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1.
Int J Biol Macromol ; 275(Pt 2): 133827, 2024 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-39084983

RESUMO

Monitoring of food freshness is considered one of the crucial challenges for both customers/consumers and the food industries. In this study, we developed a curcumin-based starch film (F1) for pH-sensitive intelligent food packaging application. The starch was obtained from waste seeds of Artocarpus lakoocha (NS-MJF). The native starch underwent various physical and chemical modifications to yield modified starches (S1 [Autoclave heat treated], S2 [osmotic-pressure treated], S3 [citric acid treated]). The native starch was then used further for the formation of curcumin (2.5 % w/w)-based film (F1). We had analyzed these starches for solubility, colour analysis, biodegradability, oil absorption capacity, and moisture content, etc. Scanning electron microscopy (SEM) and atomic force microscopy (AFM) revealed favourable microstructures. The addition of curcumin to the starch enhanced the contact angle and elongation at the break of the resulting films. Antioxidant and antimicrobial assays, along with real-time freshness monitoring of chicken fillets, were also conducted. Thus, our findings may contribute to the optimization of pH-responsive biopolymer-based films for intelligent poultry packaging, promising advancements in food preservation and safety.


Assuntos
Antibacterianos , Antioxidantes , Artocarpus , Curcumina , Embalagem de Alimentos , Amido , Artocarpus/química , Curcumina/química , Curcumina/farmacologia , Amido/química , Antioxidantes/farmacologia , Antioxidantes/química , Concentração de Íons de Hidrogênio , Embalagem de Alimentos/métodos , Antibacterianos/farmacologia , Antibacterianos/química , Animais , Solubilidade
2.
Nat Prod Res ; : 1-9, 2024 Mar 05.
Artigo em Inglês | MEDLINE | ID: mdl-38440935

RESUMO

Ayurveda, the traditional Indian medical system, has potential applications in early malaria treatment. In an in silico docking study, 50 phytochemicals from two plants Artocarpus lakoocha Roxb. (AL) And Artocarpus heterophyllus Lam. (AH), were examined for their interactions with anti-malarial proteins (PDB IDs: 3BWK, 3BPF, 1LF3). The nucleotide analogue Artemisinin, a current malaria treatment, served as a positive control. Result showed that phytochemicals from AL and AH exhibited binding affinities as high as -9.6 kcal/mol, respectively. Additionally, molecular dynamics simulation for Artocarpin: 3BPF demonstrated stable complexes over 100 ns. Notably, Artocarpin and Quercetin displayed higher binding affinities (up to -9.6 as well as -9.5 kcal/mol, respectively) compared to Artemisinin (-7.5 up to kcal/mol), have shown. Pharmacokinetic predictions indicated the compounds were likely non-carcinogenic, water-soluble and biologically safe. In-vitro analysis using ß-Hematin assay supported these findings, suggesting the phytochemicals as Hemozoin pathway inhibitors.

3.
Front Plant Sci ; 15: 1341454, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38476686

RESUMO

The latex of the medicinal plant Artocarpus lakoocha (A. lakoocha), which has been shown to have potential anti-inflammatory and wound-healing capabilities, contains a novel heme-peroxidase. This protein was subjected to activity assays, fluorescence spectroscopy, and far-UV circular dichroism to investigate its structure, dynamics, and stability. The results demonstrated the presence of three folding states: the native state (N) at neutral pH, intermediate states including molten globule (MG) at pH 2 and acid-unfolded (UA) at pH 1.5 or lower, and acid-refolded (A) at pH 0.5, along with alkaline denatured (UB) at pH 8-12 and the third denatured state (D) at GuHCl concentrations exceeding 5 M. Absorbance studies indicated the presence of loosely associated form of heme in the pH range of 1-2. The protein showed stability and structural integrity across a wide pH range (3-10), temperature (70°C), and high concentrations of GuHCl (5 M) and urea (8 M). This study is the first to report multiple 'partially folded intermediate states' of A. lakoocha peroxidase, with varying amounts of secondary structure, stability, and compactness. These results demonstrate the high stability of A. lakoocha peroxidase and its potential for biotechnological and industrial applications, making it a valuable model system for further studies on its structure-function relationship.

