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Two prenylated 2-arylbenzofurans were isolated from roots of Artocarpus heterophyllus, with a combination of various chromatographic approaches, including ODS, MCI, Sephadex LH-20, and semipreparative high performance liquid chromatography(HPLC). They were identified as 5-[6-hydroxy-4-methoxy-5,7-bis(3-methylbut-2-enyl)benzofuran-2-yl]-1,3-benzenediol(1) and 5-[2H,9H-2,2,9,9-tetramethyl-furo[2,3-f]pyrano[2,3-h][1]benzopyran-6-yl]-1,3-benzenediol(2) with spectroscopic methods, such as HR-ESI-MS, IR, 1D NMR, and 2D NMR, and named artoheterins B(1) and C(2), respectively. The anti-respiratory burst activities of the two compounds were evaluated with rat polymorphonuclear neutrophils(PMNs) stimulated by phorbol 12-myristate 13-acetate(PMA). The results showed that 1 and 2 exhibited significant inhibitory effect on respiratory burst of PMNs with IC_(50) values of 0.27 and 1.53 μmol·L~(-1), respectively.
Subject(s)
Rats , Animals , Molecular Structure , Artocarpus/chemistry , Plant Extracts/pharmacology , Magnetic Resonance Spectroscopy , Plant Roots/chemistryABSTRACT
Water scarcity and water quality is a subject of constant debate around the world, with the accumulation of salts in water and on soils causing a negative impact on food production, man and herds, especially in the arid and semi-arid regions. The use of bovine manure biofertilizers that potentiate the use of brackish water, normally restricted in agriculture due to its salinity, has been suggested for seedling formation and crop production, including jackfruit plants. An experiment was carried out from October/2012 to February/2013, in a protected environment, at Agrarian Sciences Center, Federal University of Paraíba, Areia county, Paraíba State, Brazil, to evaluate the effects of saline water and bovine biofertilizer chemically enriched with gypsum, cow's milk and molasses. The experimental design was completely randomized, with five replications of a plant, in a factorial scheme 5 × 2, corresponding at values of electrical conductivity of the water of 0.5, 1.0, 2.0, 3.0 and 4.0 dS m-1 substrate with and without bovine biofertilizer. Measurements were made of substrate salinity, height of growth, stem diameter, length mean root, leaf area, leaf area ratio, and total dry mass (root, shoots and leaves). The biofertilizer enriched with cow's milk, sugar cane molasses and agricultural gypsum increased the salinity of the soil; however, it attenuated the negative effects of the salts during establishment of jackfruit seedlings, to 95 days after emergence. All the growth variables studied were higher for seedlings developed in substrate with bovine biofertilizer chemically enriched.
A escassez e a qualidade da água são assuntos de constante debate em todo o mundo, com o acúmulo de sais na água e nos solos, causando um impacto negativo na produção de alimentos, homem e rebanhos, especialmente nas regiões áridas e semiáridas. O uso de biofertilizante de esterco bovino que possibilita o uso de água salobra, normalmente restrita à agricultura devido à salinidade, tem sido sugerido para formação demudas e produção agrícola, inclusive de jaqueira. Um experimento foi desenvolvido entre outubro de 2012 e fevereiro de 2013, em ambiente protegido, no Centro de Ciências Agrárias, da Universidade Federal da Paraíba, Areia, Paraíba, Brasil, para avaliar os efeitos da água salina e biofertilizante bovino enriquecido quimicamente com calcário, leite de vaca e melaço. O delineamento experimental foi inteiramente casualizado, com cinco repetições e uma planta, em esquema fatorial 5 × 2. Água com condutividade elétrica de 0,5, 1,0, 2,0, 3,0 e 4,0 foram aplicadas no substrato com e sem biofertilizante bovino. Foi avaliada a salinidade do substrato, crescimento em altura, diâmetro caulinar, crescimento da raiz principal, área foliar, razão de área foliar e massa seca total (raiz, parte aérea e folhas). O biofertilizante enriquecido com leite de vaca, melaço de cana-de-açúcar e gesso agrícola aumentou a salinidade do solo, no entanto, atenuou os efeitos negativos da salinidade durante o estabelecimento das mudas de jaqueira, aos 95 dias após a emergência. Todas as variáveis estudadas foram maiores nas mudas que cresceram no substrato com biofertilizante enriquecido quimicamente.
