Objective:To explore the effect of a hydrogel of Piper longum(P.longum)root against biofilm-forming multidrug-resistant(MDR)Staphylococcus aureus(S.aureus)through in vitro,in silico,and in vivo studies.Methods:We isol...Objective:To explore the effect of a hydrogel of Piper longum(P.longum)root against biofilm-forming multidrug-resistant(MDR)Staphylococcus aureus(S.aureus)through in vitro,in silico,and in vivo studies.Methods:We isolated the P.longum root ethanolic extract and the compounds using p-HPLC.In vitro antibacterial and antibiofilm activities of P.longum root extract and isolated alkamide compounds against biofilm-forming MDR S.aureus(ATCC 33591)were assessed using agar diffusion and broth microdilution methods,respectively.In silico investigations were conducted to investigate the interaction of alkamide compounds with three target proteins glycogen synthase kinase 3β(GSK3β),matrix metalloproteinases-8(MMP-8),and inducible nitric oxide synthase(iNOS).In addition,the wound healing effect of P.longum root extract 2%and 5%(w/v)-containing hydrogels was determined in mice.Results:The ethanolic root extract of P.longum and its compounds exhibited in vitro antibacterial activity with minimum inhibitory concentrations between 50µg/mL and 700µg/mL,as well as significantly reduced biofilm formation.Piperdardine isolated from P.longum root extract had the best molecular docking score(-9.7,-9.8,and-9.2 kcal/mol)with target proteins GSK3β,MMP-8,and iNOS.In vivo studies showed that P.longum hydrogels significantly lowered the number of colony-forming units(P<0.05).The P.longum 5%(w/v)hydrogel-treated group showed enhanced wound healing activity,achieving a wound contraction rate of 99.34%on day 14.Furthermore,histopathological analysis confirmed increased re-epithelialization and reduced inflammation in mice treated with P.longum 5%(w/v)hydrogel.Conclusions:P.longum root extract has pharmacological potential as an antibacterial and wound-healing agent,and further research is required to confirm its efficacy and clinical application.展开更多
Three new amide alkaloids piperlongumamides A-C(1-3),together with 12 known ones(4-15),were isolated from the fruits of Piper longum.The structures of the new isolates were determined using spectroscopic data analyses...Three new amide alkaloids piperlongumamides A-C(1-3),together with 12 known ones(4-15),were isolated from the fruits of Piper longum.The structures of the new isolates were determined using spectroscopic data analyses.Cytotoxic activity of these amides against HL-60(human leukemia),A-549(human lung cancer),MCF-7(human breast cancer),SMMC-7721(human liver cancer)and SW480(human rectal cancer)cell lines were evaluated.Piperchabamide B(11)exhibited weak inhibitory activity against HL-60(IC_(50)=21.32μM),A-549(IC_(50)=23.82μM)and MCF-7(IC_(50)=16.58μM)cell lines.展开更多
Piper sarmentosum Roxb.(Piperaceae)is a traditional medicinal and food plant widely distributed in the tropical and subtropical regions of Asia,offering both health and culinary benefits.In this study the secondary me...Piper sarmentosum Roxb.(Piperaceae)is a traditional medicinal and food plant widely distributed in the tropical and subtropical regions of Asia,offering both health and culinary benefits.In this study the secondary metabolites in different organs of P.sarmentosum were identified and their relative abundances were characterized.The metabolic profiles of leaves,roots,stems and fruits were comprehensively investigated by liquid chromatography high-resolution mass spectrometry(LC-HR-MS)and the data subsequently analyzed using multivariate statistical methods.Manual interpretation of the tandem mass spectrometric(MS/MS)fragmentation patterns revealed the presence of 154 tentatively identified metabolites,mostly represented by alkaloids and flavonoids.Principle component analysis and hierarchical clustering indicated the predominant occurrence of flavonoids,lignans and phenyl propanoids in leaves,aporphines in stems,piperamides in fruits and lignan-amides in roots.Overall,this study provides extensive data on the metabolite composition of P.sarmentosum,supplying useful information for bioactive compounds discovery and patterns of their preferential biosynthesis or storage in specific organs.This can be used to optimize production and harvesting as well as to maximize the plant’s economic value as herbal medicine or in food applications.展开更多
