive constituents. Network pharmacology analysis linked to these phytochemicals was performed to determine its role in oxidative stress and associated complications.
The results showed a significant DPPH activity of the flower extract of B. orellana. HPTLC profiling showed several major and minor metabolites at different Rf values while LC-MS profiling revealed quercetin kaempferol genestin etc. as key components of the flower extract. In network pharmacology analysis quercetin showed a significant interaction with genes like TP53 NOS2 and CAT while kaempferol targeted SOD2 and NFE2L2 both crucial in oxidative stress regulation. The results highlight the multi-targeted approach of B. orellana flower extract compounds in modulating oxidative stress pathways.
This comprehensive approach revealed multiple molecular pathways influenced by B. orellana compounds providing a strong foundation for their therapeutic potential in oxidative stress-related diseases.
Drug Delivery through Co-amorphous Solid Dispersions: A Comprehensive and Updated Review on Physicochemical Characteristics and Biological Potential
New chemical entities with low aqueous solubility and permeability encounter significant challenges in formulation development. Low solubility is further accompanied by slow dissolution and poor bioavailability which in turn leads to unpredictability in terms of both bioavailability and toxicity. Therefore a significant amount of exertion is necessary to enhance solubility dissolution and eventually bioavailability. Additionally to enhance the solubility properties and amorphous stability of BCS Class II medications and ultimately increase drug bioavailability co-amorphization has emerged as a promising strategy. Co-amorphous solid dispersions (CASD) are multi-component single-phase amorphous solid dispersions comprising two or more small molecules (usually known as co-formers) that might be a combination of drug-drug or drug-excipients. The selection of appropriate co-formers is critical and the surface properties of co-amorphous formulations must be carefully evaluated as they influence physical and chemical stability in addition to dissolution performance. Scaling up and processing co-amorphous formulations into the final dosage forms presents challenges that need to be addressed. This review will largely concentrate on the challenges improvements and innovations in physicochemical properties biological characterization and advancements of co-amorphous systems. This review will also furnish a comprehensive explanation of both established and emerging approaches utilized in the estimation of physicochemical attributes and characterization of CASD (in vitro and in vivo). Regarding CASD’s potential to improve patient outcomes and therapeutic efficacy it has emerged as a viable approach for drug candidates posing the problems of solubility and bioavailability. This approach has also increased the physical stability of drugs.
Beyond the Surface: The Role of Implantable Drug Delivery Systems in Modern Medicine
Advanced drug delivery methods have emerged mainly because of the limitations of traditional drug delivery systems like oral and intravenous routes along with fluctuating concentrations of drugs that have compromised therapeutic outcomes. An implantable drug delivery system (IDDS) presents an attractive alternative: long-term continuous drug release improves therapeutic efficacy while minimizing toxicity and side effects. IDDS first presented in the 1930s as subcutaneous hormone pellets have gained much attention recently in drug delivery due to their controlled release of drugs in a localized and sustained manner. In systemic treatments drugs administered through IDDS evade first-pass metabolism and enzymatic degradation within the gastrointestinal tract therefore enhancing drug bioavailability. The most suitable properties of IDDS are its application with drugs that have poor stability or solubility in oral formulations. Even though implantation is invasive the benefits of infrequent administration higher patient compliance and being able to discontinue therapy when side effects are present far outweigh the disadvantages. Today IDDSs are used in a myriad of therapeutic areas: contraception chemotherapy and pain management to name a few. Future developments in such technologies fine-tuning these systems further will revolutionize drug therapy by bringing even better and more patient-friendly drugs with both better efficacy and sustained periods of effects.
Isoquinoline Quaternary Alkaloid (IQA) Nano-dressings: A Comprehensive Review on Design Strategies, Therapeutic Applications, and Advancements in Transdermal Delivery for Chronic Wound Management
Transdermal delivery systems and wound dressings are essential components of modern healthcare with ongoing efforts focused on enhancing their efficacy biocompatibility and cost-effectiveness. Among emerging innovations natural compounds particularly those derived from plants have shown great promise. Isoquinoline Quaternary Alkaloids (IQAs) are one such class of compounds with notable therapeutic properties warranting exploration for advanced wound care applications.
