Context: In the last decade, resistance to epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs) in lung cancer cases has been widespread. The discovery and development of new drugs need to be done to overcome the case. Aims: To develop lung anticancer candidates with benzylidene hydrazine benzamides derivatives that can inhibit the growth of human lung cancer cell line A459. Methods: The in silico approach method, along with the QSAR technique, plays an important role in the process of discovery and development of new drugs. In this study, we focused on developing benzylidene hydrazine benzamides derivatives that are much more potent by making the best QSAR equation of 11 benzylidene hydrazine benzamides that have been tested in vitro for its anticancer activity against human lung cancer cell line A459. Results: The best QSAR equation was obtained from benzylidene hydrazine benzamides derivatives as anticancer activity against human lung cancer cell line A459, with PIC50 = 0.738 (± 0.217) Log S - 0.031 (± 0.007) rerank + 0.017 (± 0.016) MR -1.359 ± (1.381) (n = 11; Sig = 0.003; r = 0.921; R2 = 0.849; F= 13.096; Q2 = 0.61). Conclusions: The best QSAR equation can be a tool to obtain a new chemical structure model with more potential and reduce trials and errors.
{"title":"QSAR study of benzylidene hydrazine benzamides derivatives with in vitro anticancer activity against human lung cancer cell line A459","authors":"Galih Satrio Putra, Melanny Ika Sulistyowaty, Tegar Achsendo Yuniarta, Yahmin Yahmin, Sumari Sumari, Charinrat Saechan, Takayasu Yamauchi","doi":"10.56499/jppres23.1718_11.6.1123","DOIUrl":"https://doi.org/10.56499/jppres23.1718_11.6.1123","url":null,"abstract":"Context: In the last decade, resistance to epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs) in lung cancer cases has been widespread. The discovery and development of new drugs need to be done to overcome the case. Aims: To develop lung anticancer candidates with benzylidene hydrazine benzamides derivatives that can inhibit the growth of human lung cancer cell line A459. Methods: The in silico approach method, along with the QSAR technique, plays an important role in the process of discovery and development of new drugs. In this study, we focused on developing benzylidene hydrazine benzamides derivatives that are much more potent by making the best QSAR equation of 11 benzylidene hydrazine benzamides that have been tested in vitro for its anticancer activity against human lung cancer cell line A459. Results: The best QSAR equation was obtained from benzylidene hydrazine benzamides derivatives as anticancer activity against human lung cancer cell line A459, with PIC50 = 0.738 (± 0.217) Log S - 0.031 (± 0.007) rerank + 0.017 (± 0.016) MR -1.359 ± (1.381) (n = 11; Sig = 0.003; r = 0.921; R2 = 0.849; F= 13.096; Q2 = 0.61). Conclusions: The best QSAR equation can be a tool to obtain a new chemical structure model with more potential and reduce trials and errors.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135270798","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-11-01DOI: 10.56499/jppres23.1646_11.6.953
Enoel Hernández-Barreto, Vivian Ruz-Sanjuan, Venancio Ribalta-Ribalta, Luis A. Torres-Gómez
Context: The present experimental conditions of the molybdenum blue spectrophotometric method, used for antioxidant activity estimation, promote the degradation of flavonoids with potential interferences in the above determination. Aims: To evaluate the effects of physicochemical factors on the formation of the complex for optimizing the total antioxidant activity method to better estimate the antioxidant activity of natural products. Methods: A 34-1 fractional experimental design was applied. Independent variables were temperature, color development time, type of acid and acidity, and the dependent variable was the absorbance of the complex. The concentration of ammonium molybdate tetrahydrate and sodium hydrogen phosphate remained constant throughout the study. The effects of the reducing agent and its concentration were studied independently. The effect of acidity in a wide range of values, the color development time considering temperature, the influence of co-solvents, and the antioxidant activity of various natural metabolites were also evaluated. Results: Acid concentration and temperature greatly influenced the complex formation, making the type of acid and incubation time less significant. Ascorbic acid showed a shorter color development time than reference metabolites. Ethanol negatively influenced the amount of complex formed. The proposed conditions for developing this method were: type of acid, HCl or H2SO4; acid concentration 0.01 N; incubation temperature 65°C; and incubation time 40 min. Under these experimental conditions, the ranking order of antioxidant activity was pyrogallol>quercetin>ascorbic acid>gallic acid>rutin. Conclusions: The new experimental conditions for the molybdenum complex assay give a more reliable determination of the antioxidant activity of natural products.
