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result(s) for
"Pharmacological profile"
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Camptothecin and its derivatives: Advancements, mechanisms and clinical potential in cancer therapy
by
Pandhi, Shikha
,
Büsselberg, Dietrich
,
Kumar, Pradeep
in
Animals
,
Antineoplastic Agents, Phytogenic - pharmacology
,
Antineoplastic Agents, Phytogenic - therapeutic use
2024
Camptothecin (CPT), an alkaloid isolated from the
Camptotheca
tree, has demonstrated significant anticancer properties in a range of malignancies. However, its therapeutic efficacy is limited by its hydrophobicity, poor bioavailability, and systemic toxicity. Derivatives, analogues, and nanoformulations of CPT have been synthesized to overcome these limitations. The aim of this review is to comprehensively analyze existing studies to evaluate the therapeutic efficacy, mechanistic aspects, and clinical potential of CPT and its modified forms, including derivatives, analogues, and nanoformulations, in cancer treatment. A comprehensive literature review was performed using PubMed/Medline, Scopus, and Web of Science databases; articles were selected based on specific inclusion criteria, and data were extracted on the pharmacological profile, clinical studies, and therapeutic efficacy of CPT and its different forms. Current evidence suggests that derivatives and analogues of CPT have improved water solubility, bioavailability, and reduced systemic toxicity compared to CPT. Nanoformulations further enhance targeted delivery and reduce off-target effects. Clinical trials indicate promising outcomes with enhanced survival rates and lower side effects. CPT and its modified forms hold significant promise as potent anticancer agents. Ongoing research and clinical trials are essential for establishing their long-term efficacy and safety; the evidence overwhelmingly supports further development and clinical testing of these compounds.
Journal Article
Pharmacological Profile, Bioactivities, and Safety of Turmeric Oil
by
Orellana-Paucar, Adriana Monserrath
,
Machado-Orellana, María Gabriela
in
Alzheimer's disease
,
Antioxidants
,
Arthritis
2022
The pharmacological attributes of turmeric have been extensively described and frequently related to the action of curcuminoids. However, there is also scientific evidence of the contribution of turmeric oil. Since the oil does not contain curcuminoids in its composition, it is crucial to better understand the therapeutic role of other constituents in turmeric. The present review discusses the pharmacokinetics of turmeric oil, pointing to the potential application of its active molecules as therapeutic compounds. In addition, the bioactivities of turmeric oil and its safety in preclinical and clinical studies were revised. This literature-based research intends to provide an updated overview to promote further research on turmeric oil and its constituents.
Journal Article
The phytochemical and pharmacological profile of taraxasterol
2022
Taraxasterol is one of the bioactive triterpenoids found in dandelion, a member of the family Asteraceae. In the animal or cellular models of several ailments, including liver damage, gastritis, colitis, arthritis, pneumonia, tumors, and immune system diseases, taraxasterol has been shown to have significant preventive and therapeutic effects. This review aims to evaluate the current state of research and provide an overview of the possible applications of taraxasterol in various diseases. The reported phytochemical properties and pharmacological actions of taraxasterol, including anti-inflammatory, anti-oxidative, and anti-carcinogenic properties, and its potential molecular mechanisms in developing these diseases are highlighted. Finally, we further explored whether taraxasterol has protective effects on neuronal death in neurodegenerative diseases. In addition, more animal and clinical studies are also required on the metabolism, bioavailability, and safety of taraxasterol to support its applications in pharmaceuticals and medicine.
Journal Article
Pharmacological profile of dicaffeoylquinic acids and their role in the treatment of respiratory diseases
by
Hufnagel, Matthias
,
Franken, Sebastian
,
Häberlein, Hanns
in
Acids
,
Antioxidants
,
Biosynthesis
2024
Dicaffeoylquinic acids (DCQAs) are polyphenolic compounds found in various medicinal plants such as Echinacea species and Hedera helix, whose multi-constituent extracts are used worldwide to treat respiratory diseases. Besides triterpenes, saponins, alkamides, and other constituents, DCQAs are an important group of substances for the pharmacological activity of plant-derived extracts. Therefore, the pharmacological properties of DCQAs have been studied over the last decades, suggesting antioxidative, anti-inflammatory, antimicrobial, hypoglycaemic, cardiovascular protective, neuroprotective, and hepatoprotective effects. However, the beneficial pharmacological profile of DCQAs has not yet been linked to their use in treating respiratory diseases such as acute or even chronic bronchitis. The aim of this review was to assess the potential of DCQAs for respiratory indications based on published in vitro and in vivo pharmacological and pre-clinical data, with particular focus on antioxidative, anti-inflammatory, and respiratory-related effects such as antitussive or antispasmodic properties. A respective literature search revealed a large number of publications on the six DCQA isoforms. Based on this search, a focus was placed on 1,3-, 3,4-, 3,5-, and 4,5-DCQA, as the publications focused mainly on these isomers. Based on the available pre-clinical data, DCQAs trigger cellular mechanisms that are important in the treatment of respiratory diseases such as decreasing NF-κB activation, reducing oxidative stress, or activating the Nrf2 pathway. Taken together, these data suggest an essential role for DCQAs within herbal medicines used for the treatment of respiratory diseases and highlights the need for the identifications of DCQAs as lead substances within such extracts.