This review investigates the design fabrication techniques and therapeutic potential of IQA-based nano dressings. It also provides a comparative analysis of these novel systems against conventional wound care methods to assess their advantages and clinical relevance.
Dissolving IQA nano dressings exhibit transformative potential in chronic wound management. Their intrinsic properties such as antimicrobial and anti-inflammatory activity biocompatibility and sustained drug release support enhanced wound healing and reduced treatment burden.
Compared to traditional approaches IQA nano dressings offer improved outcomes and patient compliance positioning them as a potential paradigm shift in wound care. By integrating nanotechnology with the unique pharmacological attributes of IQAs these nano dressings demonstrate significant promise in promoting tissue regeneration while minimizing dressing frequency. This innovation holds the potential to revolutionize chronic wound treatment through safer more effective and patient-friendly therapeutic strategies.
Formulation and Evaluation of Canagliflozin Hemihydrate-loaded Nanostructured Lipid Carriers Using Box-Behnken Design: Physicochemical Characterization, Ex-vivo Analysis, and In-vivo Pharmacokinetics
Type 2 Diabetes Mellitus (T2DM) is a prevalent metabolic disease significantly impacting healthcare characterized by increased blood glucose levels from the average level due to insulin resistance or a lack of insulin production. Canagliflozin Hemihydrate (CGN) is one of the drugs of choice in the treatment of the disease. However CGN belongs to BCS class IV making it difficult to formulate into suitable dosage form. The purpose of the present study was to systematically optimize and explore the potential of Nanostructured Lipid Carriers (NLCs) to improve the solubility and bioavailability of CGN.
The emulsification and ultrasonication methods were used for the preparation of CGN-loaded NLCs (CGN-NLCs) by employing the Box-Behnken design. The solid lipid to liquid lipid ratio (X1) surfactant concentration (X2) and sonication time (X3) were independent variables while particle size (Y1) and entrapment efficiency (EE) (Y2) were selected as dependent variables.
The optimized batch showed particle size zeta potential Polydispersity Index (PDI) and EE of 221.2 ± 2.25 nm -37 mV 0.268 ± 0.024 and 98.2 ± 1.62%. The TEM revealed a homogeneous spherical shape of CGN-NLCs. Further the DSC and XRD studies revealed reduced crystallinity with complete encapsulation of CGN in NLCs. The in vitro drug release study in simulated intestinal fluid (pH 6.8) showed significant CGN release from CGN-NLCs compared to CGN dispersion. Further the ex vivo intestinal permeability and in vivo pharmacokinetic study showed a 1.33-fold and 3.81-fold increase in permeability and bioavailability along with improvement in Cmax Tmax and [AUC]0–24 as compared to CGN dispersion.
Thus the prepared CGN-NLCs could be a better viable option for T2DM with improved therapeutic efficacy.
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Neuroprotective Effect of Naturally Occurring Flavonoids
Flavonoids have a wide range of neuroprotective effects on the brain including the capacity to reduce neuroinflammation shield neurons from harm caused by neurotoxins and maybe improve memory learning and cognitive function. These functions are most likely a result of two similar mechanisms. Inhibiting neurotoxic substance-induced apoptosis and promoting synaptic plasticity and neuronal survival are achieved by first interacting with key protein and lipid kinase signaling pathways in the brain. Second they have positive effects on the vascular system that alter cerebrovascular blood flow and can result in angiogenesis neurogenesis and morphological alterations in neurons. Through these pathways eating foods high in flavonoids has the potential to avoid or delay age-related impairments in cognitive abilities as well as neurodegeneration. Due to the high level of interest in creating new pharmaceuticals that might improve the cognitive function of the brain Flavonoids could be important preparatory substances in the development of a new class of brain-improving drugs.