4.
Plants (Basel) ; 12(18)2023 Sep 16.
Artigo em Inglês | MEDLINE | ID: mdl-37765449

RESUMO

Breadfruit (Artocarpus altilis) is a traditional fruit tree of 15-30 m height in the tropics. The presence of size-controlling rootstock in the species is not known. A small tropical tree species, lakoocha (Artocarpus lakoocha), was recently identified as a potential vigor-controlling rootstock, conferring over a 65% reduction in breadfruit tree height. To better understand the intriguing scion/rootstock interactions involved in dwarfing, we investigate flavonoid accumulation and its regulation in breadfruit scions in response to different rootstocks. To this end, we isolated a chalcone synthase cDNA, AaCHS, and a full-length bifunctional dihydroflavonol 4-reductase cDNA, AaDFR, from breadfruit scion stems. The expression of both AaCHS and AaDFR genes was examined over the period of 16 to 24 months following grafting. During the development of the dwarf phenotype, breadfruit scion stems on lakoocha rootstocks display significant increases in total flavonoid content, and show upregulated AaCHS expression when compared with those on self-grafts and non-grafts. There is a strong, positive correlation between the transcript levels of AaCHS and total flavonoid content in scion stems. The transcript levels of AaDFR are not significantly different across scions on different rootstocks. This work provides insights into the significance of flavonoid biosynthesis in rootstock-induced breadfruit dwarfing.

5.
Curr Pharm Des ; 28(19): 1543-1560, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35652402

RESUMO

The World Health Organization predicts a 70% increase in cancer incidents in developing nations over the next decade, and it will be the second leading cause of death worldwide. Traditional plant-based medicine systems play an important role against various diseases and provide health care to a large section of the population in developing countries. Indigenous fruits and their bioactive compounds with beneficial effects like antioxidant, antiproliferative, and immunomodulatory are shown to be useful in preventing the incidence of cancer. India is one of the biodiversity regions and is native to numerous flora and fauna in the world. Of the many fruiting trees indigenous to India, Mango (Mangifera indica), Black plum (Eugenia jambolana or Syzygium jambolana), Indian gooseberry (Emblica officinalis or Phyllanthus emblica), kokum (Garcinia indica or Brindonia indica), stone apple or bael (Aegle marmelos), Jackfruit (Artocarpus heterophyllus), Karaunda (Carissa carandas) and Phalsa (Grewia asiatica), Monkey Jackfruit (Artocarpus lakoocha) and Elephant apple (Dillenia indica) have been shown to be beneficial in preventing cancer and in the treatment of cancer in validated preclinical models of study. In this review, efforts are also made to collate the fruits' anticancer effects and the important phytochemicals. Efforts are also made to address the underlying mechanism/s responsible for the beneficial effects of these fruits in cancer prevention and treatment. These fruits have been a part of the diet, are non-toxic, and easily acceptable for human application. The plants and some of their phytochemicals possess diverse medicinal properties. The authors propose that future studies should be directed at detailed studies with various preclinical models of study with both composite fruit extract/juice and the individual phytochemicals. Additionally, translational studies should be planned with the highly beneficial, well-investigated and pharmacologically multifactorial amla to understand its usefulness as a cancer preventive in the high-risk population and as a supportive agent in cancer survivors. The outcome of both preclinical and clinical studies will be useful for patients, the healthcare fraternity, pharmaceutical, and agro-based sectors.


