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Found 756 Results / Page 4 of 51
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Ultrashort All-Hydrocarbon Stapled α-Helix Amphiphile as a Potent and Stable Antimicrobial Compound
2023 / Journal of Medicinal ChemistryThe ravaging effect of drug-resistant bacteria has heightened the need for the development of membrane-soluble antimicrobial peptides (AMPs). However, their potential for clinical use is hindered by issues such as poor biocompatibility, salt sensitivity, and proteolytic lability. In this study, a series of ultrashort stapled cyclization heptapeptides were obtained ...
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Perspective use of bio-adhesive liquid crystals as ophthalmic drug delivery systems
2023 / Scientific ReportsThe success of many drugs in ophthalmic treatments is hindered by their physico-chemical properties and the limited precorneal retention time. Here, lyotropic liquid crystals are proposed as a new ophthalmic drug delivery system. Acyclovir was chosen as model drug for its solubility and its controlled release from cubic phase was achieved. We demonstrated the eff...
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Structure-Based Design and Synthesis of Stapled 10Panx1 Analogues for Use in Cardiovascular Inflammatory Diseases
2023 / Journal of Medicinal ChemistryFollowing a rational design, a series of macrocyclic (“stapled”) peptidomimetics of 10Panx1, the most established peptide inhibitor of Pannexin1 (Panx1) channels, were developed and synthesized. Two macrocyclic analogues SBL-PX1-42 and SBL-PX1-44 outperformed the linear native peptide. During in vitro adenosine triphosphate (ATP) release and Yo-Pro-1 up...
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Synthesis and Preclinical Evaluation of [Methylpiperazine-11C]brigatinib as a PET Tracer Targeting Both Mutated Epidermal Growth Factor Receptor and Anaplastic Lymphoma Kinase
2023 / Journal of Medicinal ChemistryBrigatinib, a tyrosine kinase inhibitor (TKI) with specificity for gene rearranged anaplastic lymphoma kinase (ALK), such as the EML4–ALK, has shown a potential to inhibit mutated epidermal growth factor receptor (EGFR). In this study, N-desmethyl brigatinib was successfully synthesized as a precursor in five steps. Radiolabeling with [11C]methyl iodide produ...
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Four new lignans obtained from the leaves of Schisandra cauliflora and their effect on skeletal muscle cell proliferation
2023 / Journal of Natural MedicinesPlants of the Schisandra genus are commonly used in folk medicinal remedies. Some Schisandra species and their lignans have been reported to improve muscle strength. In the present study, four new lignans, named schisacaulins A–D, together with three previously described compounds ananonin B, alismoxide, and pregomisin were isolated from the leaves of S. caul...
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Novel Triazoles with Potent and Broad-Spectrum Antifungal Activity In Vitro and In Vivo
2023 / Journal of Medicinal ChemistryTriazoles have demonstrated significant efficacy in the treatment of fungal infections. However, increasing drug resistance is a growing concern that negatively impacts their effectiveness. By designing a well-crafted side chain, triazoles can be endowed with advantages, like higher potency and the ability to overcome drug resistance. This highlights the diverse in...
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Screening of promising chemotherapeutic candidates from plants against human adult T-cell leukemia/lymphoma (VIII): six new withanolides from Physalis philadelphica
2023 / Journal of Natural MedicinesAdult T-cell leukemia/lymphoma (ATL) is a malignancy of mature peripheral T-lymphocytes caused by human T-cell leukemia virus type I (HTLV-I). There are an estimated 5–20 million HTLV-1-infected individuals worldwide. Conventional chemotherapeutic regimens used against other malignant lymphomas have been administered to patients with ATL, but the therapeuti...