The identification of natural, plant-derived compounds with pesticidal properties is crucial for developing environmentally sustainable alternatives to synthetic pesticides. In this study, four major lignans—dihydroc...The identification of natural, plant-derived compounds with pesticidal properties is crucial for developing environmentally sustainable alternatives to synthetic pesticides. In this study, four major lignans—dihydroclusin, cubebin, clusin, and yatein—were isolated from the crude extract of Piper cubeba fruit. Phytotoxicity assays revealed herbicidal activity against Agrostis stolonifera, with dihydroclusin and clusin exhibiting the highest efficacy, inhibiting seed germination by 50% and showing IC50 values of 2.9 µM and 45 µM, respectively, against Lemna paucicostata. Additionally, all compounds, except dihydroclusin, demonstrated fungicidal activity against the strawberry anthracnose pathogen Colletotrichum fragariae. Moreover, only dihydroclusin exhibited larvicidal activity against Aedes aegypti, causing 96% mortality of mosquito larvae at the 100-ppm concentration tested. These findings highlight the broad-spectrum bioactivity of Piper cubeba lignans, suggesting their potential as alternative agents of synthetic pesticides for managing agricultural pests.展开更多
Aim To investigate the chemical constituents of Piper wallichii. Methods Five compounds were isolated by silica gel column chromatography and Sephadex LH-20 gel column chromatography, and the structures of compounds w...Aim To investigate the chemical constituents of Piper wallichii. Methods Five compounds were isolated by silica gel column chromatography and Sephadex LH-20 gel column chromatography, and the structures of compounds were identified by spectral analysis. Result Five compounds were identified as piperlonguminine （trans, trans） （1）, 4-hydroxy-3,5-dimethoxy-benzoic acid （2）, galgravin （3）, β-sitosterol （4）, and daucosterol （5）. Conclusion Five compounds were isolated from Piper wallichii for the first time, and compounds 1 -3 were isolated from this genus far the first time.展开更多
The aim of the research was to discuss the genetic relationships between Piper methysticum, Pepper and other wild species in Pepper genus. DNA was extracted from leaves which belonged to 28 germplasms including 6 mate...The aim of the research was to discuss the genetic relationships between Piper methysticum, Pepper and other wild species in Pepper genus. DNA was extracted from leaves which belonged to 28 germplasms including 6 materials of P. methysticum, 21 maerials of cultivated and wild Pepper, 1 material of Peperomia pellucida belonged to different genus. Premiers with good band-type and high polymorphism and resolution were selected from 64 pairs of primers for AFLP amplification and the clustering analysis was conducted with MVSP3.13f software. 191 bands were amplified by 4 pairs of premiers, 189 of which had polymorphism, being 98.6%. 28 germplasms were classified into 6 different groups at the genetic similarity coefficient of 0.52 by silver staining AFLP, in which 6 materials of Piper methysticum were clustered into a single group, indicating that P. methysticum belonged to Pepper family of Pepper genus but were distantly related to the others. The research provided the basis for selecting rootstocks for P. methysticum graft, molecular identification of P. methysticum and the fingerprint construction of P. methysticum.展开更多
Objective:To carry out the physicochemical and phytochemical standardization with high performance thin layer chromatography fingerprinting of Piper nigrum L.(P.nigrum)fruits in order to ascertain the standard pharmac...Objective:To carry out the physicochemical and phytochemical standardization with high performance thin layer chromatography fingerprinting of Piper nigrum L.(P.nigrum)fruits in order to ascertain the standard pharmacognostical parameters of this king of spices.Methods:Many standardization parameters like extractive values,total ash value,water soluble ash value and acid insoluble ash,moisture content,loss on drying and pH values of P.nigrum L.fruits were analyzed.The method of Harborne was adopted for the preliminary phytochemicals screening.Analysis of total phenolic and flavonoid contents,pesticides residues,aflatoxin and heavy metals were also performed.CAMAG-high performance thin layer chromatography system was used for fingerprinting of methanolic extract of P.nigrum L.fruits.Results:The results of phytochemicals testing indicated the presence of carbohydrates,phenolic compounds,flavonoids,alkaloids,proteins,saponins,lipids,sterols and tannins in various solvent extracts.Total phenolic and flavonoid contents in methanolic extract were found to be 1.728 1 mg/g and 1.087 ug/g,respectively.Heavy metals concentrations were found to be within standard limits.Aflatoxins and pesticides residues were absent.Conclusions:The outcome of this study might prove beneficial in herbal industries for identification,purification and standardization of P.nigrum L.fruits.展开更多