Subject(s)
Saline Waters , ArtocarpusABSTRACT
Objective: To evaluate the immunosuppressive effect on human phagocytes and antibacterial activity of dihydromorin and norartocarpetin isolated from Artocarpus heterophyllus heartwoods. Methods: Dihydromorin and norartocarpetin were isolated from Artocarpus heterophyllus heartwoods. A modified Boyden chamber was used to determine the chemotactic activity of human phagocyte. The respiratory burst was evaluated by chemiluminescence assay. Myeloperoxidase (MPO) activity was quantified using a colorimetric assay. The broth microdilution method was performed to assess their antibacterial activity. Results: Dihydromorin exhibited potent inhibitory effect on the chemotactic activity of polymorphonuclear neutrophils (PMNs) with an IC50 value of 5.03 μg/mL. Dihydromorin also inhibited reactive oxygen species production of whole blood cells, PMNs, and monocytes with IC50 values of 7.88, 7.59 and 7.24 μg/mL, respectively. Interestingly, dihydromorin also strongly inhibited the MPO activity of PMNs with an IC50 value of 5.24 μg/mL, which was lower than indomethacin (24.6 μg/mL). Molecular docking of dihydromorin and crystal structure of MPO showed that dihydromorin had close interaction with key amino acid residues such as Arg239 and Gln91. Antibacterial activity assay showed that only dihydromorin had a strong effect against Streptococcus pyogenes with MIC and MBC values of 15.62 and 31.25 μg/mL, respectively. Conclusions: The results suggest that dihydromorin could be developed as an anti-inflammatory and antibacterial agent.
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@#Introduction: There are numerous studies on the therapeutic properties of Artocarpus heterophyllus. However, studies on the aqueous extraction of A. heterophyllus leaves are limited. This present study was conducted to optimize the extraction conditions of A. heterophyllus leaves to yield the highest phenolic, flavonoids and antioxidant contents. Methods: Response surface methodology (RSM) was employed to obtain a higher phenolic extraction parameter(s) of A. heterophyllus leaves using Central Composite Design (CCD). The antioxidant activity was then determined via ABTS (2,29-azinobis (3 ethylbenzothiazoline-6-sulfonic acid)) and DPPH (2,2-Diphenyl-1-picrylhydrazyl) assay and analysis of the individual phenolics was performed by high performance liquid chromatography (HPLC). Results: The optimum extraction conditions with higher phenolics content and antioxidant activity was achieved at 81°C, 100 min and 40 mL/g sample with a good desirability value of 0.87. Under these optimized parameters, total phenolics and flavonoids were 174.48 ± 4.05 mg GAE/g sample and 21.44 ± 0.05 mg RE/g sample, respectively. Meanwhile, antioxidant activity via ABTS and DPPH assays were 90.88% ± 0.09 and 87.22% ± 0.62, respectively. Finally, under optimal extraction conditions revealed 4 compounds identified as chlorogenic acid, quercetin, rutin and kaempferol. Conclusion: The optimisation are promising to improve phenolic yield and antioxidant activity in A. heterophyllus leaves. It also proved that A. heterophyllus leaves can be used as an alternative natural antioxidant especially in medicinal applications since all identified compound possess significant biological activities for human health.