{"title":"Optimization of the molybdenum blue method for estimating the antioxidant activity of natural products","authors":"Enoel Hernández-Barreto, Vivian Ruz-Sanjuan, Venancio Ribalta-Ribalta, Luis A. Torres-Gómez","doi":"10.56499/jppres23.1646_11.6.953","DOIUrl":"https://doi.org/10.56499/jppres23.1646_11.6.953","url":null,"abstract":"Context: The present experimental conditions of the molybdenum blue spectrophotometric method, used for antioxidant activity estimation, promote the degradation of flavonoids with potential interferences in the above determination. Aims: To evaluate the effects of physicochemical factors on the formation of the complex for optimizing the total antioxidant activity method to better estimate the antioxidant activity of natural products. Methods: A 34-1 fractional experimental design was applied. Independent variables were temperature, color development time, type of acid and acidity, and the dependent variable was the absorbance of the complex. The concentration of ammonium molybdate tetrahydrate and sodium hydrogen phosphate remained constant throughout the study. The effects of the reducing agent and its concentration were studied independently. The effect of acidity in a wide range of values, the color development time considering temperature, the influence of co-solvents, and the antioxidant activity of various natural metabolites were also evaluated. Results: Acid concentration and temperature greatly influenced the complex formation, making the type of acid and incubation time less significant. Ascorbic acid showed a shorter color development time than reference metabolites. Ethanol negatively influenced the amount of complex formed. The proposed conditions for developing this method were: type of acid, HCl or H2SO4; acid concentration 0.01 N; incubation temperature 65°C; and incubation time 40 min. Under these experimental conditions, the ranking order of antioxidant activity was pyrogallol>quercetin>ascorbic acid>gallic acid>rutin. Conclusions: The new experimental conditions for the molybdenum complex assay give a more reliable determination of the antioxidant activity of natural products.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136371315","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Context: Lactic acid bacteria (LAB), which are found in many fermented foods, are known to produce antimicrobial compounds that play a vital role in food bio-preservation. Aims: To screen, identify, characterize, and determine the secondary metabolites of LAB isolated from Thai fermented foods that are beneficial against Escherichia coli and Staphylococcus aureus. Methods: The antimicrobial activity of cell free supernatant (CFS) was evaluated by agar well diffusion assay, and determining the minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC). Bacterial strains were identified by matrix-assisted laser desorption ionization-time of flight mass spectrometry (MALDI-TOF MS), and chemical compound was conducted by gas chromatography and mass spectrometry (GC-MS). Additionally, microbial dynamic and bile salt tolerance were assessed. Results: Seven of the 90 lactic acid isolates from Thai fermented foods, showed antibacterial activity against E. coli and S. aureus in the 12.00–16.00 mm inhibitory zone. It was identified that the bacteria were Lactobacillus pentosus, Lactobacillus farciminis, Lactobacillus brevis, and Lactobacillus plantarum. The best antibacterial activity was represented by LBST1861 strain, which also provided bile salt resistance at 0.3% for 24 hours and had MIC and MBC values of 12.5 mg/mL and 50.0 mg/mL against S. aureus and E. coli, respectively. Furthermore, the GC-MS discovered a total of 16 chemical compounds that may be used to limit microbial growth and has a potential to be employed as a bio-preservative. Conclusions: The most potent strain of LBST1861 strain against S. aureus and E. coli as L. plantarum, isolated from fermented foods in Thailand, generated significant bioactive chemicals that can be applied to promote food products.