Objective： The combination effect of Piperbetle （PB） and 5-fluorouracil （5-FU） in enhancing the cytotoxic potential of 5-FU in inhibiting the growth of colon cancer cells was investigated. Methods： HT29 and HCT1...Objective： The combination effect of Piperbetle （PB） and 5-fluorouracil （5-FU） in enhancing the cytotoxic potential of 5-FU in inhibiting the growth of colon cancer cells was investigated. Methods： HT29 and HCT116 cells were subjected to 5-FU or PB treatment. 5-FU and PB were then combined and their effects on both cell lines were observed after 24 h of treatment. PB-5-FU interaction was elucidated by isobologram analysis. Apoptosis features of the treated cells were revealed by annexin V/PI stain. High-performance liquid chromatography （HPLC） was performed to exclude any possible chemical interaction between the compounds. Results： In the presence of PB extract, the cytotoxicity of 5-FU was observed at a lower dose （IC^0 12.5 pmol/L） and a shorter time （24 h） in both cell lines. Both cell lines treated with 5-FU or PB alone induced a greater apoptosis effect compared with the combination treatment. Isobologram analysis indicated that PB and 5-FU interacted synergistically and antagonistically in inhibiting the growth of HT29 and HCT116 cells, respectively. Conclusions： In the presence of PB, a lower dosage of 5-FU is required to achieve the maximum drug effect in inhibiting the growth of HT29 cells. However, PB did not significantly reduce 5-FU dosage in HCT116 cells. Our result showed that this interaction may not solely contribute to the apoptosis pathway.展开更多
This paper describes the detailed anatomy and micromorphology of the vegetative parts of Piper sarmentosum Roxb. (synonym, P. lolot C.DC.), which is a southeast Asian medicinal plant valued for its medicinal and culin...This paper describes the detailed anatomy and micromorphology of the vegetative parts of Piper sarmentosum Roxb. (synonym, P. lolot C.DC.), which is a southeast Asian medicinal plant valued for its medicinal and culinary uses. The study also compares the anatomy of the leaf, petiole, stem and root of P. sarmentosum with those of the well-characterized P. betle L. The leaves of both the species are morphologically comparable and have similar culinary uses. The present study showed that the leaves of both the species possess more or less comparable anatomical features with a few differences;whereas, the microscopic features of the petiole, stem, and root of the two species are distinctive.展开更多
One undescribedamide,pipermullesine A,twoundescribed isoquinoline alkaloids,pipermullesinesBand C,and six undescribed dipeptides,pipermullamides A–F,along with 28 known compounds,were isolated from the aerial parts o...One undescribedamide,pipermullesine A,twoundescribed isoquinoline alkaloids,pipermullesinesBand C,and six undescribed dipeptides,pipermullamides A–F,along with 28 known compounds,were isolated from the aerial parts of Piper mullesua.The structures of the undescribed compounds were elucidated based on the analysis of 1D and 2D NMR and MS data.Furthermore,the structures of pipermullesines A–Cwere confirmed by single crystal X-ray diffraction analysis.All isolates were evaluated for inhibitory activity against platelet aggregation induced by thrombin(IIa)or platelet-activating factor(PAF).(-)-Mangochinine,pellitorine,and(2E,4E)-N-isobutyl-2,4-dodecadienamide showed weak inhibitory activity against rabbit platelet aggregation induced by PAF,with IC_(50)values of 470.3μg/mL,614.9μg/mL,and 579.7μg/mL,respectively.展开更多
Three new cyclohexene epoxides,polysyphoside A,B and C,along with a known compound crotepoxide(4),were isolated from Piper polysyphorum C.DC.Based on spectroscopic analysis,their structures were established as 1-benzo...Three new cyclohexene epoxides,polysyphoside A,B and C,along with a known compound crotepoxide(4),were isolated from Piper polysyphorum C.DC.Based on spectroscopic analysis,their structures were established as 1-benzoyloxymethylene-2-hydroxy-3-benzoyloxy-1,6- epoxycyclohex-4-ene(1),1-benzoyloxymethylene-2-hydroxy-5-benzoyloxy-1,6-epoxycyclohex-3-ene (2)and 2-hydroxy-3-benzoyloxymethylene-5-benzoyloxy-1,6-epoxycyclohex-3-ene(3),respectively.It was the first time that(1),(2)and(3)had been isolated from a natural source.展开更多