Journal Article
Budesonide Attains Its Wide Clinical Profile by Alternative Kinetics
2024
The introduction of inhaled corticosteroids (ICSs) changed over a few decades the treatment focus of mild-to-moderate asthma from bronchodilation to reduction in inflammation. This was achieved by inhaling a suitable corticosteroid (CS), giving a high, protracted airway concentration at a low total dose, thereby better combining efficacy and tolerance than oral therapy. Successful trials with the potent, lipophilic “skin” CS beclomethasone dipropionate (BDP) paved the way, suggesting that ICSs require a very low water solubility, prolonging their intraluminal dissolution within airways. The subsequent ICS development, with resulting clinical landmarks, is exemplified here with budesonide (BUD), showing that a similar efficacy/safety relationship is achievable by partly alternative mechanisms. BUD is much less lipophilic, giving it a 100-fold higher water solubility than BDP and later developed ICSs, leading to its more rapid intraluminal dissolution and faster airway and systemic uptake rates. In airway tissue, a BUD fraction is reversibly esterified to intracellular fatty acids, a lipophilic conjugate, which prolongs airway efficacy. Another mechanism is that the rapidly absorbed bulk fraction, via short plasma peaks, adds anti-inflammatory activity at the blood and bone marrow levels. Importantly, these plasma peaks are too short to provoke systemic adverse actions. Controlled clinical trials with BUD changed the use of ICS from a last resort to first-line treatment. Starting ICS treatment immediately after diagnosis (“early intervention”) became a landmark for BUD. An established dose response made BUD suitable for the treatment of patients with all degrees of asthma severity. With the development of the budesonide/formoterol combination inhaler (BUD/FORM), BUD contributed to the widely used BUD/FORM maintenance and reliever therapy (MART). Recent studies demonstrated the value of BUD/FORM as a generally recommended as-needed therapy for asthma (“anti-inflammatory reliever”, AIR). These abovementioned qualities have all influenced international asthma management and treatment guidelines.
Journal Article
Synthetic approaches, emerging applications, and challenges of indole-based five-membered heterocycles in medicinal chemistry
2025
Scientists are fascinated by the indole structure due to its diverse biological activities, encompassing both indole itself and its numerous substituted derivatives. Heterocycles, particularly those containing indoles, play pivotal roles in the domains of medicinal chemistry, drug designing and discovery, agrochemicals, photochemistry, dyes, and other applications, which has led to their prominence in the chemistry field. This review highlights the diverse applications of indole-based five-membered heterocycles as versatile scaffolds for drug development, emphasizing their therapeutic potential as antidiabetic, anti-inflammatory, anticancer, antimicrobial, antioxidant agents, antialzheimer and anticonvulsant agents. A comprehensive literature search was carried out to explore the chemical, biological, and structural activity correlations of indole-based hybrids. Studies published between 2017 and 2024 were chosen from databases such as PubMed, Scopus and Google Scholar, emphasizing the synthesis, activity and application of indole-based heterocycles in medicinal chemistry. Unique to this review is the exploration of structure–activity relationships (SAR), synthetic approaches and emerging challenges in the development of indole-based drugs. Key insights include innovative strategies to enhance biological efficacy through structural modifications and various applications of indole-based derivatives in therapeutic areas. These findings hold great potential for improving the design of more effective pharmaceuticals.
Journal Article
Overview for Various Aspects of the Health Benefits of Piper Longum Linn. Fruit
2011
Herbal remedies have become popular, due in part to the lower risk of adverse reactions. Thousands of plants have been used traditionally to treat various diseases. Among them, species of the genus Piper are important medicinal plants used in various systems of medicine. The Piper longum fruit has been used in traditional medicine, including the Ayurvedic system of medicine. Although there are numerous indications for its use, controlled trials are needed to determine its efficacy. The primary constituents isolated from various parts of P. longum are piperine, piperlongumine, sylvatin, sesamin, diaeudesmin piperlonguminine, pipermonaline, and piperundecalidine. It is most commonly used to treat chronic bronchitis, asthma, constipation, gonorrhea, paralysis of the tongue, diarrhea, cholera, chronic malaria, viral hepatitis, respiratory infections, stomachache, bronchitis, diseases of the spleen, cough, and tumors. This study provides detailed information about the P. longum fruit, including phytochemistry, pharmacological profile and safety profile. In view of the commercial, economic, and medicinal importance of the P. longum plant, it is useful for researchers to study the plant in detail.
