Synthesis and novel structural hybrid analogs of oxindole derivatives bearing piperidine ring, their antidiabetics II activity and molecular docking Study

Journal of Molecular Structure, Год журнала: 2025, Номер unknown, С. 141666 - 141666

Опубликована: Фев. 1, 2025

Язык: Английский

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Mechanism of action of certain medicinal plants for the treatment of asthma

Journal of Ethnopharmacology, Год журнала: 2023, Номер 317, С. 116828 - 116828

Опубликована: Июнь 25, 2023

Язык: Английский

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The impact of piperine on the metabolic conditions of patients with NAFLD and early cirrhosis: a randomized double-blind controlled trial

Scientific Reports, Год журнала: 2024, Номер 14(1)

Опубликована: Янв. 11, 2024

Abstract Non-alcoholic fatty liver disease (NAFLD) is a metabolic dysfunction of the defined as an abnormal accumulation fat within without secondary triggers like alcohol consumption or viral hepatitis. Piperine, bio-active ingredient black pepper, can exert significant function in treatment individuals with NAFLDand early cirrhosis. We investigated impact piperine duration 12 weeks on patients NAFLD and cirrhosis compared toplacebo consumption. In double-blind study, stage were haphazardly distributed into case control groups. They prescribed placebo 5 mg for weeks, respectively. The demographic laboratory parameters assessed baseline after intake. Piperine daily dosage could significantly decrease hepatic enzymes glucose, alleviate dyslipidemia arm rather than arm. Moreover, HOMA levels insulin resistance reduced participants to counterparts. absence approved medicinal intervention NAFLD, regarding favorable more studies this subject are warranted.

Язык: Английский

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Dual drug-loaded cubosome nanoparticles for hepatocellular carcinoma: a design of experiment approach for optimization and in vitro evaluation

Future Journal of Pharmaceutical Sciences, Год журнала: 2024, Номер 10(1)

Опубликована: Март 11, 2024

Abstract Background Liver cancer, a formidable and complex disease, poses significant global health threat, stemming from various causes, including chronic infections like hepatitis B C, cirrhosis, lifestyle factors. In liver cancer treatment, targeted delivery revolutionizes precision therapy, minimizing side effects by directing drugs specifically to cells. This study aims develop statistically optimize cubosomal formulations containing piperine quercetin with the goal of augmenting their activity against hepatocellular carcinoma. Results Employing central-composite design, we utilized Design-Expert® software guide experiment. The key formulation variables were concentration glyceryl monooleate (GMO) Poloxamer-407, while dependent responses particle size (PS) entrapment efficiency (EE%). optimized was validated through utilization high-resolution transmission electron microscopy (HR-TEM), in vitro release studies, an cell proliferation assay conducted on HepG2 line. High-performance liquid chromatography employed for determination nanoparticle. had composition 2.5 (w/w%) GMO 0.5 Poloxamer 407. predicted values PS EE% 102.34 75.11%, respectively. cytotoxicity exhibited enhanced efficacy line, even at lower concentrations, when compared standard. Notably, it demonstrated superior cytotoxic effect Conclusion findings indicated that cubosomes exhibit promise as effective carrier delivering quercetin, addressing carcinoma effectively. Graphical abstract

Язык: Английский

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Curcumin in treatment of hematological cancers: Promises and challenges

Journal of Traditional and Complementary Medicine, Год журнала: 2024, Номер 14(2), С. 121 - 134

Опубликована: Янв. 5, 2024

Hematological cancers include leukemia, myeloma and lymphoma up to 178.000 new cases are diagnosed with these tumors each year. Different kinds of treatment including radiotherapy, chemotherapy, immunotherapy stem cell transplantation have been employed in the therapy hematological cancers. However, they still causing death among patients. On other hand, curcumin as an anti-cancer agent for suppression human has introduced. The using followed. Curcumin diminishes viability survival rate cells. stimulates apoptosis G2/M arrest impair progression tumor. decreases levels matrix metalloproteinases suppressing cancer metastasis. A number downstream targets VEGF, Akt STAT3 undergo by DNA damage reduces resistance cells irradiation. Furthermore, causes drug sensitivity tumors, especially myeloma. For targeted delivery improving its pharmacokinetic features, nanostructures containing agents developed.