Assuntos
Frutas , Neoplasias , Compostos Fitoquímicos , Extratos Vegetais , Atenção à Saúde , Frutas/química , Humanos , Neoplasias/tratamento farmacológico , Neoplasias/prevenção & controle , Phyllanthus emblica/química , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Extratos Vegetais/química
6.
Front Pharmacol ; 12: 694562, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34305605

RESUMO

Oxyresveratrol (OXY) is a small molecule phytochemical which has been reported to have important biological function. The aim of this study was to elucidate the gene expression and biological pathways altered in MCF-7, breast cancer cells following exposure to OXY. The cytotoxicity to different cancer cell lines was screened using MTT assay and then whole gene expression was elucidated using microarray. The pathways selected were also validated by quantitative PCR analysis, fluorometric and western blot assay. A total of 686 genes were found to have altered mRNA expression levels of two-fold or more in the 50 µM OXY-treated group, while 2,338 genes were differentially expressed in the 100 µM-treated group. The relevant visualized global expression patterns of genes and pathways were generated. Apoptosis was activated through mitochondria-lost membrane potential, caspase-3 expression and chromatin condensation without DNA damage. G0/G1 and S phases of the cell cycle control were inhibited dose-dependently by the compound. Rad51 gene (DNA repair pathway) was significantly down-regulated (p < 0.0001). These results indicate that OXY moderates key genes and pathways in MCF-7 cells and that it could be developed as a chemotherapy or chemo-sensitizing agent.

7.
Pharmaceuticals (Basel) ; 13(10)2020 Oct 14.
Artigo em Inglês | MEDLINE | ID: mdl-33066628

RESUMO

Artocarpus lakoocha (Al) and Glycyrrhiza glabra (Gg) extracts have been reported to show tyrosinase inhibitory activity and melanin pigment reduction. This is the first study to assess the combination of Al and Gg extracts in enhancing inhibition of tyrosinase and reduction of melanin pigments. Al and Gg extracted by maceration in 70% and 95% ethanol were analyzed for oxyresveratrol and glabridin using Ultra High Performance Liquid Chromatography. Extracts of Al and Gg singly and combinations of Al95 and Gg95 were tested for cytotoxicity, tyrosinase inhibitory activity, and reduction of melanin pigments in melanoma B16 cells. Al95 had higher antioxidant, tyrosinase inhibitory activity and reduced more melanin pigments in B16 cells compared to Al70, and exhibited higher levels of oxyresveratrol. Gg95 inhibited oxidative stress and mushroom tyrosinase better than Gg70, and exhibited higher levels of glabridin. Combinations of Al95 and Gg95 at various ratios (concentration of 0.1 mg/mL) were not cytotoxic to B16 cells. Interestingly, Al95 and Gg95 combined at a ratio 9:1 reduced melanin pigment up to 53% in B16 cells. This combination of Al95 and Gg95 extracts exhibited the additive effect of reducing melanin pigments by suppressing the expression of microphthalmia-associated transcription factor (MITF), tyrosinase (TYR) and tyrosinase-related protein-2 (TRP-2) in B16 cells. The combination of Al and Gg extracts could be developed as skin care products for hyperpigmentation treatment.

8.
Plants (Basel) ; 9(10)2020 Oct 09.
Artigo em Inglês | MEDLINE | ID: mdl-33050190

RESUMO

Artocarpus heterophyllus Lam. (AH) and Artocarpus lakoocha Roxb. (AL) are two endemic plants that grow on the Asian continent. To date, their applications have been aimed at using their fruit as a food source or for some of their therapeutic virtues. In this study, attention was given to the flowers of AH and AL. Initially, the cytotoxicity of the phytoextracts was assessed, and the content of minerals, phenols, and flavonoids was determined. Furthermore, some antioxidant components were identified by HPLC. Furthermore, the ability of AH and AL extracts to modulate the gene expression of some targets involved in the antioxidant response was studied. The results obtained highlighted the nutritional and antioxidant value of the AH and AL flower extracts. This study will contribute to enhancing the use of AH and AL flowers as potential supplements in human nutrition.

