RESUMO
Dracocephalum heterophyllum Benth (Lamiaceae) is a wild herb that possesses a number of biologically active phytomolecules. The aim of this study was to investigate comparative essential oils (EOs) composition and biological (antimicrobial and anti-diabetic) activities of D. heterophyllum from higher altitudes. Gas chromatography-mass spectrometry (GC/MS) and gas chromatography-flame ionisation detector (GC-FID) were carried out for the identification and quantification of EOs components. The hydrodistillation of fresh aerial part of D. heterophyllum gave (0.1-0.8) % w/v EOs yield. Altogether, twenty-seven constituents were identified in the among samples representing (91.0-98.2) % of the EOs composition. The ß-citronellol (31.5-83.7) % contributes major constituent in all samples. The in vitro antimicrobial potential of EOs was examined against six human pathogenic bacterial and two phytopathogens fungal strains. Anti-diabetic activity exhibits excellent α-amylase and better α-glucosidase enzymes inhibitor properties.
Assuntos
Anti-Infecciosos , Lamiaceae , Óleos Voláteis , Humanos , Óleos Voláteis/química , Cromatografia Gasosa-Espectrometria de Massas , Hipoglicemiantes/farmacologia , Hipoglicemiantes/análise , Lamiaceae/química , Anti-Infecciosos/químicaRESUMO
A series of pyrazolo[1,5-c]quinazolines as EGFR inhibitors was designed and synthesized by highly efficient and novel multicomponent route involving Pd-catalyzed tandem one-pot four-component reaction. The reaction proceeds with good functional group tolerance under a simple condition with excellent regioselectivity and high efficiency. Target compounds were screened against cancer cell lines MDA-MB-231, A549 and H1299. Of these, 9b and 10b exhibited superior anticancer activity (IC50â¯<â¯2.5⯵M) to erlotinib and gefitinib. Synthetics were able to inhibit EGFR mediated kinase activity, induced ROS in cancer cells promoting mitochondrial mediated apoptosis via halting cell cycle progression at G1 phase.
Assuntos
Receptores ErbB/antagonistas & inibidores , Paládio/química , Inibidores de Proteínas Quinases/síntese química , Pirazóis/química , Quinazolinas/química , Apoptose/efeitos dos fármacos , Sítios de Ligação , Catálise , Domínio Catalítico , Linhagem Celular Tumoral , Desenho de Fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Receptores ErbB/metabolismo , Cloridrato de Erlotinib/química , Cloridrato de Erlotinib/metabolismo , Cloridrato de Erlotinib/farmacologia , Pontos de Checagem da Fase G1 do Ciclo Celular/efeitos dos fármacos , Humanos , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Simulação de Acoplamento Molecular , Inibidores de Proteínas Quinases/metabolismo , Inibidores de Proteínas Quinases/farmacologia , Pirazóis/metabolismo , Pirazóis/farmacologia , Quinazolinas/metabolismo , Quinazolinas/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Relação Estrutura-AtividadeRESUMO
A Pd-catalyzed cascade reaction of four versatile privileged synthons is described. The sequential reaction involves the formation of five new chemical bonds by concatenating three distinct chemical steps. One of the derivatives exhibited absorption in the visible region, fluorescence with a high quantum yield, and excellent photostability. Its application is explored in live cell imaging, which exhibited cytoplasmic and mitochondrial specific staining with no toxicity.
Assuntos
Corantes Fluorescentes/síntese química , Indazóis/síntese química , Quinazolinas/síntese química , Aminas/síntese química , Aminas/química , Aminas/farmacocinética , Catálise , Linhagem Celular Tumoral , Técnicas Citológicas/métodos , Citoplasma/química , Citoplasma/metabolismo , Corantes Fluorescentes/química , Corantes Fluorescentes/farmacocinética , Humanos , Indazóis/química , Indazóis/farmacocinética , Mitocôndrias/química , Mitocôndrias/metabolismo , Paládio/química , Quinazolinas/química , Quinazolinas/farmacocinética , Coloração e Rotulagem/métodosRESUMO
Needles of seven cultivated clones (C1 - C7) of Juniperus communis at lower altitude and three wild Juniperus species (J. communis, J. recurva and J. indica) at higher altitudes were investigated comparatively for their essential oils (EOs) yields, chemical composition, cytotoxic and antibacterial activities. The EOs yields varied from 0.26 to 0.56% (v/w) among samples. Sixty-one volatile components were identified by gas chromatography-mass spectrometry (GC/MS) and quantified using gas chromatography GC (FID) representing 82.5 - 95.7% of the total oil. Monoterpene hydrocarbons (49.1 - 82.8%) dominated in all samples (α-pinene, limonene and sabinene as major components). Principal component analysis (PCA) of GC data revealed that wild and cultivated Juniperus species are highly distinct due to variation in chemical composition. J. communis (wild species) displayed cytotoxicity against SiHa (human cervical cancer), A549 (human lung carcinoma) and A431 (human skin carcinoma) cells (66.4 ± 2.2%, 74.4 ± 1.4% and 57.4 ± 4.0%), respectively, at 200 µg/ml. EOs exhibited better antibacterial activity against Gram-positive bacteria than against Gram-negative bacteria with the highest zone of inhibition against Staphylococcus aureus MTCC 96 (19.2 ± 0.7) by clone-7. As per the conclusion of the findings, EOs of clone-2, clone-5 and clone-7 can be suggested to the growers of lower altitude, as there is more possibility of uses of these EOs in food and medicinal preparations.