Язык: Английский

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Phytochemical Profiling of Sambucus nigra L. Flower and Leaf Extracts and Their Antimicrobial Potential against Almond Tree Pathogens

International Journal of Molecular Sciences, Год журнала: 2023, Номер 24(2), С. 1154 - 1154

Опубликована: Янв. 6, 2023

Despite extensive research on the chemical composition of elderberries and their numerous uses in pharmaceutical, beverage, food production, there is still a lack knowledge about Sambucus nigra leaves flowers' antimicrobial activity against plant pathogens. In this study, phytoconstituents aqueous ammonia extracts were first characterized by infrared spectroscopy gas chromatography-mass spectrometry. The major phytocompounds identified flower extract octyl 2-methylpropanoate; 3,5-dihydroxy-6-methyl-2,3-dihydropyran-4-one; propyl malonic acid; adenine; 1-methyl-2-piperidinemethanol. Concerning leaf extract, 1,6-anhydro-β-D-glucopyranose; oleic 2,1,3-benzothiadiazole; 2,3-dihydro-benzofuran; 4-((1E)-3-hydroxy-1-propenyl)-2-methoxyphenol other phenol derivatives main constituents. potential to act as bioprotectants was then investigated three almond tree pathogens: Diaporthe amygdali, Phytophthora megasperma, Verticillium dahliae. vitro tests showed higher with EC90 values 241-984 μg·mL-1 range (depending pathogen) vs. 354-1322 for extract. addition, led full protection P. megasperma at dose 1875 ex situ artificially-infected excised stems. These inhibitory concentrations lower than those commercial fungicides. findings suggest that S. aerial organs may be susceptible valorization an alternative synthetic fungicides important crop.

Язык: Английский

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Extraction, Characterization, and Evaluation of the Cytotoxic Activity of Piperine in Its Isolated form and in Combination with Chemotherapeutics against Gastric Cancer

Molecules, Год журнала: 2023, Номер 28(14), С. 5587 - 5587

Опубликована: Июль 22, 2023

Gastric cancer is one of the most frequent types neoplasms worldwide, usually presenting as aggressive and difficult-to-manage tumors. The search for new structures with anticancer potential encompasses a vast research field in which natural products arise promising alternatives. In this scenario, piperine, an alkaloid Piper species, has received attention due to its biological activity, including attributes. present work proposes three heating-independent, reliable, low-cost, selective methods obtaining piperine from nigrum L. (Black pepper). Electronic (SEM) optical microscopies, X-ray diffraction, nuclear magnetic resonance spectroscopies (13C 1H NMR), (UV–Vis, photoluminescence, FTIR) confirm obtention crystals. MTT assay reveals that samples exhibit good cytotoxic activity against primary metastasis models gastric cell lines Brazilian Amazon. showed cytotoxicity on evaluated models, revealing higher effectiveness cells bearing degree aggressiveness. Moreover, investigated crystals demonstrated ability act enhancer when combined traditional chemotherapeutics (5-FU GEM), allowing drugs achieve same effect employing lower concentrations. These results establish molecule therapy investigations cancer, both isolated form or bioenhancer.

Язык: Английский

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Piperine improves the sensitivity of osteosarcoma cells to doxorubicin by inducing apoptosis and inhibiting the PI3K/AKT/GSK-3β pathway

Journal of Orthopaedic Surgery and Research, Год журнала: 2023, Номер 18(1)

Опубликована: Март 9, 2023

Abstract Background Osteosarcoma is a primary bone malignancy associated with the highest incidence rate. Chemotherapy for osteosarcoma has not substantially changed, and survival of patients metastatic tumours reached plateau. Doxorubicin (DOX) broad-spectrum anti-osteosarcoma drug; however, its application limited due to high cardiotoxicity. Piperine (PIP) been verified drive certain cancer cell death increases chemosensitivity DOX. However, effects PIP in promoting DOX have studied. Methods We examined combined effect on U2OS 143B cells. CCK-8 assays, scratch flow cytometry analysis, western blotting were performed. Furthermore, was observed vivo using nude mice. Results can increase cells Both vitro results showed dramatic inhibition proliferation tumour growth by therapy group compared monotherapy groups. Apoptosis analysis revealed that augments DOX-induced apoptosis upregulating BAX P53 expression, as well reducing Bcl-2 expression. also attenuated initiation PI3K/AKT/GSK-3β signaling pathway altering expression levels P-AKT, P-PI3K P-GSK3β. Conclusions This study first time potentiate sensitivity cytotoxicity during , which probably achieved inhibiting signalling pathway.

Язык: Английский

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Alkaloids' wide world: Biological activity, extraction, quantification

Elsevier eBooks, Год журнала: 2025, Номер unknown, С. 337 - 369

Опубликована: Янв. 1, 2025

Язык: Английский

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Piperine-loaded electrospun nanofibers, an implantable anticancer controlled delivery system for postsurgical breast cancer treatment

International Journal of Pharmaceutics, Год журнала: 2022, Номер 624, С. 121990 - 121990

Опубликована: Июль 6, 2022

Язык: Английский

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