In order to clarify the insecticidal active ingredients of Piper sarmentosum,one active ingredient was isolated from ethanol extract of P. sarmentosum by bioassay-guided fractionation method. Its chemical structures w...In order to clarify the insecticidal active ingredients of Piper sarmentosum,one active ingredient was isolated from ethanol extract of P. sarmentosum by bioassay-guided fractionation method. Its chemical structures were identified to be piperine by MS,1H NMR,13C NMR. The insecticidal activity of piperine and ethanol extract of P. sarmentosum against Aleurodicus dispels Russell were tested by leaf dip method. The results showed that piperine and ethanol extract of P. sarmentosum exhibited strong insecticidal activity against adults and nymphs of A. dispels; LC50values against adults were 28. 59 and 224. 31 mg/L,and LC50values against nymphs were 65. 91 and 336. 68 mg/L,respectively. There was no significant difference between piperine and azadirachtin against adults and nymphs of A.dispels. Therefore,piperine might be one of the main insecticidal ingredients of P. sarmentosum. In addition,piperine and ethanol extract showed ovicidal activity with different mode of action,piperine reduced the survival rate of newly hatched nymphs while ethanol extract impacted hatch of eggs.展开更多
Two new amides(E)-N-cinnamoyl-2-methoxypiperidine(1)and(R)-1-(2-oxopyrrolidin-3-yl)-5,6-dihydropyridin-2(1H)-one(2),four new amide glucosides,retrofractosides A-D(3-6),and two new phenylpropanoid glucosides,retrofract...Two new amides(E)-N-cinnamoyl-2-methoxypiperidine(1)and(R)-1-(2-oxopyrrolidin-3-yl)-5,6-dihydropyridin-2(1H)-one(2),four new amide glucosides,retrofractosides A-D(3-6),and two new phenylpropanoid glucosides,retrofractosides E(7)and F(8),together with 24 known compounds(9-32)were isolated from the fruits of Piper retrofractum.The chemical structures of these new compounds were elucidated based on extensive spectroscopic analysis.All of these isolates(1-32)were evaluated for inhibitory activity against mouse platelet aggregation induced by the peptide AYPGKF-NH2.(E)-N-(Tetrahydro-2H-pyran-2-yl)cinnamamide(9)showed a weak inhibitory efect,with an inhibition ratio of 52.0%at a concentration of 150μM.展开更多
In the pharmaceutical world the majority of the active pharmaceutical ingredients (API) have been obtained from the natural products. Piperine is such naturally occurring alkaloid which can be considered as major bioa...In the pharmaceutical world the majority of the active pharmaceutical ingredients (API) have been obtained from the natural products. Piperine is such naturally occurring alkaloid which can be considered as major bioactive phytochemical having broad spectrum of pharmacological activities. It is obtained from the most valuable ethnomedicinal spices peppercorns i.e. black pepper and white pepper, which are the fruits of the Asian vine Piper nigrum L. Because of the widespread traditional uses of this medicinal compound, present article reveals a simple and effective isolation method of bulk piperine. The novelty of this investigation is to provide an idea for utilizing such natural method of large scale commercial piperine production as API drug in spite of chemical synthesis. Piperine was isolated in a pure crystal form and characterized by its melting point, X-Ray diffraction (XRD) studies and spectral data, including two-dimensional nuclear magnetic resonance (2D-NMR) spectroscopy. Chromatographic techniques like Thin Layer Chromatography (TLC) and High Performance Liquid Chromatography (HPLC) were applied to determine the purity of the yielded piperine. It was found that piperine yield from black pepper was within 2.5% - 3.0% and from white pepper within 4.0% - 4.5% and the purity of the yielded piperine was found to be up to 98.5% for black pepper and 98.2% for white pepper. Considering this yield value and purity it is indicated that, such effective isolation method can be successfully utilized for industrial large-scale production commercially. According to the result, it can be claimed that, as a natural product the isolated piperine can also be utilized as API drug like other expensive chemically synthesized piperine in different drug formulation.展开更多
基金supported by NPDF fellowship grants from the Central Council for Research in Ayurvedic Sciences,Ministry of AYUSH,Govt.of India(HQ-ESTT012/60/2022-ESTT/6783).