{"title":"Bioactive compound and chemical characterization of lactic acid bacteria from fermented food as bio-preservative agents to control food-borne pathogens","authors":"Surachai Techaoei, Khemjira Jarmkom, Thisakorn Dumrongphuttidecha, Warachate Khobjai","doi":"10.56499/jppres23.1713_11.6.1044","DOIUrl":"https://doi.org/10.56499/jppres23.1713_11.6.1044","url":null,"abstract":"Context: Lactic acid bacteria (LAB), which are found in many fermented foods, are known to produce antimicrobial compounds that play a vital role in food bio-preservation. Aims: To screen, identify, characterize, and determine the secondary metabolites of LAB isolated from Thai fermented foods that are beneficial against Escherichia coli and Staphylococcus aureus. Methods: The antimicrobial activity of cell free supernatant (CFS) was evaluated by agar well diffusion assay, and determining the minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC). Bacterial strains were identified by matrix-assisted laser desorption ionization-time of flight mass spectrometry (MALDI-TOF MS), and chemical compound was conducted by gas chromatography and mass spectrometry (GC-MS). Additionally, microbial dynamic and bile salt tolerance were assessed. Results: Seven of the 90 lactic acid isolates from Thai fermented foods, showed antibacterial activity against E. coli and S. aureus in the 12.00–16.00 mm inhibitory zone. It was identified that the bacteria were Lactobacillus pentosus, Lactobacillus farciminis, Lactobacillus brevis, and Lactobacillus plantarum. The best antibacterial activity was represented by LBST1861 strain, which also provided bile salt resistance at 0.3% for 24 hours and had MIC and MBC values of 12.5 mg/mL and 50.0 mg/mL against S. aureus and E. coli, respectively. Furthermore, the GC-MS discovered a total of 16 chemical compounds that may be used to limit microbial growth and has a potential to be employed as a bio-preservative. Conclusions: The most potent strain of LBST1861 strain against S. aureus and E. coli as L. plantarum, isolated from fermented foods in Thailand, generated significant bioactive chemicals that can be applied to promote food products.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135011778","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Context: Co-crystal formation, a method for enhancing the physicochemical properties of active pharmaceutical ingredients (APIs), has gained traction in pharmaceutical research. However, the current landscape lacks comprehensive and dependable co-crystal screening methods. Aims: To implement and assess a comprehensive methodology for co-crystal screening. This methodology combines hot-stage polarized microscopy (HSPM) and attenuated total reflection Fourier-transform infrared (ATR-FTIR) spectroscopy, along with principal component analysis (PCA) and cluster analysis (CA). Methods: Three binary compounds containing ramipril, an API that had not previously been co-crystallized, and three pharmaceutical coformers were investigated. The Kofler mixed fusion method was initially employed for initial co-crystal system identification. Subsequently, potential co-crystals were produced in a solid state via a procedure involving the gradual evaporation of the solvent. PCA and CA were applied to ATR-FTIR spectral data to identify patterns indicative of co-crystal formation. Results: Our analysis revealed characteristic ATR-FTIR bands indicative of the formation of hydrogen bonds between ramipril and its coformers, signifying the successful formation of co-crystals. Differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) measurements confirmed these findings. Experiments revealed two potential co-crystals, ramipril-vanillin, and ramipril-anthranilic acid. The study discusses the intricate HSPM images, spectra, thermogram of DSC, and X-ray diffraction properties of these systems in depth. Conclusions: Our findings validate the proposed methodology as a prospective tool for co-crystal screening, as ramipril co-crystals were successfully identified and characterized. This integrated method simplifies co-crystal screening and has the potential to substantially advance pharmaceutical research.