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Objective: To evaluate the immunosuppressive effect on human phagocytes and antibacterial activity of dihydromorin and norartocarpetin isolated from Artocarpus heterophyllus heartwoods. Methods: Dihydromorin and norartocarpetin were isolated from Artocarpus heterophyllus heartwoods. A modified Boyden chamber was used to determine the chemotactic activity of human phagocyte. The respiratory burst was evaluated by chemiluminescence assay. Myeloperoxidase (MPO) activity was quantified using a colorimetric assay. The broth microdilution method was performed to assess their antibacterial activity.Results: Dihydromorin exhibited potent inhibitory effect on the chemotactic activity of polymorphonuclear neutrophils (PMNs) with an IC50 value of 5.03 μg/mL. Dihydromorin also inhibited reactive oxygen species production of whole blood cells, PMNs, and monocytes with IC50 values of 7.88, 7.59 and 7.24 μg/mL, respectively. Interestingly, dihydromorin also strongly inhibited the MPO activity of PMNs with an IC50 value of 5.24 μg/mL, which was lower than indomethacin (24.6 μg/mL). Molecular docking of dihydromorin and crystal structure of MPO showed that dihydromorin had close interaction with key amino acid residues such as Arg239 and Gln91. Antibacterial activity assay showed that only dihydromorin had a strong effect against Streptococcus pyogenes with MIC and MBC values of 15.62 and 31.25 μg/mL, respectively. Conclusions: The results suggest that dihydromorin could be developed as an anti-inflammatory and antibacterial agent.
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Phytochemical investigation on the liquid media of Pestalotiopsis microspora HF 12440, an endophytic fungusisolated from the stem of Artocarpus heterophyllus, led to the isolation of three lactones, (+)-acetylpestalotin (1),(−)-pestalotin (2), (6S,7S,8R)-hydroxypestalotin (3) and a lignan, (+)-pinoresinol (4). Interestingly, one of them (1)is a new compound, while compound 4 is reported for the first time from endophytic fungi. Structures of the isolatedcompounds were determined based on spectroscopic data, including MS, NMR 1D and 2D. Cytotoxic values of thecrude extract and all isolated compounds were evaluated against P388 cells, showing that compound 3 was the mostactive with IC50 3.34 μg/ml. Overall, this is the first phytochemical report of endophytic fungi isolated from the hostplant Artocarpus
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Artocarpus heterophyllus has been used as traditional medicine. This plant is one of the sources of flavonoid. Flavonoid compounds possessed a wide range of biological properties including anticancer. This study was performed to investigate the cytotoxic effect of flavonoids from A. heterophyllus on H460 and MCF-7 cell lines. The interaction of flavonoids and cisplatin against tested cancer cells was also evaluated. MTT assay was used to determine the cytotoxic effect of flavonoid. Isobologram analysis was selected to evaluate the synergistic effect between flavonoid and cisplatin, their interaction was then confirmed using AO/PI staining method. Amongst of flavonoid compounds, artocarpin exhibited strong cytotoxic effect on both MCF-7 and H460 cell lines with IC₅₀ values of 12.53 µg/mL (28.73 µM) and 9.77 µg/mL (22.40 µM), respectively. This compound enhanced anticancer activity of cisplatin against H460 and MCF-7. The combination produced a synergistic effect on H460 and MCF-7 cell lines with a combination index (CI) values of 0.2 and 0.18, respectively. The AO/PI stained demonstrated that the combination of artocarpin and cisplatin caused morphological changes that indicated apoptosis. Moreover, artocarpanone also significantly increased cytotoxic effect of cisplatin compared to its single concentration with CI below than 1. This result suggested the potency of flavonoid named artocarpin to enhance the anticancer activity of cisplatin on H460 and MCF-7 cell lines.
Subject(s)
Apoptosis , Artocarpus , Cell Line , Cisplatin , Flavonoids , MCF-7 Cells , Medicine, Traditional , Methods , PlantsABSTRACT
The ethyl acetate extracts obtained from under-ripe (Young Stage), mature (Mature Stage) and ripe fruit (Ripe Stage) fruit pulp of Artocarpus heterophyllus Lam. were evaluated for their Total Phenolic Content, Total Flavonoid Content and antioxidant property. Total Moisture Content and the Total Ash Content of pulp were determined by subjecting to heat treatment. Total Phenolic Content was evaluated using Folin-Ciocalteu method and Total Flavonoid Content by Aluminium Chloride Colorimetric Assay. Antioxidant activity was determined by DPPH Radical Scavenging, ABTS Radical Scavenging and FRAP Assays. The highest moisture content varies as Young Stage>Mature Stage>Ripe Stage in 84.71% to 70.38% range and Total Ash Content of the Ripe Stage pulp was the highest (6.86 %) and the least was observed for the Young Stage with a value of 5.40 %. For the Total Phenolic Content, crude extracts isolated from Mature Stage showed highest value (434.04 mg GAE/g) and Total Flavonoid Content was highest in crude extract of the Young Stage (446.79 mg QE/g). Ripe Stage Crude extract gave lowest value for both Total Phenolic Content and Total Flavonoid Content. For DPPH Radical Scavenging, ABTS Radical Scavenging and FRAP Assays, highest activity was reported by crude extract of Young Stage followed by crude extract of Mature Stage and least activity was given by crude extract of Ripe Stage. A correlation between Total Phenolic Content and Total Flavonoid Content with antioxidant activity was noticeable. A declination of the antioxidant activity was observed as the fruit reaches its maturity.
