Synthesis of 5-substituted-1,3,4-oxadiazole clubbed pyrazole and dihydropyrimidine derivatives as potent bioactive agents

2021 ◽  
Vol 10 (1) ◽  
pp. 13
Author(s):  
Bonny Y. Patel ◽  
Tushar J. Karkar ◽  
Malay J. Bhatt
Keyword(s):  
Bioactive Agents

Drug Delivery Systems Based on Titania Nanotubes and Active Agents for Enhanced Osseointegration of Bone Implants

2020 ◽  
Vol 27 (6) ◽  
pp. 854-902 ◽  
Author(s):  
Raluca Ion ◽  
Madalina Georgiana Necula ◽  
Anca Mazare ◽  
Valentina Mitran ◽  
Patricia Neacsu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Tio2 Nanotubes ◽  
Therapeutic Agent ◽  
Bone Defects ◽  
Delivery Systems ◽  
Antimicrobial Compounds ◽  
Bone Implant ◽  
Bioactive Agents ◽  
Localized Drug Delivery ◽  
Regeneration Of Bone

TiO2 nanotubes (TNTs) are attractive nanostructures for localized drug delivery. Owing to their excellent biocompatibility and physicochemical properties, numerous functionalizations of TNTs have been attempted for their use as therapeutic agent delivery platforms. In this review, we discuss the current advances in the applications of TNT-based delivery systems with an emphasis on the various functionalizations of TNTs for enhancing osteogenesis at the bone-implant interface and for preventing implant-related infection. Innovation of therapies for enhancing osteogenesis still represents a critical challenge in regeneration of bone defects. The overall concept focuses on the use of osteoconductive materials in combination with the use of osteoinductive or osteopromotive factors. In this context, we highlight the strategies for improving the functionality of TNTs, using five classes of bioactive agents: growth factors (GFs), statins, plant derived molecules, inorganic therapeutic ions/nanoparticles (NPs) and antimicrobial compounds.

Potential Pharmaceutical and Food Applications of Postbiotics: A Review

2020 ◽  
Vol 21 (15) ◽  
pp. 1576-1587 ◽  
Author(s):  
Aziz H. Rad ◽  
Amin Abbasi ◽  
Hossein S. Kafil ◽  
Khudaverdi Ganbarov
Keyword(s):  
Functional Foods ◽  
Animal Health ◽  
Pharmaceutical Formulations ◽  
Live Cells ◽  
Beneficial Effects ◽  
Safe Product ◽  
Potential Applications ◽  
Food Applications ◽  
Potential Alternative ◽  
Bioactive Agents

In recent decades, functional foods with ingredients comprising probiotics, prebiotics and postbiotics have been gaining a lot of attention from scientists. Probiotics and postbiotics are usually applied in pharmaceutical formulations and/or commercial food-based products. These bioactive agents can be associated with host eukaryotic cells and have a key role in maintaining and restoring host health. The review describes the concept of postbiotics, their quality control and potential applications in pharmaceutical formulations and commercial food-based products for health promotion, prevention of disease and complementary treatment. Despite the effectiveness of probiotic products, researchers have introduced the concept of postbiotic to optimize their beneficial effects as well as to meet the needs of consumers to provide a safe product. The finding of recent studies suggests that postbiotics might be appropriate alternative agents for live probiotic cells and can be applied in medical, veterinary and food practice to prevent and to treat some diseases, promote animal health status and develop functional foods. Presently scientific literature confirms that postbiotics, as potential alternative agents, may have superiority in terms of safety relative to their parent live cells, and due to their unique characteristics in terms of clinical, technological and economical aspects, can be applied as promising tools in the drug and food industry for developing health benefits, and therapeutic aims.

Therapeutic Aspects of Squill; An Evidence-Based Review

2020 ◽  
Vol 17 (3) ◽  
pp. 318-324 ◽  
Author(s):  
Khadije Saket ◽  
Jalil T. Afshari ◽  
Ehsan Saburi ◽  
Mahdi Yousefi ◽  
Roshanak Salari
Keyword(s):  
Side Effects ◽  
Traditional Medicine ◽  
Respiratory Diseases ◽  
Low Cost ◽  
Current Evidence ◽  
Evidence Based ◽  
Helminthic Infections ◽  
Traditional Persian Medicine ◽  
Healing Of Wounds ◽  
Bioactive Agents

From ancient times, medicinal plants have been usually utilized to treat many disorders, but today, interest in these herbs is again aroused, because of their fewer side effects and low-cost. In traditional medicine, for many diseases, various medicinal herbs have been suggested so far. Drimia maritime, also named squill, is an important medicinal plant for the treatment of many diseases, especially respiratory diseases. In the current evidence-based study, we conducted a review of the general characteristics, ingredients, administration form, and side effects of squill in traditional medicine. For this purpose, traditional Persian medicine literatures and electronic databases were examined including PubMed, Scopus, and Google Scholar. Many compounds are isolated from D.maritima, including scillaren, scillirubroside, scillarenin, and bufadienolide glycosides. Oxymel is the most commonly used form of squill for various diseases, especially respiratory diseases. Besides, squill has been used in the treatment of cardiovascular, digestive, and dermatological disorders, it is also used against various cancer cells for its antioxidant and cytotoxic properties. Moreover, there is relatively reliable evidence of its benefits for bacterial and helminthic infections, rheumatism, edema, gout, abortion induction, healing of wounds and urine induction. It seems that supplementary studies are required to explore the bioactive agents and their effective mechanisms.