9.
Chem Pharm Bull (Tokyo) ; 68(7): 671-674, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32612002

RESUMO

Chromatographic separation of the acetone extracts from the twigs and barks of Artocarpus lakoocha led to the isolation of the one new flavanone, lakoochanone (1), together with eleven known compounds (2-12). Lakoochanone (1) and moracin C (4) exhibited weak antiplasmodial activity against Plasmodium falciparum Dd2 with IC50 values of 36.7 and 33.9 µM, respectively. Moreover, moracin C (4) and sanggenofuran B (5) showed cytotoxic activity against A2780 cell line with the respective IC50 values of 15.0 and 57.1 µM. In addition, cyclocommunin (7) displayed strong antimycobacterial activity against Mycobacterium tuberculosis H37Ra with the minimum inhibitory concentration (MIC) value of 12.3 µM.


Assuntos
Antiprotozoários/farmacologia , Antituberculosos/farmacologia , Artocarpus/química , Flavanonas/farmacologia , Mycobacterium tuberculosis/efeitos dos fármacos , Plasmodium falciparum/efeitos dos fármacos , Antiprotozoários/química , Antiprotozoários/isolamento & purificação , Antituberculosos/química , Antituberculosos/isolamento & purificação , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Flavanonas/química , Flavanonas/isolamento & purificação , Humanos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Testes de Sensibilidade Parasitária , Casca de Planta/química , Caules de Planta/química , Relação Estrutura-Atividade
10.
Molecules ; 25(11)2020 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-32492964

RESUMO

Artocarpus lakoocha Wall. ex Roxb. (family: Moraceae) has been used as a traditional Thai medicine for the treatment of various parasitic diseases. This species has been reported to be the source of phytochemicals, which show potent biological activities. The objective of this study was to investigate the phytochemical profile of the extracts of the heartwood of A. lakoocha and their pro-oxidant activity in vitro. The heartwood was ground, extracted, and then chromatographic and spectroscopic analyses were carried out; oxyresveratrol was identified as the major component in the extracts. The pro-oxidant activity was investigated using DNA-nick, reactive oxygen species and reducing assays. The results showed that oxyresveratrol induced DNA damage dose-dependently in the presence of copper (II) ions. It was also found to generate reactive oxygen species (ROS) in a dose-dependent manner and reduce copper (II) to copper (I). It is concluded that oxyresveratrol is the most abundant stilbenoid in A. lakoocha heartwood. The compound exhibited pro-oxidant activity in the presence of copper (II) ions, which may be associated with its ability to act as an anticancer compound.


Assuntos
Artocarpus/química , Dano ao DNA , DNA/efeitos dos fármacos , Oxidantes/química , Extratos Vegetais/farmacologia , Estilbenos/farmacologia , Anti-Helmínticos/farmacologia , Antineoplásicos/farmacologia , Antiparasitários/farmacologia , Antivirais/farmacologia , Cromatografia , Cromatografia Líquida de Alta Pressão , Cobre/química , DNA/química , Íons , Espectroscopia de Ressonância Magnética , Compostos Fitoquímicos/farmacologia , Pós , Espécies Reativas de Oxigênio/química , Estilbenos/química
11.
Plants (Basel) ; 9(3)2020 Mar 22.
Artigo em Inglês | MEDLINE | ID: mdl-32235808

RESUMO

'Mahat' is a well-known medicinal plant utilized in Thailand. The Thai name 'Mahat' has been used in many scientific articles for years. However, it is, unpredictably, a homonym of two scientific names in Flora of Thailand, i.e., A. lacucha and A. thailandicus. Additionally, both species are complex due to their high morphological variation. This causes difficulties in species identification especially when this Thai name is referred to as the scientific name for research publication, quality control of pharmaceutical raw materials, and registration of pharmaceutical products. In this study, we scrutinized the taxonomy of 'Mahat' by detailed examination of its morphology and distribution, including molecular and qualitative phytochemical studies. Leaf surfaces were inspected using scanning electron microscopy. The phylogeny of both species was studied using DNA sequences of nuclear and plastid regions. Chromatographic fingerprints, focusing on the major active compound oxyresveratrol, were identified using high-performance liquid chromatography. According to our current study, phylogenetic evidence showed that some samples of both species were clustered together in the same clade and phytochemical fingerprints were almost identical. These results are valuable data for taxonomic revision in the near future and reveal the possible utilization of A. thailandicus as a new material source of oxyresveratrol in the pharmaceutical industry.

