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
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
Betelvine(Piper betle L.) is cultivated for its deep green heart shaped leaf for(15-20) million Indian and 2 billion foreign consumers annually. The crop provides Rs(6 000-7 000) million of national income per year an...Betelvine(Piper betle L.) is cultivated for its deep green heart shaped leaf for(15-20) million Indian and 2 billion foreign consumers annually. The crop provides Rs(6 000-7 000) million of national income per year and at the same time leaves worth Rs(30-40) million is exported to other countries. The leaves are not only used directly for chewing purposes but also possesses antioxidant, anti-inflammatory, anti-apoptotic, anti-cancer and anti-microbial properties. Besides, the leaves also contain eugenol rich essential oil(1%-3%) which is the source for medicine, stimulant, antiseptic, tonic and other ayurvedic formulations. The essential oil also contains chavibetol, caryophyllene and methyl eugenol which are the potent source for preparation in ayurvedic medicine and herbal products. Cost of betelvine essential oil is 10$ per 5 mL. In spite of its great economical and medicinal importance betelvine is still neglected by the researchers for proper characterization and authentication for selection of elite landraces. Lack of awareness among people, use of same planting material for many generations, existing of many synonyms for a single landraces, no proper characterization of available landraces are some of the significant constraints for its commercialization. Our review endeavours a complete advance in the research on betelvine, existing lacunae for its proper characterization and commercial cultivation. It also attempts to provide a comprehensive account on biotechnological interventions made in betelvine aimed at complementing conventional programmes for improvement of this nutraceutically important cash crop.展开更多
Activators of sesquiterpene synthase(STS) gene expression and sesquiterpene production in Piper betle L. were examined using quantitative real time PCR and gas chromatography mass spectrometry methods, and the allelop...Activators of sesquiterpene synthase(STS) gene expression and sesquiterpene production in Piper betle L. were examined using quantitative real time PCR and gas chromatography mass spectrometry methods, and the allelopathic activity of untreated and Fusarium solani-treated betel extracts was tested on seed germination and on the shoot and root growth of Thai rice variety PSL2(Oryza sativa cv. Phitsanulok 2) and three dominant paddy weeds(Eclipta prostrata, Echinochloa crus-galli and Chloris barbata). The results demonstrated that F. solani dramatically upregulated STS expression and productions of β-cubebene, β-caryophyllene and germacrene D sesquiterpene when compared with the untreated control, and that betel extracts had a greater inhibitory effect on weeds than on rice. The effects were more clearly detected on seed germination and root growth than on shoot growth, and they were found to be dose-dependent. It is also noted that F. solani-treated extract had stronger effects than the untreated extract. The species most sensitive to the allelopathic effects was C. barbata, germination of which was completely inhibited even at a dose of 0.1 mg/mL untreated extract. With regards to rice, although betel extract at 1.0 mg/mL showed no inhibition on germination, it affected the elongation of rice roots, in addition to those of the tested weeds. The obtained data suggested that F. solani has potential as an activator of sesquiterpene allelochemical production via STS expression, the latter leading to the treated betel extract having a stronger phytotoxic effect. These results were beneficial in the promotion of natural herbicide production using biotechnology.展开更多
The Piper betle,belonging to Piper genus of the Piperaceae family,is an evergreen and perennial creeper used in several traditional medicines.This plant has been known to possess antioxidant,antitumor,antibacterial,an...The Piper betle,belonging to Piper genus of the Piperaceae family,is an evergreen and perennial creeper used in several traditional medicines.This plant has been known to possess antioxidant,antitumor,antibacterial,anti-inflammatory and antimalarial activities.A wide range of chemical compounds including alkaloids,simple phenylpropanoids,lignans,flavonoids,steroids,triterpenoids,sesquiterpenes,monoterpenes have been isolated from this plant.The present review summarized the information concerning phytochemistry and biological activity of P.betle,providing references for the future research of this plant.展开更多
Piper nigrum L.,belonging to Piper genus of the Piperaceae family,is a medicinal and edible plant.Studies have shown that there are many chemical constituents in this plant,including alkaloids,lignans,steroids and oth...Piper nigrum L.,belonging to Piper genus of the Piperaceae family,is a medicinal and edible plant.Studies have shown that there are many chemical constituents in this plant,including alkaloids,lignans,steroids and other compounds.In addition,some chemical components of P.nigrum have potential values to treat cancer,inflammation and other diseases.Research progress on the chemical constituents and pharmacological effects of P.nigrum was reviewed in this study to better explore its potential medicinal value.展开更多