文摘Objective:To explore the effect of a hydrogel of Piper longum(P.longum)root against biofilm-forming multidrug-resistant(MDR)Staphylococcus aureus(S.aureus)through in vitro,in silico,and in vivo studies.Methods:We isolated the P.longum root ethanolic extract and the compounds using p-HPLC.In vitro antibacterial and antibiofilm activities of P.longum root extract and isolated alkamide compounds against biofilm-forming MDR S.aureus(ATCC 33591)were assessed using agar diffusion and broth microdilution methods,respectively.In silico investigations were conducted to investigate the interaction of alkamide compounds with three target proteins glycogen synthase kinase 3β(GSK3β),matrix metalloproteinases-8(MMP-8),and inducible nitric oxide synthase(iNOS).In addition,the wound healing effect of P.longum root extract 2%and 5%(w/v)-containing hydrogels was determined in mice.Results:The ethanolic root extract of P.longum and its compounds exhibited in vitro antibacterial activity with minimum inhibitory concentrations between 50µg/mL and 700µg/mL,as well as significantly reduced biofilm formation.Piperdardine isolated from P.longum root extract had the best molecular docking score(-9.7,-9.8,and-9.2 kcal/mol)with target proteins GSK3β,MMP-8,and iNOS.In vivo studies showed that P.longum hydrogels significantly lowered the number of colony-forming units(P<0.05).The P.longum 5%(w/v)hydrogel-treated group showed enhanced wound healing activity,achieving a wound contraction rate of 99.34%on day 14.Furthermore,histopathological analysis confirmed increased re-epithelialization and reduced inflammation in mice treated with P.longum 5%(w/v)hydrogel.Conclusions:P.longum root extract has pharmacological potential as an antibacterial and wound-healing agent,and further research is required to confirm its efficacy and clinical application.
基金This work was funded by the Natural Science Foundation of Yunnan Province,China(No.2011FZ205)the National Natural Science Foundation of China(Nos.31070288,31161140345)+1 种基金the Ministry of Education of China through its 111 and 985 projects(Nos.B08044,MUC98506-01000101&MUC985-9)the Japan Society for the Promotion of Science(No.JSPS/AP/109080).
文摘Three new amide alkaloids piperlongumamides A-C(1-3),together with 12 known ones(4-15),were isolated from the fruits of Piper longum.The structures of the new isolates were determined using spectroscopic data analyses.Cytotoxic activity of these amides against HL-60(human leukemia),A-549(human lung cancer),MCF-7(human breast cancer),SMMC-7721(human liver cancer)and SW480(human rectal cancer)cell lines were evaluated.Piperchabamide B(11)exhibited weak inhibitory activity against HL-60(IC_(50)=21.32μM),A-549(IC_(50)=23.82μM)and MCF-7(IC_(50)=16.58μM)cell lines.
基金supported by the German Academic Exchange Service(DAAD)as a grant scholarship and part of the Ph.D.thesis of IW.Funding program/-ID:Research Grants-Doctoral Programs in Germany,2017/18(57299294),ST34.
文摘Piper sarmentosum Roxb.(Piperaceae)is a traditional medicinal and food plant widely distributed in the tropical and subtropical regions of Asia,offering both health and culinary benefits.In this study the secondary metabolites in different organs of P.sarmentosum were identified and their relative abundances were characterized.The metabolic profiles of leaves,roots,stems and fruits were comprehensively investigated by liquid chromatography high-resolution mass spectrometry(LC-HR-MS)and the data subsequently analyzed using multivariate statistical methods.Manual interpretation of the tandem mass spectrometric(MS/MS)fragmentation patterns revealed the presence of 154 tentatively identified metabolites,mostly represented by alkaloids and flavonoids.Principle component analysis and hierarchical clustering indicated the predominant occurrence of flavonoids,lignans and phenyl propanoids in leaves,aporphines in stems,piperamides in fruits and lignan-amides in roots.Overall,this study provides extensive data on the metabolite composition of P.sarmentosum,supplying useful information for bioactive compounds discovery and patterns of their preferential biosynthesis or storage in specific organs.This can be used to optimize production and harvesting as well as to maximize the plant’s economic value as herbal medicine or in food applications.