12.
Heliyon ; 6(3): e03458, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-32154416

RESUMO

Long-term diabetic complications are exacerbated by post-prandial hyperglycemia which could be ameliorated by α-glucosidase inhibitor including oxyresveratrol. Puag-Haad is an aqueous extract from Artocarpus lakoocha Roxb. containing ~65% oxyresveratrol. Oxyresveratrol is an inhibitor of isolated yeast α-glucosidase enzyme but has not been tested on intact gut enterocytes where the enzyme is membrane-bound. Accordingly, differentiated Caco-2 cells that contain the native enzyme were used to test maltose hydrolysis in the present study. The results demonstrated that purified yeast α-glucosidase was non-competitively inhibited by oxyresveratrol (Ki 54.4 ± 0.7 µg/mL) and Puag-Haad (2.7 ± 0.1 µg/mL) compared to 153.8 ± 4.3 µg/mL acarbose, an anti-diabetic drug. In differentiated Caco-2 cells, both oxyresveratrol and Puag-Haad inhibited maltose hydrolysis with lesser potency compared to acarbose. Thus, although weaker than acarbose, oxyresveratrol and Puag-Haad do not inhibit pancreatic amylase which might be a therapeutic asset in preventing fermentation of unabsorbed carbohydrate causes abdominal bloating, flatulence, or diarrhea. Oxyresveratrol and Puag-Haad may help control postprandial hyperglycemia with low risk of gastrointestinal side effects.

13.
Int J Mol Sci ; 21(4)2020 02 17.
Artigo em Inglês | MEDLINE | ID: mdl-32079307

RESUMO

:Artocarpus lakoocha Roxb. (AL) has been known for its high content of stilbenoids, especially oxyresveratrol. AL has been used in Thai traditional medicine for centuries. However, the role of AL in regulating inflammation has not been elucidated. Here we investigated the molecular mechanisms underlying the anti-inflammation of AL ethanolic extract in RAW 264.7 murine macrophage cell line. The HPLC results revealed that this plant was rich in oxyresveratrol, and AL ethanolic extract exhibited anti-inflammatory properties. In particular, AL extract decreased lipopolysaccharide (LPS)-mediated production and secretion of cytokines and chemokine, including IL-6, TNF-α, and MCP-1. Consistently, the extract inhibited the production of nitric oxide (NO) in the supernatants of LPS-stimulated cells. Data from the immunofluorescence study showed that AL extract suppressed nuclear translocation of nuclear factor-kappa B (NF-κB) upon LPS induction. Results from Western blot analysis further confirmed that AL extract strongly prevented the LPS-induced degradation of IκB which is normally required for the activation of NF-κB. The protein expression of iNOS and COX-2 in response to LPS stimulation was significantly decreased with the presence of AL extract. AL extract was found to play an anti-inflammatory role, in part through inhibiting LPS-induced activation of Akt. The extract had negligible impact on the activation of mitogen-activated protein kinase (MAPK) pathways. Specifically, incubation of cells with the extract for only 3 h demonstrated the rapid action of AL extract on inhibiting the phosphorylation of Akt, but not ERK1/2. Longer exposure (24 h) to AL extract was required to mildly reduce the phosphorylation of ERK1/2, p38, and JNK MAPKs. These results indicate that AL extract manipulates its anti-inflammatory effects mainly through blocking the PI3K/Akt and NF-κB signal transduction pathways. Collectively, we believe that AL could be a potential alternative agent for alleviating excessive inflammation in many inflammation-associated diseases.