{"title":"Utilizing hot-stage polarized microscopy and ATR-FTIR for ramipril co-crystal screening, supported by principal component analysis and cluster analysis","authors":"Indra Indra, Saleh Wikarsa, Yuda Prasetya Nugraha, Veinardi Suendo, Hidehiro Uekusa, Sundani Nurono Soewandhi","doi":"10.56499/jppres23.1723_11.6.1137","DOIUrl":"https://doi.org/10.56499/jppres23.1723_11.6.1137","url":null,"abstract":"Context: Co-crystal formation, a method for enhancing the physicochemical properties of active pharmaceutical ingredients (APIs), has gained traction in pharmaceutical research. However, the current landscape lacks comprehensive and dependable co-crystal screening methods. Aims: To implement and assess a comprehensive methodology for co-crystal screening. This methodology combines hot-stage polarized microscopy (HSPM) and attenuated total reflection Fourier-transform infrared (ATR-FTIR) spectroscopy, along with principal component analysis (PCA) and cluster analysis (CA). Methods: Three binary compounds containing ramipril, an API that had not previously been co-crystallized, and three pharmaceutical coformers were investigated. The Kofler mixed fusion method was initially employed for initial co-crystal system identification. Subsequently, potential co-crystals were produced in a solid state via a procedure involving the gradual evaporation of the solvent. PCA and CA were applied to ATR-FTIR spectral data to identify patterns indicative of co-crystal formation. Results: Our analysis revealed characteristic ATR-FTIR bands indicative of the formation of hydrogen bonds between ramipril and its coformers, signifying the successful formation of co-crystals. Differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) measurements confirmed these findings. Experiments revealed two potential co-crystals, ramipril-vanillin, and ramipril-anthranilic acid. The study discusses the intricate HSPM images, spectra, thermogram of DSC, and X-ray diffraction properties of these systems in depth. Conclusions: Our findings validate the proposed methodology as a prospective tool for co-crystal screening, as ramipril co-crystals were successfully identified and characterized. This integrated method simplifies co-crystal screening and has the potential to substantially advance pharmaceutical research.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135412019","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-11-01DOI: 10.56499/jppres23.1579_11.6.1072
Wiwied Ekasari, Retno Widyowati, Tutik S. Wahyuni, Suciati Suciati, Rice D. Oktarina, Chrismawan Ardianto, Elsa S. Prameswari, Windri A. A. Suri, Alfaniady I. Kurnia, Rahma K. Wirabuana, Vita M. A. Angembani, Ram K. Sahu
Context: Senna spectabilis (DC.) H.S.Irwin & Barneby which belongs to Fabaceae family is widely used traditionally in the treatment of various diseases and disorders such as constipation, insomnia, anxiety, epilepsy, malaria and skin diseases. Aims: To investigate the central nervous system (CNS) depressant effect of 70% ethanol extract of S. spectabilis leaves (70SSEE) using different neuropharmacological models in mice. Methods: The CNS depressant effect of 70SSEE was investigated by the classical models of depression as elevated plus maze (EPM), hole cross (HC), and thiopental sodium (TS)-induced sleeping time tests in mice. The EPM test was used to assess the anxiolytic activity of 70SSEE at doses of 10, 50, and 100 mg/kg, while HC and TS-induced sleeping time tests at doses of 100, 250, and 500 mg/kg were used to assess the locomotor and sedative activity in mice. Results: In EPM test, 70SSEE at doses of 50 and 100 mg/kg significantly (p<0.05) increased the number of open arm entries and time spent in open arm by mice compared to controls. In HC test, 70SSEE significantly inhibited the movement of animals across the hole in a dose-dependent manner. In addition, the administration of 70SSEE to mice significantly (p<0.05) decreased sleep latency time and increased sleep duration of TS-induced mice. Conclusions: 70SSEE has CNS depressant effects which is a rational explanation for its use in traditional medicine. From these findings, it is hoped that this plant could be used in the treatment of various neurological disorders, including anxiety and insomnia.