Hybrids of Coumarin Derivatives as Potent and Multifunctional Bioactive Agents: A Review

2020 ◽  
Vol 16 (3) ◽  
pp. 272-306
Author(s):  
Ioannis Fotopoulos ◽  
Dimitra Hadjipavlou-Litina
Keyword(s):  
Pharmacological Activity ◽  
Biological Activities ◽  
Structural Characteristics ◽  
Pharmacokinetic Profile ◽  
Biologically Active ◽  
Hybridization Technique ◽  
Coumarin Derivatives ◽  
Hybrid Molecules ◽  
Pharmacokinetic Properties ◽  
Bioactive Agents

Background: Coumarins exhibit a plethora of biological activities, e.g. antiinflammatory and anti-tumor. Molecular hybridization technique has been implemented in the design of novel coumarin hybrids with several bioactive groups in order to obtain molecules with better pharmacological activity and improved pharmacokinetic profile. Objective: Therefore, we tried to gather as many as possible biologically active coumarin hybrids referred in the literature till now, to delineate the structural characteristics in relation to the activities and to have a survey that might help the medicinal chemists to design new coumarin hybrids with drug-likeness and varied bioactivities. Results: The biological activities of the hybrids in most of the cases were found to be different from the biological activities presented by the parent coumarins. The results showed that the hybrid molecules are more potent compared to the standard drugs used in the evaluation experiments. Conclusion: Conjugation of coumarin with varied pharmacophore groups/druglike molecules responsible for different biological activities led to many novel hybrid molecules, with a multitarget behavior and improved pharmacokinetic properties.

Smart Gn-Keto Nanohybrid Embedded Topical System for Effective Management of Dermatophytosis

2019 ◽  
Vol 9 (1) ◽  
pp. 21-28
Author(s):  
Nisha Sharma ◽  
Shashikiran Misra
Keyword(s):  
Antifungal Activity ◽  
Fungal Infections ◽  
High Surface ◽  
High Surface Area ◽  
Vital Role ◽  
Common Disease ◽  
Microdilution Method ◽  
Enhanced Solubility ◽  
Bioactive Agents

Background and Objectives: Dermatophytosis (topical fungal infection) is the 4th common disease in the last decade, affecting 20-25% world’s population. Patients of AIDS, cancer, old age senescence, diabetes, cystic fibrosis become more vulnerable to dermatophytosis. The conventional topical dosage proves effective as prophylactic in preliminary stage. In the advanced stage, the therapeutics interacts with healthy tissues before reaching the pathogen site, showing undesirable effects, thus resulting in pitiable patient compliance. The youngest carbon nano-trope “Graphene” is recently used to manipulate bioactive agents for therapeutic purposes. Here, we explore graphene via smart engineering by virtue of high surface area and high payload for therapeutics and developed graphene–ketoconazole nanohybrid (Gn-keto) for potent efficacy towards dermatophytes in a controlled manner. </P><P> Methods: Polymethacrylate derivative Eudragit (ERL100 and ERS 100) microspheres embedded with keto and Gn-keto nanohybrid were formulated and characterized through FTIR, TGA, and SEM. In vitro drug release and antifungal activity of formulated Gn-keto microspheres were assessed for controlled release and better efficacy against selected dermatophytes. </P><P> Results: Presence of numerous pores within the surface of ERL100 microspheres advocated enhanced solubility and diffusion at the site of action. Controlled diffusion across the dialysis membrane was observed with ERS100 microspheres owing to the nonporous surface and poor permeability. Antifungal activity against T. rubrum and M. canis using microdilution method focused on a preeminent activity (99.785 % growth inhibition) of developed nanohybrid loaded microspheres as compared to 80.876% of keto loaded microspheres for T. rubrum. The culture of M. canis was found to be less susceptible to formulated microspheres. Conclusion: Synergistic antifungal activity was achieved by nanohybrid Gn-Keto loaded microspheres against selected topical fungal infections suggesting a vital role of graphene towards fungi.