Assuntos
Artocarpus/química , Lipopolissacarídeos/efeitos adversos , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Ciclo-Oxigenase 2/metabolismo , Citocinas/metabolismo , Inflamação/metabolismo , Camundongos , Proteínas Quinases Ativadas por Mitógeno/metabolismo , NF-kappa B/metabolismo , Óxido Nítrico/metabolismo , Fosfatidilinositol 3-Quinases/metabolismo , Fosforilação , Células RAW 264.7 , Transdução de Sinais/efeitos dos fármacos , Estilbenos/farmacologia
14.
Biomed Pharmacother ; 110: 554-560, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30530291

RESUMO

Oxyresveratrol, an active ingredient of Artocarpus lakoocha, is known to possess anti-inflammatory and immunomodulatory properties. Current study investigates the immunomodulatory effect of oxyresveratrol in mouse model of ethanol-induced ulcer. Anti-ulcer effect was determined using histopathological evaluation (H&E staining) and different tests like, gastric ulcer scoring, ulcer index, total acid secretion, and gastric pH. The mRNA expression levels of interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), nuclear factor-kappaB (NF-ĸB), cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2) and trefoil factor 2 (TFF-2) were evaluated using reverse transcription polymerase chain reaction (RT-PCR). The data showed marked percentage inhibition of erosion, hemorrhage, fibrinoid necrosis, inflammatory infiltrate, and ulcer in low (30 mg/kg b.w.) and high dose (50 mg/kg b.w.) groups of oxyresveratrol. Treatment with oxyresveratrol inhibited ulcer score and ulcer index as compared with disease control group. Oxyresveratrol significantly increased gastric pH (P < 0.001) and attenuated total acid (P < 0.001) secretion. RT-PCR analysis showed significant suppression in the mRNA expression levels of IL-6 (P < 0.001), TNF-α (P < 0.01), NF-ĸB (P < 0.001), and COX-2 (P < 0.05) in oxyresveratrol treated groups, while COX-1 expression levels were found unaltered. Treatment with oxyresveratrol significantly elevated (P < 0.01) the expression levels of cytoprotective TFF-2 levels. Similar Immunomodulatory and anti-ulcer effects were found with ranitidine treatment, which was used as a reference drug. In conclusion, oxyresveratrol possess significant anti-ulcer property which might be attributed to attenuated expression levels of IL-6, TNF-α, NF-ĸB, and COX-2 and elevated expression levels of TFF-2.


Assuntos
Ciclo-Oxigenase 2/metabolismo , Interleucina-6/metabolismo , NF-kappa B/metabolismo , Extratos Vegetais/uso terapêutico , Estilbenos/uso terapêutico , Úlcera Gástrica/metabolismo , Fator Trefoil-2/biossíntese , Fator de Necrose Tumoral alfa/metabolismo , Animais , Antiulcerosos/farmacologia , Antiulcerosos/uso terapêutico , Inibidores de Ciclo-Oxigenase 2/farmacologia , Inibidores de Ciclo-Oxigenase 2/uso terapêutico , Regulação para Baixo/efeitos dos fármacos , Regulação para Baixo/fisiologia , Etanol/toxicidade , Interleucina-6/antagonistas & inibidores , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Moraceae , NF-kappa B/antagonistas & inibidores , Extratos Vegetais/farmacologia , Estilbenos/farmacologia , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/tratamento farmacológico , Fator Trefoil-2/agonistas , Fator de Necrose Tumoral alfa/antagonistas & inibidores
15.
Eur J Med Chem ; 143: 1301-1311, 2018 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-29126732