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@#<p style="text-align: justify;"><strong>BACKGROUND AND OBJECTIVE:</strong> Pectin is a complex polysaccharide which is commonly used as a gelling agent for food preparations and pharmaceutical formulations. Currently, the Philippines imports 100% of its pectin requirement from other countries which adds to the cost of products that utilizes pectin. Hence, the aim of this study was to isolate and characterize pectin from ripe jackfruit peels.</p><p style="text-align: justify;"><strong>MATERIALS AND METHODS: </strong>Peels of ripe jackfruit (Artocarpus heterophyllus Lam.) were subjected to digestion with water and sulfuric acid at 90°C then purified using alcohol and acetone. The isolated material from the peels was subjected to pectin identification tests using the methods from the US Pharmacopeia (USP). To further characterize the isolate, the methoxy and anhydrouronic acid contents, degree of esterification, functional groups (through FT-IR), ash content, and swelling index were determined.</p><p style="text-align: justify;"><strong>RESULTS:</strong> Ripe jackfruit peels yielded 5.74% of brown-colored pectin which was verified using the US Pharmacopeia identification tests for pectin. The methoxy and anhydrouronic acid contents were found to be 4.05% and 1.77%, respectively, with results comparable with the standard pectin (p<0.05). The peel's pectin has a degree of esterification of 26.34, 1.77% ash content, and swelling index of 9.09. FT-IR analysis of isolated pectin revealed functional groups identical to that of the standard pectin.</p><p style="text-align: justify;"><strong>CONCLUSION:</strong> Pectin from the ripe jackfruit peels is reported to be a potential source of pharmaceutical grade pectin. However, the AUA content and methoxy content of the isolated pectin did not meet the USP specification. Thus, the authors recommend that future investigators must optimize the isolation procedure to obtain pectin which meets the specification of USP.</p>
Subject(s)
PlantsABSTRACT
Ten isoprenylated flavonoids were isolated from 95% ethanol extraction of Artocarpus heterophyllus, with a combination of various chromatographic approaches, including ODS, MCI, CHP-20 P, Sephadex LH-20 and high performance liquid chromatography. On the basis of physic-chemical characters and spectroscopic data analysis, these compounds were identified as artoheteroid E (1), cycloheterophyllin (2), artelastoxanthone (3), artoindonesianin Q (4), cudraflavone C (5), 8-(γ,γ-dimethylallyl)-5,2',4'-trihydroxy-7-methoxyflavone (6), kuwanon T (7), 6-(3-methylbut-2-enyl) apigenin (8), 5,7,2',4'-tetrahydroxy-6-(3-methylbut-3-enyl) flavone (9), albanin A (10). Among them, compound 1 is a new one, while compounds 2-4 were isolated for the first time from the plant of Artocarpus heterophyllus. All isolated compounds were screened for their inhibitory abilities against cathepsin K. Of them, compounds 3-5, 7 and 10 showed inhibitory effects with the IC50 values of 0.9, 1.6, 4.5, 24.5 and 63.5 μmol·L-1, respectively.