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Screening of promising chemotherapeutic candidates from plants against human adult T-cell leukemia/lymphoma (VIII): six new withanolides from Physalis philadelphica
2023 / Journal of Natural MedicinesAdult T-cell leukemia/lymphoma (ATL) is a malignancy of mature peripheral T-lymphocytes caused by human T-cell leukemia virus type I (HTLV-I). There are an estimated 5–20 million HTLV-1-infected individuals worldwide. Conventional chemotherapeutic regimens used against other malignant lymphomas have been administered to patients with ATL, but the therapeuti...
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Fighting Multidrug Resistance with Ruthenium–Cyclopentadienyl Compounds: Unveiling the Mechanism of P-gp Inhibition
2023 / Journal of Medicinal ChemistryThe search for more effective and selective drugs to overcome cancer multidrug resistance is urgent. As such, a new series of ruthenium-cyclopentadienyl (“RuCp”) compounds with the general formula [Ru(η5-C5H4R)(4,4′-R′-2,2′-bipy)(PPh3)] were prepared and fully characterized. All compounds were evaluated toward non-small cell lung c...
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Antibacterial activity of silver nanoparticle LED-synthesized using Citrus maxima peels
2023 / INTERNATIONAL JOURNAL OF PLANT BASED PHARMACEUTICALSSilver nanoparticles have garnered significant attention in research and applications due to their unique properties. The synthesis of these nanoparticles has aligned with the principles of green chemistry, utilizing environmentally-friendly materials and techniques. In this study, silver nanoparticles were synthesized using the Citrus maxima peel extract and blue ...
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Biocompatible topical delivery system of high-molecular-weight hyaluronan into human stratum corneum using magnesium chloride
2023 / Scientific ReportsNon-invasive delivery of hyaluronan into the stratum corneum (SC) is extremely difficult because of its high molecular weight and the strong barrier of the SC. We developed a safe method of administering hyaluronan into the human SC and determined its penetration route. The amount of hyaluronan that penetrated into the SC was 1.5–3 times higher in the prese...
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Thiophene Carboxamide Analogs with Long Alkyl Chains Comprising Ethylene Glycol Units Inhibit Glioblastoma Cell Proliferation by Activating AMPK
2023 / Journal of Medicinal ChemistryGlioblastoma is a refractory malignant tumor that requires novel therapeutic strategies for effective treatment. We have previously reported that JCI-20679 (1), an analog of annonaceous acetogenins, shows potent antitumor activity against glioblastomas. However, the synthesis of 1 requires 23 steps, including 16 steps for the preparation of a tetrahydrofuran (THF) ...
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Techno-economics feasibility of supercritical CO2 ambrette seed extraction for optimised parameters obtained using RSM
2023 / Journal of Applied Research on Medicinal and Aromatic PlantsSeeds of a native aromatic plant of India, Abelmoschus moschatus (Ambrette), Malvaceae family, were considered for extraction and techno-economic evaluation in this study considering the commercial importance of unique volatile oil in the seed coat. Supercritical fluid extraction (SFE) using CO2 as the extraction fluid was performed at different process parameters....
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Phototunable Cell Killing by Photochromic Diarylethene of Thiazoyl and Thienyl Derivatives
2023 / Journal of Medicinal ChemistryWe report a unique phototunable cell killing technique using diarylethene molecules as photo-isomerizing-molecular switches. These molecules were delivered to DNA in the cell nucleus due to closed-form generated by UV light, and then blue light triggered cell killing. A UV light irradiation switches the open form, having no DNA intercalation activity, to the closed...
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Characterization, Preclinical Efficacy and Toxicity Evaluations of Flavonoids Glycosides based Standardized Fenugreek Seed Extract (FEFLG)
2023 / Pharmacognosy JournalIntroduction: Fenugreek seeds, a natural food chain raw material, is known to have many flavonoid glycosides. Objective: Characterization, preclinical efficacy, and safety evaluation of flavonoid glycosidebased standardized fenugreek seed extract (FEFLG). Methods: FEFLG was characterized for a group of flavonoid glycoside marker compounds by HPLC. The CD38+ enzyme ...
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