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 activ...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 antiHCV activity with an inhibitory concentration(IC_(50)) value of(1.5 ± 0.6) mg/mL without obvious toxicity. The DCM extracts from Artocarpus altilis and Artocarpus camansi showed moderate anti-HCV activities with IC_(50) values being(6.5 ± 0.3) mg/mL and(9.7 ± 1.1) mg/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.展开更多
Objective:To evaluate the immunosuppressive effect on human phagocytes and antibacterial activity of dihydromorin and norartocarpetin isolated from Artocarpus heterophyllus heartwoods.Methods:Dihydromorin and norartoc...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 5.03μg/mL.Dihydromorin also inhibited reactive oxygen species production of whole blood cells,PMNs,and monocytes with IC50 values of 7.88,7.59 and 7.24μg/mL,respectively.Interestingly,dihydromorin also strongly inhibited the MPO activity of PMNs with an IC50 value of 5.24μg/mL,which was lower than indomethacin(24.6μg/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 31.25μg/mL,respectively.Conclusions:The results suggest that dihydromorin could be developed as an anti-inflammatory and antibacterial agent.展开更多
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 th...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 antiangiogenic 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 mg/m L 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.展开更多
One new 2-arylbenzofuran derivative, artocarstilbene B（1）, one new benzaldehyde derivative,（E）-3,5-dihydroxy-4-（3-methylbut-1-enyl）benzaldehyde（2）, as well as 18 known compounds（3–20） were obtained from the...One new 2-arylbenzofuran derivative, artocarstilbene B（1）, one new benzaldehyde derivative,（E）-3,5-dihydroxy-4-（3-methylbut-1-enyl）benzaldehyde（2）, as well as 18 known compounds（3–20） were obtained from the leaves of Artocarpus heterophyllus. Their structures were elucidated on the basis of extensive spectroscopic techniques including 2D NMR and HR-ESIMS. Many compounds exhibited moderate to weak inhibitory activity against the proliferation of the PC-3, NCI-H460, and A549 cancer cell lines.展开更多
基金supported in part by Mandat Project Airlangga University and Science and Technology Research Partnerships for Sustainable Development (SATREPS) program from Japan Science and Technology Agency (JST) and Japan International Cooperation Agency (JICA)
文摘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 antiHCV activity with an inhibitory concentration(IC_(50)) value of(1.5 ± 0.6) mg/mL without obvious toxicity. The DCM extracts from Artocarpus altilis and Artocarpus camansi showed moderate anti-HCV activities with IC_(50) values being(6.5 ± 0.3) mg/mL and(9.7 ± 1.1) mg/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.
基金supported by Universiti Kebangsaan Malaysia(grant no.AP2014-023)
文摘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 5.03μg/mL.Dihydromorin also inhibited reactive oxygen species production of whole blood cells,PMNs,and monocytes with IC50 values of 7.88,7.59 and 7.24μg/mL,respectively.Interestingly,dihydromorin also strongly inhibited the MPO activity of PMNs with an IC50 value of 5.24μg/mL,which was lower than indomethacin(24.6μg/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 31.25μg/mL,respectively.Conclusions:The results suggest that dihydromorin could be developed as an anti-inflammatory and antibacterial agent.
基金Supported by Beasiswa Unggulan Directorate General of Higher Education 2012,and BOPTN-WUR,Universitas Gadjah Mada(Grant No.578A/KJM/XI/2015)
文摘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 antiangiogenic 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 mg/m L 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.
基金Financial supports from National Natural Science Foundation of China (No. 31500280)Shandong Provincial Natural Science Foundation, China (No. ZR2015PC006)
文摘One new 2-arylbenzofuran derivative, artocarstilbene B（1）, one new benzaldehyde derivative,（E）-3,5-dihydroxy-4-（3-methylbut-1-enyl）benzaldehyde（2）, as well as 18 known compounds（3–20） were obtained from the leaves of Artocarpus heterophyllus. Their structures were elucidated on the basis of extensive spectroscopic techniques including 2D NMR and HR-ESIMS. Many compounds exhibited moderate to weak inhibitory activity against the proliferation of the PC-3, NCI-H460, and A549 cancer cell lines.