{"title":"Central nervous system depressant effect of ethanol extract of Senna spectabilis (DC.) H.S.Irwin & Barneby in mice","authors":"Wiwied Ekasari, Retno Widyowati, Tutik S. Wahyuni, Suciati Suciati, Rice D. Oktarina, Chrismawan Ardianto, Elsa S. Prameswari, Windri A. A. Suri, Alfaniady I. Kurnia, Rahma K. Wirabuana, Vita M. A. Angembani, Ram K. Sahu","doi":"10.56499/jppres23.1579_11.6.1072","DOIUrl":"https://doi.org/10.56499/jppres23.1579_11.6.1072","url":null,"abstract":"Context: Senna spectabilis (DC.) H.S.Irwin & Barneby which belongs to Fabaceae family is widely used traditionally in the treatment of various diseases and disorders such as constipation, insomnia, anxiety, epilepsy, malaria and skin diseases. Aims: To investigate the central nervous system (CNS) depressant effect of 70% ethanol extract of S. spectabilis leaves (70SSEE) using different neuropharmacological models in mice. Methods: The CNS depressant effect of 70SSEE was investigated by the classical models of depression as elevated plus maze (EPM), hole cross (HC), and thiopental sodium (TS)-induced sleeping time tests in mice. The EPM test was used to assess the anxiolytic activity of 70SSEE at doses of 10, 50, and 100 mg/kg, while HC and TS-induced sleeping time tests at doses of 100, 250, and 500 mg/kg were used to assess the locomotor and sedative activity in mice. Results: In EPM test, 70SSEE at doses of 50 and 100 mg/kg significantly (p<0.05) increased the number of open arm entries and time spent in open arm by mice compared to controls. In HC test, 70SSEE significantly inhibited the movement of animals across the hole in a dose-dependent manner. In addition, the administration of 70SSEE to mice significantly (p<0.05) decreased sleep latency time and increased sleep duration of TS-induced mice. Conclusions: 70SSEE has CNS depressant effects which is a rational explanation for its use in traditional medicine. From these findings, it is hoped that this plant could be used in the treatment of various neurological disorders, including anxiety and insomnia.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135012445","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-11-01DOI: 10.56499/jppres23.1727_11.6.1056
Adelina Simamora, Kris H. Timotius, Heri Setiawan, Masteria Y. Putra, Abdul Mun’im
Context: Curcuma xanthorrhiza, a native to Indonesia, has been recognized as a potential medicinal plant. Xanthorrhizol (XTZ), curcumin (Cur), bisdemethoxycurcumin (BDMC), and demethoxycurcumin (DMC) are the main major metabolites with different bioactivities. Thus, the selective extraction of these markers is required. Aims: To characterize and use natural deep eutectic solvents (NADES) for the extraction of XTZ and curcuminoids (CURS) from C. xanthorrhiza. Methods: Four NADES, comprising of glucose:lactic acid (Glu:LA, 1:3), choline chloride: malic acid (ChCl:MA, 1:1), choline chloride: glycerol (ChCl:Gly, 1:1), and choline chloride: sucrose (ChCl:Suc, 3:1) were synthesized and subjected to FTIR. The physicochemical properties of NADES were characterized, including polarity, viscosity, and density. Their antioxidant profiles were evaluated. The toxicity of NADES was assessed towards Escherichia coli by real-time growth monitoring. Tested NADES were employed to extract marker compounds from the rhizome of C. xanthorrhiza. A validated high-performance liquid chromatography (HPLC) method was applied to simultaneously quantify XTZ and CURS in NADES extracts. Results: FTIR spectra confirmed the formation of hydrogen bonds between components. Using the DPPH and FRAP methods, all NADES and NADES extracts displayed antioxidative activity, suggesting the contribution of NADES to the activity. Of the tested NADES, Glu:LA (1:3) obtained the highest content of XTZ over Cur, BDMC, and DMC, comparable to that of ethanol maceration. All tested NADES were harmless to E. coli, except for ChCl:MA (1:1). However, NADES extracts of Glu:LA (1:3) and ChCl:MA (1:1) suppressed the growth of the bacterium. Scanning electron micrographs demonstrated the destruction of the surface structure of the rhizome powder by NADES-ultrasonication. Conclusions: The study recommended the use of Glu:LA (1:3) to selectively extract XTZ to promote environmentally friendly and sustainable extraction.