Journal Article
Pharmacological profile of Shiva Gutika : an uncharted and versatilepolyherbal drug
by
Jayanthi, M. K.
,
Pushpa, V. H.
,
Patil, Shashank M.
in
Diabetes mellitus
,
Dyslipidemia
,
Medicinal plants
2021
Polyherbal drugs have been regarded as the most advantageous results of Ayurveda as they consist of numerous phytoconstituents with ameliorative effects on body metabolism. The resultant synergistic effect of these formulations has been remarked with pharmacological efficiency as well as minimal toxic effects. In the context, Shiva Gutika proves to be an effective treatment against some uncommon health maladies like spondyloepiphyseal dysplasia tarda (SEDT), HIV-AIDS and dyslipidemia. The phytochemical profiling of Shiva Gutika depicts the uncommon combination of phytochemicals extracted from different medicinal plants. However, much the pharmacological effect of Shiva Gutika on diseases like cancer and diabetes mellitus are poorly understood and still needs to be elucidated. The present commentary highlights the importance of Shiva Gutika by emphasizing on its phytochemical profile and pharmacological activity on some uncommon morbidities as mentioned above. The commentary also projects the essential factors that need to be concerned to use Shiva Gutika as an efficient replacement to the conventional therapeutic agents.
Journal Article
Exploring the therapeutic potential of Ixora extract: a comprehensive review of mediated studies
by
Younas, Umer
,
Imran, Muhammad
,
Pervaiz, Muhammad
in
Biomedical and Life Sciences
,
Biomedicine
,
Pharmacy
2025
Traditional Herbal Medicine Systems, commonly known as Complementary and Alternative Systems of Medicine, is currently one of the most extensively researched subjects. The genus
Ixora
belongs to the family Rubiaceae, which is commonly referred to as the Madder family. It comprises 500 species and is one of the most investigated herbs today. For centuries, ethnic groups have incorporated various parts of the
Ixora
plant (flowers, leaves, stems, and roots) into Ayurvedic medicine to treat a range of ailments, including hepatic disorders, diarrhea, cancer, tumors, microbial infections, antioxidants, pain, ulcers, anti-tumor properties, and anti-inflammatory effects. Due to the extensive use of the
Ixora
genus in traditional medicine, researchers were compelled to examine the phytochemical composition of its various species. Multiple studies on the genus
Ixora
, which belongs to the Rubiaceae family, have uncovered a rich assortment of phenolic compounds. These include flavonoids, tannins, aromatic acrid oils, poly-sterols, saponins, carbohydrates, fatty acids, peptides, and terpenoids. Over the past 50 years, extensive phytochemical studies have been conducted on the genus
Ixora
, these studies have not only revealed the composition of the plant extract, but they have also helped to develop a comprehensive pharmacological profile. In doing so, these studies have provided scientific evidence supporting the ethno-medicinal uses of the plant. Every part of various
Ixora
species is said to possess beneficial properties which have added to its value as a medicinal plant. The purpose of this review is to thoroughly analyze the phytochemical and pharmacological properties of the
Ixora
genus. Along the way present an updated and categorized compilation of the scientific evidence of its medicinal properties. As a result, it aims to inspire scholars to pursue additional research on this particular genus.
Graphical abstract
Journal Article
Psychotropic Drugs for the Management of Chronic Pain and Itch
by
Belinskaia, Mariia A.
,
Barygin, Oleg I.
,
Shestakova, Natalia N.
in
Analgesics
,
animal model
,
Anticonvulsants
2019
Clinical observations have shown that patients with chronic neuropathic pain or itch exhibit symptoms of increased anxiety, depression and cognitive impairment. Such patients need corrective therapy with antidepressants, antipsychotics or anticonvulsants. It is known that some psychotropic drugs are also effective for the treatment of neuropathic pain and pruritus syndromes due to interaction with the secondary molecular targets. Our own clinical studies have identified antipruritic and/or analgesic efficacy of the following compounds: tianeptine (atypical tricyclic antidepressant), citalopram (selective serotonin reuptake inhibitor), mianserin (tetracyclic antidepressant), carbamazepine (anticonvulsant), trazodone (serotonin antagonist and reuptake inhibitor), and chlorprothixene (antipsychotic). Venlafaxine (serotonin-norepinephrine reuptake inhibitor) is known to have an analgesic effect too. The mechanism of such effect of these drugs is not fully understood. Herein we review and correlate the literature data on analgesic/antipruritic activity with pharmacological profile of these compounds.
Journal Article