文摘The identification of natural, plant-derived compounds with pesticidal properties is crucial for developing environmentally sustainable alternatives to synthetic pesticides. In this study, four major lignans—dihydroclusin, cubebin, clusin, and yatein—were isolated from the crude extract of Piper cubeba fruit. Phytotoxicity assays revealed herbicidal activity against Agrostis stolonifera, with dihydroclusin and clusin exhibiting the highest efficacy, inhibiting seed germination by 50% and showing IC50 values of 2.9 µM and 45 µM, respectively, against Lemna paucicostata. Additionally, all compounds, except dihydroclusin, demonstrated fungicidal activity against the strawberry anthracnose pathogen Colletotrichum fragariae. Moreover, only dihydroclusin exhibited larvicidal activity against Aedes aegypti, causing 96% mortality of mosquito larvae at the 100-ppm concentration tested. These findings highlight the broad-spectrum bioactivity of Piper cubeba lignans, suggesting their potential as alternative agents of synthetic pesticides for managing agricultural pests.
文摘Aim To investigate the chemical constituents of Piper wallichii. Methods Five compounds were isolated by silica gel column chromatography and Sephadex LH-20 gel column chromatography, and the structures of compounds were identified by spectral analysis. Result Five compounds were identified as piperlonguminine （trans, trans） （1）, 4-hydroxy-3,5-dimethoxy-benzoic acid （2）, galgravin （3）, β-sitosterol （4）, and daucosterol （5）. Conclusion Five compounds were isolated from Piper wallichii for the first time, and compounds 1 -3 were isolated from this genus far the first time.
基金Supported by the National Key Project of Tenth-five Year Plan(2001BA707B)School Foundation Program of Henan Science and Technology University~~
文摘The aim of the research was to discuss the genetic relationships between Piper methysticum, Pepper and other wild species in Pepper genus. DNA was extracted from leaves which belonged to 28 germplasms including 6 materials of P. methysticum, 21 maerials of cultivated and wild Pepper, 1 material of Peperomia pellucida belonged to different genus. Premiers with good band-type and high polymorphism and resolution were selected from 64 pairs of primers for AFLP amplification and the clustering analysis was conducted with MVSP3.13f software. 191 bands were amplified by 4 pairs of premiers, 189 of which had polymorphism, being 98.6%. 28 germplasms were classified into 6 different groups at the genetic similarity coefficient of 0.52 by silver staining AFLP, in which 6 materials of Piper methysticum were clustered into a single group, indicating that P. methysticum belonged to Pepper family of Pepper genus but were distantly related to the others. The research provided the basis for selecting rootstocks for P. methysticum graft, molecular identification of P. methysticum and the fingerprint construction of P. methysticum.
基金Supported by AYUSH.Ministry of Health and Family Welfare.Government of India[Grant No.CCRUM-UPC-Ⅱ(3-15/2009.CCRUM/UPC)]
文摘Objective:To carry out the physicochemical and phytochemical standardization with high performance thin layer chromatography fingerprinting of Piper nigrum L.(P.nigrum)fruits in order to ascertain the standard pharmacognostical parameters of this king of spices.Methods:Many standardization parameters like extractive values,total ash value,water soluble ash value and acid insoluble ash,moisture content,loss on drying and pH values of P.nigrum L.fruits were analyzed.The method of Harborne was adopted for the preliminary phytochemicals screening.Analysis of total phenolic and flavonoid contents,pesticides residues,aflatoxin and heavy metals were also performed.CAMAG-high performance thin layer chromatography system was used for fingerprinting of methanolic extract of P.nigrum L.fruits.Results:The results of phytochemicals testing indicated the presence of carbohydrates,phenolic compounds,flavonoids,alkaloids,proteins,saponins,lipids,sterols and tannins in various solvent extracts.Total phenolic and flavonoid contents in methanolic extract were found to be 1.728 1 mg/g and 1.087 ug/g,respectively.Heavy metals concentrations were found to be within standard limits.Aflatoxins and pesticides residues were absent.Conclusions:The outcome of this study might prove beneficial in herbal industries for identification,purification and standardization of P.nigrum L.fruits.