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Objective To examine the anti-angiogenic potential of Artocarpus heterophyllus (A. heterophyllus) seed extract in chicken chorioallantoic membrane (CAM). Methods This study used chicken CAM ex ovo culture to examine the potential anti-angiogenic activity of A. heterophyllus seed methanolic extract. Basic fibroblast growth factor was used to induce the ectopic formation of blood vessels on CAM treated with extract. Blood vessel number was assessed by macroscopic and microscopic observation, and compared and analyzed for all treatments and controls. Results Macroscopic observation revealed that a dose of 35 μg/mL of methanolic extract of A. heterophyllus seeds could inhibit basic fibroblast growth factor-induced angiogenesis by 61% in chicken CAM ex ovo culture. This concurred with microscopic observations on the histological structure of blood vessels, which indicated that extract treatment repressed the formation of new blood vessels. Conclusions This is the first study to report the anti-angiogenic effect of methanolic extract derived from A. heterophyllus seeds and its potential as a candidate for future anticancer therapy.
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Objective To determine anti-viral activities of three Artocarpus species: Artocarpus altilis, Artocarpus camansi, and Artocarpus heterophyllus (A. heterophyllus) against Hepatitis C Virus (HCV). Methods Antiviral activities of the crude extracts were examined by cell culture method using Huh7it-1 cells and HCV genotype 2a strain JFH1. The mode of action for anti-HCV activities was determined by time-of-addition experiments. The effect on HCV RNA replication and HCV accumulation in cells were analyzed by quantitative reverse transcription-PCR and western blotting, respectively. Results The dichloromethane (DCM) extract of A. heterophyllus exhibited strong anti-HCV activity with an inhibitory concentration (IC
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Objective: To examine the anti-angiogenic potential of Artocarpus heterophyllus (A. heterophyllus) seed extract in chicken chorioallantoic membrane (CAM). Methods: This study used chicken CAM ex ovo culture to examine the potential anti-angiogenic activity of A. heterophyllus seed methanolic extract. Basic fibroblast growth factor was used to induce the ectopic formation of blood vessels on CAM treated with extract. Blood vessel number was assessed by macroscopic and microscopic observation, and compared and analyzed for all treatments and controls. Results: Macroscopic observation revealed that a dose of 35 μg/mL of methanolic extract of A. heterophyllus seeds could inhibit basic fibroblast growth factor-induced angiogenesis by 61% in chicken CAM ex ovo culture. This concurred with micro-scopic observations on the histological structure of blood vessels, which indicated that extract treatment repressed the formation of new blood vessels. Conclusions: This is the first study to report the anti-angiogenic effect of methanolic extract derived from A. heterophyllus seeds and its potential as a candidate for future anticancer therapy.
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Objective: To determine anti-viral activities of three Artocarpus species: Artocarpus altilis, Artocarpus camansi, and Artocarpus heterophyllus (A. heterophyllus) against Hepatitis C Virus (HCV). Methods: Antiviral activities of the crude extracts were examined by cell culture method using Huh7it-1 cells and HCV genotype 2a strain JFH1. The mode of action for anti-HCV activities was determined by time-of-addition experiments. The effect on HCV RNA replication and HCV accumulation in cells were analyzed by quantitative reverse transcription-PCR and western blotting, respectively. Results: The dichloromethane (DCM) extract of A. heterophyllus exhibited strong anti-HCV activity with an inhibitory concentration (IC50) value of (1.5 ± 0.6)μg/mL without obvious toxicity. The DCM extracts from Artocarpus altilis and Artocarpus camansi showed moderate anti-HCV activities with IC50 values being (6.5 ± 0.3) μg/mL and (9.7 ± 1.1) μg/mL, respectively. A time-of-addition studies showed that DCM extract from A. heterophyllus inhibited viral entry process though a direct virucidal activity and targeting host cells. HCV RNA replication and HCV protein expression were slightly reduced by the DCM treatment at high concentration. Conclusions: The DCM extract from A. heterophyllus is a good candidate to develop an antiviral agent to prevent HCV grant reinfection following liver transplantation.