Parkinson’s disease(PD)is a common neurodegenerative disease.Despite a great deal of research on this disease,there is still no definitive treatment plan.Literature investigations have shown that Piper nigrum L.has a...Parkinson’s disease(PD)is a common neurodegenerative disease.Despite a great deal of research on this disease,there is still no definitive treatment plan.Literature investigations have shown that Piper nigrum L.has a protective effect on the nerve center.Therefore,network pharmacology was used in this study to investigate the therapeutic potential of P.nigrum for PD.As a result,six active alkaloid ingredients and four potential targets were obtained.This study laid the foundation for finding the lead compounds from P.nigrum to treat PD.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Betelvine(Piper betle L.) is cultivated for its deep green heart shaped leaf for(15-20) million Indian and 2 billion foreign consumers annually. The crop provides Rs(6 000-7 000) million of national income per year and at the same time leaves worth Rs(30-40) million is exported to other countries. The leaves are not only used directly for chewing purposes but also possesses antioxidant, anti-inflammatory, anti-apoptotic, anti-cancer and anti-microbial properties. Besides, the leaves also contain eugenol rich essential oil(1%-3%) which is the source for medicine, stimulant, antiseptic, tonic and other ayurvedic formulations. The essential oil also contains chavibetol, caryophyllene and methyl eugenol which are the potent source for preparation in ayurvedic medicine and herbal products. Cost of betelvine essential oil is 10$ per 5 mL. In spite of its great economical and medicinal importance betelvine is still neglected by the researchers for proper characterization and authentication for selection of elite landraces. Lack of awareness among people, use of same planting material for many generations, existing of many synonyms for a single landraces, no proper characterization of available landraces are some of the significant constraints for its commercialization. Our review endeavours a complete advance in the research on betelvine, existing lacunae for its proper characterization and commercial cultivation. It also attempts to provide a comprehensive account on biotechnological interventions made in betelvine aimed at complementing conventional programmes for improvement of this nutraceutically important cash crop.
基金graduate study (2016) from The National Research Council of Thailand (NRCT) for financial support
文摘Activators of sesquiterpene synthase(STS) gene expression and sesquiterpene production in Piper betle L. were examined using quantitative real time PCR and gas chromatography mass spectrometry methods, and the allelopathic activity of untreated and Fusarium solani-treated betel extracts was tested on seed germination and on the shoot and root growth of Thai rice variety PSL2(Oryza sativa cv. Phitsanulok 2) and three dominant paddy weeds(Eclipta prostrata, Echinochloa crus-galli and Chloris barbata). The results demonstrated that F. solani dramatically upregulated STS expression and productions of β-cubebene, β-caryophyllene and germacrene D sesquiterpene when compared with the untreated control, and that betel extracts had a greater inhibitory effect on weeds than on rice. The effects were more clearly detected on seed germination and root growth than on shoot growth, and they were found to be dose-dependent. It is also noted that F. solani-treated extract had stronger effects than the untreated extract. The species most sensitive to the allelopathic effects was C. barbata, germination of which was completely inhibited even at a dose of 0.1 mg/mL untreated extract. With regards to rice, although betel extract at 1.0 mg/mL showed no inhibition on germination, it affected the elongation of rice roots, in addition to those of the tested weeds. The obtained data suggested that F. solani has potential as an activator of sesquiterpene allelochemical production via STS expression, the latter leading to the treated betel extract having a stronger phytotoxic effect. These results were beneficial in the promotion of natural herbicide production using biotechnology.
文摘The Piper betle,belonging to Piper genus of the Piperaceae family,is an evergreen and perennial creeper used in several traditional medicines.This plant has been known to possess antioxidant,antitumor,antibacterial,anti-inflammatory and antimalarial activities.A wide range of chemical compounds including alkaloids,simple phenylpropanoids,lignans,flavonoids,steroids,triterpenoids,sesquiterpenes,monoterpenes have been isolated from this plant.The present review summarized the information concerning phytochemistry and biological activity of P.betle,providing references for the future research of this plant.
文摘Piper nigrum L.,belonging to Piper genus of the Piperaceae family,is a medicinal and edible plant.Studies have shown that there are many chemical constituents in this plant,including alkaloids,lignans,steroids and other compounds.In addition,some chemical components of P.nigrum have potential values to treat cancer,inflammation and other diseases.Research progress on the chemical constituents and pharmacological effects of P.nigrum was reviewed in this study to better explore its potential medicinal value.
文摘Parkinson’s disease(PD)is a common neurodegenerative disease.Despite a great deal of research on this disease,there is still no definitive treatment plan.Literature investigations have shown that Piper nigrum L.has a protective effect on the nerve center.Therefore,network pharmacology was used in this study to investigate the therapeutic potential of P.nigrum for PD.As a result,six active alkaloid ingredients and four potential targets were obtained.This study laid the foundation for finding the lead compounds from P.nigrum to treat PD.
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.