基金supported by the Ministry of Higher Education,Malaysia(No.UKM-JJ-03-FRGS0044-2010)Universiti Kebangsaan Malaysia(No.UKM-DPP-2014-131)
文摘Objective： The combination effect of Piperbetle （PB） and 5-fluorouracil （5-FU） in enhancing the cytotoxic potential of 5-FU in inhibiting the growth of colon cancer cells was investigated. Methods： HT29 and HCT116 cells were subjected to 5-FU or PB treatment. 5-FU and PB were then combined and their effects on both cell lines were observed after 24 h of treatment. PB-5-FU interaction was elucidated by isobologram analysis. Apoptosis features of the treated cells were revealed by annexin V/PI stain. High-performance liquid chromatography （HPLC） was performed to exclude any possible chemical interaction between the compounds. Results： In the presence of PB extract, the cytotoxicity of 5-FU was observed at a lower dose （IC^0 12.5 pmol/L） and a shorter time （24 h） in both cell lines. Both cell lines treated with 5-FU or PB alone induced a greater apoptosis effect compared with the combination treatment. Isobologram analysis indicated that PB and 5-FU interacted synergistically and antagonistically in inhibiting the growth of HT29 and HCT116 cells, respectively. Conclusions： In the presence of PB, a lower dosage of 5-FU is required to achieve the maximum drug effect in inhibiting the growth of HT29 cells. However, PB did not significantly reduce 5-FU dosage in HCT116 cells. Our result showed that this interaction may not solely contribute to the apoptosis pathway.
文摘This paper describes the detailed anatomy and micromorphology of the vegetative parts of Piper sarmentosum Roxb. (synonym, P. lolot C.DC.), which is a southeast Asian medicinal plant valued for its medicinal and culinary uses. The study also compares the anatomy of the leaf, petiole, stem and root of P. sarmentosum with those of the well-characterized P. betle L. The leaves of both the species are morphologically comparable and have similar culinary uses. The present study showed that the leaves of both the species possess more or less comparable anatomical features with a few differences;whereas, the microscopic features of the petiole, stem, and root of the two species are distinctive.
基金This work was funded by the Southeast Asia Biodiversity Research Institute,Chinese Academy of Sciences(Y4ZK111B01)the Natural Science Foundation of Yunnan Province,China(2011FZ205)+2 种基金the International Partneship Program of Chinese Academy of Sciences(153631KYSB20160004)the Key Laboratory of Ethnomedicine(Minzu University of China)of Ministry of Education of China(KLEM-ZZ201806)the National Natural Science Foundation of China(31761143001&31161140345).
文摘One undescribedamide,pipermullesine A,twoundescribed isoquinoline alkaloids,pipermullesinesBand C,and six undescribed dipeptides,pipermullamides A–F,along with 28 known compounds,were isolated from the aerial parts of Piper mullesua.The structures of the undescribed compounds were elucidated based on the analysis of 1D and 2D NMR and MS data.Furthermore,the structures of pipermullesines A–Cwere confirmed by single crystal X-ray diffraction analysis.All isolates were evaluated for inhibitory activity against platelet aggregation induced by thrombin(IIa)or platelet-activating factor(PAF).(-)-Mangochinine,pellitorine,and(2E,4E)-N-isobutyl-2,4-dodecadienamide showed weak inhibitory activity against rabbit platelet aggregation induced by PAF,with IC_(50)values of 470.3μg/mL,614.9μg/mL,and 579.7μg/mL,respectively.
文摘Three new cyclohexene epoxides,polysyphoside A,B and C,along with a known compound crotepoxide(4),were isolated from Piper polysyphorum C.DC.Based on spectroscopic analysis,their structures were established as 1-benzoyloxymethylene-2-hydroxy-3-benzoyloxy-1,6- epoxycyclohex-4-ene(1),1-benzoyloxymethylene-2-hydroxy-5-benzoyloxy-1,6-epoxycyclohex-3-ene (2)and 2-hydroxy-3-benzoyloxymethylene-5-benzoyloxy-1,6-epoxycyclohex-3-ene(3),respectively.It was the first time that(1),(2)and(3)had been isolated from a natural source.