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A reversed-phase high-performance liquid chromatographic method is described for the simultaneous determination of three antibacterial flavonoids, artocarpanone, artocarpin, and cycloartocarpin in ethyl acetate extracts from Artocarpus heterophyllus heartwoods. Separation was achieved using a TSK-gel ODS-80Tm column (5 µm, 4.6 × 150 mm) at 25℃ with a gradient elution system of methanol and water as follows: 0-8 min, 60:40; 8-27 min, 80:20; 27-35 min, 60:40, v/v, at a flow rate of 1 mL/min, and a quantitative UV detection at 285 nm. The method was validated by measuring the key parameters, including specificity, linearity, sensitivity, accuracy, repeatability and reproducibility. A high degree of specificity and sensitivity was achieved. The calibration curves for all three flavonoids showed good linearity with a coefficient of determinations (R²) of ≥ 0.9995. The recoveries of the method were from 98-104%, with good reproducibility and repeatability (RSD values of less than 2%) were also achieved. Ethyl acetate was the best solvent for extraction of these three flavonoids using the heat reflux conditions for 1 h. This optimized sample preparation and HPLC method can be practically used for a routine standardization process of the extracts from the A. heterophyllus heartwoods.
Subject(s)
Artocarpus , Calibration , Chromatography, High Pressure Liquid , Flavonoids , Hot Temperature , Methanol , Methods , Sensitivity and Specificity , WaterABSTRACT
Objective: To investigate the phenolic constituents from the roots of Artocarpus heterophyllus. Methods: Compounds were isolated from the roots of the plant by column chromatography over ODS, MCI GEL CHP-20P, Sephadex LH-20 and by preparative HPLC. Their structures were identified by the analysis of their physicochemical properties and the spectral data of NMR and MS. Results: Seventeen phenolic compounds were isolated from the roots of the plant, namely 1-O-feruloylglycerol (1), hypargystilbene A (2), oxyresveratrol (3), 2', 3, 4', 5, 5'-pentahydroxy-cis-stilbene (4), resveratrol (5), ethyl 2, 4-dihydroxybenzoate (6), ethyl 3, 4-dihydroxybenzoate (7), umbelliferone (8), 8-(3, 3-dimethylallyl)-6, 7-dihydroxycoumarin (9), morachalcone A (10), artocarpanone (11), styracifolin C (12), cudraflavone C (13), heterophyllin (14), cycloheterophyllin (15), artonin A (16), and artonin B (17). Conclusion: It is the first report of the occurrence of compound 9 as a natural product. Compounds 1, 4, and 6 are isolated from the plants of Moraceae family for the first time. Compound 8 is first obtained from the plants of Artocarpus J. R. et G. Forst., while compounds 3, 5, 10, 11, 14, and 15 are first found in A. heterophyllus.
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The aim of this work was to analyse the comparative effects of the antibacterial properties of partially purified lectins from the seeds of Artocarpus heterophyllus (jack fruit), Canavalia ensiformis (jack bean), Lens culinaris (lentil) and Pisum sativum (pea) against the bacteria Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa. The lectins were isolated by partial purification using ammonium sulphate precipitation and dialysis. The antimicrobial activity was studied using agar well diffusion method. The results showed that the Jack fruit lectin had a potent anti-bacterial activity against S. aureus, B. subtilis, E. coli and P. aeruginosa whereas Pea and jack bean lectin were found to be effective bacteriostatic agents which reduced the growth of bacteria and lentil lectin showed the least antibacterial activity. A comparison of the antibacterial activity of phytolectins with conventional antibiotics namely ampicillin and tetracycline was also carried out. Studies revealed that the antibacterial activities of the conventional antibiotics are higher than that of the plant extracts at the same concentration in accordance to literature.
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The aim of this work was to analyse the comparative effects of the antibacterial properties of partially purified lectins from the seeds of Artocarpus heterophyllus (jack fruit), Canavalia ensiformis (jack bean), Lens culinaris (lentil) and Pisum sativum (pea) against the bacteria Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa. The lectins were isolated by partial purification using ammonium sulphate precipitation and dialysis. The antimicrobial activity was studied using agar well diffusion method. The results showed that the Jack fruit lectin had a potent anti-bacterial activity against S. aureus, B. subtilis, E. coli and P. aeruginosa whereas Pea and jack bean lectin were found to be effective bacteriostatic agents which reduced the growth of bacteria and lentil lectin showed the least antibacterial activity. A comparison of the antibacterial activity of phytolectins with conventional antibiotics namely ampicillin and tetracycline was also carried out. Studies revealed that the antibacterial activities of the conventional antibiotics are higher than that of the plant extracts at the same concentration in accordance to literature.