{"title":"Natural deep eutectic solvent extraction of xanthorrhizol and curcuminoids from Curcuma xanthorrhiza Roxb and simultaneous determination by high-performance liquid chromatography","authors":"Adelina Simamora, Kris H. Timotius, Heri Setiawan, Masteria Y. Putra, Abdul Mun’im","doi":"10.56499/jppres23.1727_11.6.1056","DOIUrl":"https://doi.org/10.56499/jppres23.1727_11.6.1056","url":null,"abstract":"Context: Curcuma xanthorrhiza, a native to Indonesia, has been recognized as a potential medicinal plant. Xanthorrhizol (XTZ), curcumin (Cur), bisdemethoxycurcumin (BDMC), and demethoxycurcumin (DMC) are the main major metabolites with different bioactivities. Thus, the selective extraction of these markers is required. Aims: To characterize and use natural deep eutectic solvents (NADES) for the extraction of XTZ and curcuminoids (CURS) from C. xanthorrhiza. Methods: Four NADES, comprising of glucose:lactic acid (Glu:LA, 1:3), choline chloride: malic acid (ChCl:MA, 1:1), choline chloride: glycerol (ChCl:Gly, 1:1), and choline chloride: sucrose (ChCl:Suc, 3:1) were synthesized and subjected to FTIR. The physicochemical properties of NADES were characterized, including polarity, viscosity, and density. Their antioxidant profiles were evaluated. The toxicity of NADES was assessed towards Escherichia coli by real-time growth monitoring. Tested NADES were employed to extract marker compounds from the rhizome of C. xanthorrhiza. A validated high-performance liquid chromatography (HPLC) method was applied to simultaneously quantify XTZ and CURS in NADES extracts. Results: FTIR spectra confirmed the formation of hydrogen bonds between components. Using the DPPH and FRAP methods, all NADES and NADES extracts displayed antioxidative activity, suggesting the contribution of NADES to the activity. Of the tested NADES, Glu:LA (1:3) obtained the highest content of XTZ over Cur, BDMC, and DMC, comparable to that of ethanol maceration. All tested NADES were harmless to E. coli, except for ChCl:MA (1:1). However, NADES extracts of Glu:LA (1:3) and ChCl:MA (1:1) suppressed the growth of the bacterium. Scanning electron micrographs demonstrated the destruction of the surface structure of the rhizome powder by NADES-ultrasonication. Conclusions: The study recommended the use of Glu:LA (1:3) to selectively extract XTZ to promote environmentally friendly and sustainable extraction.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135012446","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-11-01DOI: 10.56499/jppres23.1697_11.6.975
Yenny Y. Lozano, Sara E. Giraldo, Angela C. Zapata, Jesús E. Escobar, Ruth M. Sánchez
Context: Cutaneous leishmaniasis is a disease of public health importance; treatment is based on the use of pentavalent antimonials with high toxicity and low efficacy; therefore, it´s necessary to search for therapeutic alternatives derived from natural products, based on the study of medicinal plants as a source of molecules with highly effective leishmanicidal potential. Aims: To carry out a systematic review between 2018 and 2022 on medicinal plants with potential leishmanicidal activity on parasite strains from the New World causing cutaneous leishmaniasis. Methods: The review study was conducted in four phases following the PRISMA methodology. First, research questions and objectives were formulated to establish the topic areas and construct the search algorithm. Second, a search was performed across different databases, including ScienceDirect, Scopus, PubMed, Web of Science, EBSCO, Taylor and Francis, and Scielo. Third, articles were chosen based on specific inclusion and exclusion criteria. Finally, the relevant information for the review was systematically organized. Results: The search yielded 163 articles, and 12 of them were selected as the basis for the construction of the review. Ethanolic and aqueous extracts stand out, as well as biocompounds such as terpenes and flavonoids. Antioxidant activity on reactive oxygen species was the most frequently cited. Conclusions: Promising terpene and flavonoid molecules with high antileishmanial activity (IC50 <2 μM or <10 μg/mL and SI >1) were identified in this study; these findings provide a scientific basis for the traditional use that communities have given to plants as a therapeutic source to treat cutaneous leishmaniasis in the New World.