基金Supported by Fundamental Research Fund of Chinese Academy of Tropical Agricultural Science(1630042013017)Special Fund for Agro-scientific Research in the Public Interest(201103026-1)+2 种基金Fundamental Research Fund for Central-level Nonprofit Research Institutes(Young Talents in Tropical Agriculture)(2013hzs1J002)Natural Science Foundation of Hainan Province of China(310086,313083)Natural Science Foundation of China(31101465)
文摘In order to clarify the insecticidal active ingredients of Piper sarmentosum,one active ingredient was isolated from ethanol extract of P. sarmentosum by bioassay-guided fractionation method. Its chemical structures were identified to be piperine by MS,1H NMR,13C NMR. The insecticidal activity of piperine and ethanol extract of P. sarmentosum against Aleurodicus dispels Russell were tested by leaf dip method. The results showed that piperine and ethanol extract of P. sarmentosum exhibited strong insecticidal activity against adults and nymphs of A. dispels; LC50values against adults were 28. 59 and 224. 31 mg/L,and LC50values against nymphs were 65. 91 and 336. 68 mg/L,respectively. There was no significant difference between piperine and azadirachtin against adults and nymphs of A.dispels. Therefore,piperine might be one of the main insecticidal ingredients of P. sarmentosum. In addition,piperine and ethanol extract showed ovicidal activity with different mode of action,piperine reduced the survival rate of newly hatched nymphs while ethanol extract impacted hatch of eggs.
基金supported by the Southeast Asia Biodiversity Research Institute,Chinese Academy of Sciences(2015CASEABRIRG001 and Y4ZK111B01)the open foundation of Key Laboratory of Ethnomedicine(Minzu University of China),Ministry of Education(KLEM-KF2018Z01)the International Partnership Program of Chinese Academy of Sciences(153631KYSB20160004).
文摘Two new amides(E)-N-cinnamoyl-2-methoxypiperidine(1)and(R)-1-(2-oxopyrrolidin-3-yl)-5,6-dihydropyridin-2(1H)-one(2),four new amide glucosides,retrofractosides A-D(3-6),and two new phenylpropanoid glucosides,retrofractosides E(7)and F(8),together with 24 known compounds(9-32)were isolated from the fruits of Piper retrofractum.The chemical structures of these new compounds were elucidated based on extensive spectroscopic analysis.All of these isolates(1-32)were evaluated for inhibitory activity against mouse platelet aggregation induced by the peptide AYPGKF-NH2.(E)-N-(Tetrahydro-2H-pyran-2-yl)cinnamamide(9)showed a weak inhibitory efect,with an inhibition ratio of 52.0%at a concentration of 150μM.
文摘In the pharmaceutical world the majority of the active pharmaceutical ingredients (API) have been obtained from the natural products. Piperine is such naturally occurring alkaloid which can be considered as major bioactive phytochemical having broad spectrum of pharmacological activities. It is obtained from the most valuable ethnomedicinal spices peppercorns i.e. black pepper and white pepper, which are the fruits of the Asian vine Piper nigrum L. Because of the widespread traditional uses of this medicinal compound, present article reveals a simple and effective isolation method of bulk piperine. The novelty of this investigation is to provide an idea for utilizing such natural method of large scale commercial piperine production as API drug in spite of chemical synthesis. Piperine was isolated in a pure crystal form and characterized by its melting point, X-Ray diffraction (XRD) studies and spectral data, including two-dimensional nuclear magnetic resonance (2D-NMR) spectroscopy. Chromatographic techniques like Thin Layer Chromatography (TLC) and High Performance Liquid Chromatography (HPLC) were applied to determine the purity of the yielded piperine. It was found that piperine yield from black pepper was within 2.5% - 3.0% and from white pepper within 4.0% - 4.5% and the purity of the yielded piperine was found to be up to 98.5% for black pepper and 98.2% for white pepper. Considering this yield value and purity it is indicated that, such effective isolation method can be successfully utilized for industrial large-scale production commercially. According to the result, it can be claimed that, as a natural product the isolated piperine can also be utilized as API drug like other expensive chemically synthesized piperine in different drug formulation.