Momordica balsamina L.: An Appraisal on Morphology, Ecological Diversity, Phytochemistry, Pharmacological and Biotechnological Applications

2020 ◽  
Vol 06 ◽  
Author(s):  
Saheed Sabiu ◽  
Christiana Eleojo Aruwa ◽  
Viresh Mohanlall ◽  
Himansu Baijnath
Keyword(s):  
Relevant Information ◽  
Perennial Herb ◽  
Biotechnological Applications ◽  
Tropical Regions ◽  
Toxicological Data ◽  
Human Disorders ◽  
Potential Applications ◽  
Baseline Information ◽  
The Caribbean ◽  
Bioactive Agents

Background: Momordica balsamina L. is a monoecious climbing vine and perennial herb native to the tropical regions of Asia, Arabia and the Caribbean, and with prominent presence in Nigeria, Botswana, Namibia, Swaziland and Southern African provinces. While evidence of its anecdotal usage as medicine exist, scientific reports complementing the claims are still emerging or at their infancy. Objective: This review appraised the morphology, therapeutic and biotechnological significance of M. balsamina. Method: Online resources such as Google Scholar, PubMed, ScienceDirect and MeSH were utilized for literature search and included relevant information from inception till May 2020 to streamline sought outcomes for in-depth discussion. Results: The data gathered and considered worthy of inclusion in this study revealed that M. balsamina is rich in phytonutrients of medicinal significance with cucurbitane-type triterpenoids, balsamin and momordins well characterized and fully elucidated. These compounds and other novel bioactive agents in M. balsamina have found remarkable pharmacological relevance and could further be harnessed for use against several debilitating human disorders. Conclusion: The potential applications of M. balsamina as nutraceutical and pharmaceutical agent should not be undermined. Also, with the inadequate toxicological data on this wild species, its consumption should be with caution and translational studies that could advance scientific knowledge and aid better understanding of both its pharmacokinetics and pharmacodynamics without sidelining its potent biotechnological applications are highly encouraged. It is hoped that this paper will provide baseline information that could serve as a guide and inspiration for further studies on the prospects of M. balsamina.

A Comprehensive Review On Alginate As Wound Dressing Biomaterial

2020 ◽  
Vol 04 ◽  
Author(s):  
Sourav Mohanto ◽  
Prithviraj Chakraborty ◽  
Chidambaram Soundra Pandian ◽  
Shubhradeep Manna ◽  
Joni Dutta
Keyword(s):  
Therapeutic Efficacy ◽  
Wound Dressing ◽  
Chronic Wound ◽  
Healing Process ◽  
Wound Healing Process ◽  
Detailed Knowledge ◽  
Pathophysiological Mechanisms ◽  
Moist Environment ◽  
Bioactive Agents ◽  
Mechanical Nature

Background: The design and characteristics of alginate biomaterial have a significant role in wound dressing and tissue regeneration. The ideal biomaterial for wound dressing must have biodegradable, biocompatible, non-inflammatory, non-toxic. Objective: Wound dressing should promote the re-epithelization and protect the wound for further infection by creating a moist environment. The physical and mechanical nature of the alginate biopolymer has the potential to influence the pathophysiological mechanisms in the chronic wound actively. The application of this biomaterial provides an ampule advantage to synthetic polymers. Method: The wound healing process is a critical step involved in different phases. The presence of cross-linkers, polymers along with alginate lead to a decrease in the mechanical property of dressing. Hence the effective material choosing along with alginate is a very critical decision. The therapeutic efficacy of the alginate dressing system (film, hydrogel, wafer, etc.) influenced by the incorporation of different materials such as bioactive agents, nanoparticles, cross-linker, nature of the excipients, etc. Results: The ion exchange occurring between dressing and exudates resulted in the formation of gel, due to the glucuronic acid presence in alginate. This gel absorbs moisture and maintains an appropriate moist environment and actively influence the pathophysiological mechanisms in the chronic wound. Conclusion: This review gives a detailed knowledge of the researchers to work with alginate and provides knowledge about the incorporation of the appropriate material and their therapeutic efficacy in wound dressing.

scholarly journals Targeting of GLUT5 for Transporter-Mediated Drug-Delivery Is Contingent upon Substrate Hydrophilicity

2021 ◽  
Vol 22 (10) ◽  
pp. 5073
Author(s):  
Nazanin Nahrjou ◽  
Avik Ghosh ◽  
Marina Tanasova
Keyword(s):  
Cancer Cells ◽  
Normal Breast ◽  
Proof Of Concept ◽  
Drug Conjugates ◽  
High Fructose ◽  
Specific Cytotoxicity ◽  
Breast Cells ◽  
Substrate Tolerance ◽  
Bioactive Agents ◽  
Positive Breast Cancer

Specific link between high fructose uptake and cancer development and progression highlighted fructose transporters as potential means to achieve GLUT-mediated discrimination between normal and cancer cells. The gained expression of fructose-specific transporter GLUT5 in various cancers offers a possibility for developing cancer-specific imaging and bioactive agents. Herein, we explore the feasibility of delivering a bioactive agent through cancer-relevant fructose-specific transporter GLUT5. We employed specific targeting of GLUT5 by 2,5-anhydro-D-mannitol and investigated several drug conjugates for their ability to induce cancer-specific cytotoxicity. The proof-of-concept analysis was carried out for conjugates of chlorambucil (CLB) in GLUT5-positive breast cancer cells and normal breast cells. The cytotoxicity of conjugates was assessed over 24 h and 48 h, and significant dependence between cancer-selectivity and conjugate size was observed. The differences were found to relate to the loss of GLUT5-mediated uptake upon increased conjugate size and hydrophobicity. The findings provide information on the substrate tolerance of GLUT5 and highlight the importance of maintaining appropriate hydrophilicity for GLUT-mediated delivery.

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