RESUMO

In vitro screening for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of the Artocarpus lakoocha root-bark extracts revealed interesting results. Bioassay-guided fractionation resulted in the isolation of two new (1 and 2) and six known 2-arylbenzofurans 3-8, along with one stilbenoid 9 and one flavonoid 10. The structures of the isolated compounds were elucidated by UV, IR, 1D- and 2D-NMR and MS spectroscopic data analysis. Compounds 4, 6 and 7 exhibited more potent AChE inhibitory activity (IC50 = 0.87-1.10 µM) than the reference drug, galantamine. Compounds 4, 8 and 9 displayed greater BChE inhibition than the standard drug. The preferential inhibition of BChE over AChE indicated that 4 also showed a promising dual AChE and BChE inhibitor. The synthetic mono-methylated analogs 4a-c and 6a-b were found to be good BChE inhibitors with IC50 values ranging between 0.31 and 1.11 µM. Based on the docking studies, compounds 4 and 6 are well-fitted in the catalytic triad of AChE. Compounds 4 and 6 showed different binding orientations on BChE, and the most potent BChE inhibitor 4 occupied dual binding to both CAS and PAS more efficiently.


Assuntos
Artocarpus/química , Benzofuranos/química , Benzofuranos/farmacologia , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacologia , Éteres Metílicos/química , Acetilcolinesterase/química , Acetilcolinesterase/metabolismo , Benzofuranos/metabolismo , Butirilcolinesterase/química , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/metabolismo , Concentração Inibidora 50 , Simulação de Acoplamento Molecular , Conformação Proteica
16.
Molecules ; 21(4): 489, 2016 Apr 19.
Artigo em Inglês | MEDLINE | ID: mdl-27104505

RESUMO

Oxyresveratrol (2,4,3',5'-tetrahydroxystilbene, 1), a phytoalexin present in large amounts in the heartwood of Artocarpus lacucha Buch.-Ham., has been reported to possess a wide variety of biological activities. As part of our continuing studies on the structural modification of oxyresveratrol, a library of twenty-six compounds was prepared via O-alkylation, aromatic halogenation, and electrophilic aromatic substitution. The two aromatic rings of the stilbene system of 1 can be chemically modulated by exploiting different protecting groups. Such a strategy allows for selective and exclusive modifications on either ring A or ring B. All compounds were evaluated in vitro for a panel of biological activities, including free radical scavenging activity, DNA protective properties, antiherpetic activity, inhibition of α-glucosidase and neuraminidase, and cytotoxicity against some cancer cell lines. Several derivatives were comparably active or even more potent than the parent oxyresveratrol and/or the appropriate positive controls. The partially etherified analogs 5'-hydroxy-2,3',4-trimethoxystilbene and 3',5'-dihydroxy-2,4-dimethoxystilbene demonstrated promising anti-herpetic and DNA protective activities, offering new leads for neuropreventive agent research, whereas 5'-hydroxy-2,3',4,-triisopropoxystilbene displayed anti-α-glucosidase effects, providing a new lead molecule for anti-diabetic drug development. 3',5'-Diacetoxy-2,4-diisopropoxystilbene showed potent and selective cytotoxicity against HeLa cancer cells, but the compound still needs further in vivo investigation to verify its anticancer potential.


Assuntos
Extratos Vegetais/química , Estilbenos/síntese química , Estilbenos/farmacologia , Antivirais/síntese química , Antivirais/química , Antivirais/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Sequestradores de Radicais Livres/síntese química , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/farmacologia , Humanos , Extratos Vegetais/farmacologia , Estilbenos/química
17.
J Investig Clin Dent ; 4(4): 219-24, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-23857911

RESUMO

AIM: The antiviral activities of Artocarpus lakoocha (A. lakoocha) extract have been reported in a number of studies; however, data regarding its antibacterial capability are limited. The aim of the present study was to examine the effectiveness of A. lakoocha extract, poloxamer 407, on Enterococcus faecalis (E. faecalis). METHODS: The effect of the antimicrobial activity of A. lakoocha extract and A. lakoocha extract, poloxamer 407, against E. faecalis was investigated. The antibacterial efficacy of A. lakoocha extract, poloxamer 407, against E. faecalis was compared to calcium hydroxide in a tooth model. RESULTS: The minimal inhibitory concentration and minimal bactericidal concentration (MBC) of A. lakoocha extract against E. faecalis were 0.39 ± 0 mg/mL and 3.12 ± 0 mg/mL, respectively; the MBC of calcium hydroxide against E. faecalis was 31.25 ± 0 mg/mL. In the tooth model, the E. faecalis count in all groups significantly decreased as the depth into the dentin increased compared to the control. There were no significant differences between 4% A. lakoocha extract poloxamer and UltraCal XS at any time period (P > 0.05) with one exception: at a depth of 0.6 mm on day 5, UltraCal XS had a significantly greater colonization than 4% A. lakoocha extract poloxamer. CONCLUSION: A. lakoocha extract, poloxamer 407, might be a useful alternative for antimicrobial medication in endodontic treatment. However, controlled clinical studies to evaluate its efficacy are needed.


Assuntos
Antibacterianos/farmacologia , Artocarpus , Enterococcus faecalis/efeitos dos fármacos , Extratos Vegetais/farmacologia , Poloxâmero/farmacologia , Carga Bacteriana/efeitos dos fármacos , Técnicas Bacteriológicas , Hidróxido de Cálcio/farmacologia , Contagem de Colônia Microbiana , Cavidade Pulpar/microbiologia , Dentina/microbiologia , Humanos , Testes de Sensibilidade Microbiana , Irrigantes do Canal Radicular/farmacologia , Estilbenos/farmacologia
18.
J Basic Clin Pharm ; 1(4): 239-45, 2010 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-24825993

RESUMO

Artocarpus lakoocha Roxb (Moraceae) is cultivated in Uttar Pradesh, Bengal, Khasi Hills and Western Ghats. Objectives of the present study were to determine antibacterial, antioxidant, anthelmintic and insecticidal efficacy of methanol extract of A. lakoocha fruit pericarp. Antibacterial activity was tested against by Agar well diffusion method. Antioxidant activity in terms of free radical scavenging ability was determined by DPPH free radical scavenging assay. Anthelmintic efficacy was determined using adult Indian earthworm. Insecticidal activity was tested against second and third instar larvae of Aedes aegypti. The extract has shown dose dependent antibacterial, antioxidant, anthelmintic and insecticidal activity. Among bacteria, S. aureus has shown more susceptibility than K. pneumoniae and P. aeruginosa. The extract exhibited marked antioxidant activity by scavenging DPPH free radical. The IC50 value for extract was found to be 49.42µg/ml. The extract exhibited marked anthelmintic activity by causing paralysis and death of worms and the effect was found to be dose dependent. The extract concentration 100mg/ml has shown marked anthelmintic effect than standard drug. In insecticidal study, the 2(nd) instar larvae were shown to be more susceptible than 3(rd) instar larvae. Phytochemical analysis revealed the presence of tannins and alkaloids. The presence of these phytoconstituents might be responsible for the biological activities of extract tested. The extract could be used to treat free radical damage, bacterial and helmintic infections and to control insect vectors. Further studies on isolation of constituents and their bio-efficacies in vitro and in vivo are under investigation.

19.
Anc Sci Life ; 28(4): 21-4, 2009 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-22557328

RESUMO

The antibacterial activity of Artocarpus lakoocha Roxb. bark was tested against different species of bacteria. The minimum inhibitory concentration (MIC) of the methanolic extract showed that there was no growth in Shigella soneii 2, E.coli MTCC 1568, Bacillus pumilus 8241, Proteus mirabilis AM 198, Bacillus subtelis ATCC 6633, E. Coli Row 7/12 Species at 200-400g/ml. From the result obtained, it was observed that the methanolic extract of. Artocarpus lakoocha at concentration of 200 gl ml and 400 gl ml exhibited a good activity against gram negative bacteria.

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