背景:皮肤利什曼病是一种具有公共卫生重要性的疾病;治疗的基础是使用高毒性、低疗效的五价锑;因此，有必要在研究药用植物作为具有高效利什曼尼分子来源的基础上，从天然产物中寻找治疗替代品。目的:对2018年至2022年间对引起皮肤利什曼病的新世界寄生虫株具有潜在杀利什曼活性的药用植物进行系统评价。方法:按照PRISMA方法学分为四个阶段进行回顾性研究。首先，制定研究问题和目标，建立主题领域，构建搜索算法。其次，在不同的数据库中进行搜索，包括ScienceDirect、Scopus、PubMed、Web of Science、EBSCO、Taylor and Francis和Scielo。第三，根据具体的纳入和排除标准选择文章。最后，对评审的相关资料进行了系统整理。结果:检索到163篇文献，选取其中12篇作为构建综述的依据。乙醇和水提取物以及萜烯和类黄酮等生物化合物脱颖而出。对活性氧的抗氧化活性是最常被引用的。结论:本研究鉴定出具有较高抗利什曼原虫活性的萜类和类黄酮分子(IC50为2 μM或10 μg/mL, SI为1);这些发现为新世界的社区将植物作为治疗皮肤利什曼病的治疗来源的传统用途提供了科学依据。
{"title":"Medicinal plants with antileishmanial activity on parasites responsible for new-world cutaneous leishmaniasis. A systematic review 2018-2022","authors":"Yenny Y. Lozano, Sara E. Giraldo, Angela C. Zapata, Jesús E. Escobar, Ruth M. Sánchez","doi":"10.56499/jppres23.1697_11.6.975","DOIUrl":"https://doi.org/10.56499/jppres23.1697_11.6.975","url":null,"abstract":"Context: Cutaneous leishmaniasis is a disease of public health importance; treatment is based on the use of pentavalent antimonials with high toxicity and low efficacy; therefore, it´s necessary to search for therapeutic alternatives derived from natural products, based on the study of medicinal plants as a source of molecules with highly effective leishmanicidal potential. Aims: To carry out a systematic review between 2018 and 2022 on medicinal plants with potential leishmanicidal activity on parasite strains from the New World causing cutaneous leishmaniasis. Methods: The review study was conducted in four phases following the PRISMA methodology. First, research questions and objectives were formulated to establish the topic areas and construct the search algorithm. Second, a search was performed across different databases, including ScienceDirect, Scopus, PubMed, Web of Science, EBSCO, Taylor and Francis, and Scielo. Third, articles were chosen based on specific inclusion and exclusion criteria. Finally, the relevant information for the review was systematically organized. Results: The search yielded 163 articles, and 12 of them were selected as the basis for the construction of the review. Ethanolic and aqueous extracts stand out, as well as biocompounds such as terpenes and flavonoids. Antioxidant activity on reactive oxygen species was the most frequently cited. Conclusions: Promising terpene and flavonoid molecules with high antileishmanial activity (IC50 <2 μM or <10 μg/mL and SI >1) were identified in this study; these findings provide a scientific basis for the traditional use that communities have given to plants as a therapeutic source to treat cutaneous leishmaniasis in the New World.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136372212","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-11-01DOI: 10.56499/jppres23.1695_11.6.926
Mochamad Bachtiar Budianto, Hamzah Sulaiman Lubis, Muhammad Luqman Fadli, Wiwit Nurwidyaningtyas
Context: Locally advanced breast cancers (LABC) are the most common women malignant tumors. Appropriate vasculature is required for tumor growth support, formed by involving protein signaling, including matrix metalloprotein 9 (MMP9) and C-X-C chemokine receptor type 4 (CXCR4). Neoadjuvant chemotherapy (NAC) administration to inoperable LABC commonly exhibits a positive response, although recurrences may be encountered in a few cases. Aims: To evaluate the MMP9 and CXCR4 expression shifting after the NAC procedure to establish evidence of the anti-angiogenic effect of NAC, which encourages knowledge of tumor size reduction pathways in LABC. Methods: Observational designs were conducted in this study. Tissue specimens before and after NAC were collected from 45 LABC-enrolled subjects. The targeted protein expression was analyzed by immunohistochemistry, and stained sections were classified according to the percentage of nuclear-stained tumor cells. Clinicopathological features of LABC were recorded. Tumor size was measured by Vernier caliper before and after NAC. Results: The results showed the nuclear expression of MMP9 and CXCR4 protein were observed in all tissue specimens. The expression of MMP9 and CXCR4 tended to decrease after the NAC but was not statistically significant for MMP9. There was a significant correlation between expression levels of CXCR4 and tumor size reduction (p<0.001) but not for MMP9. Conclusions: The results of this study demonstrate the anti-angiogenic effect of NAC by inhibiting MMP9 and CXCR4, which may be integrated with tumor size reduction in LABC. Further studies are required to highlight the possibility of recurrence following inhibition of MMP9 and CXCR4 by NAC.
{"title":"Check update pattern of tumorigenic vasculature signature based on MMP9 and CXCR4 expression in locally advanced breast cancer","authors":"Mochamad Bachtiar Budianto, Hamzah Sulaiman Lubis, Muhammad Luqman Fadli, Wiwit Nurwidyaningtyas","doi":"10.56499/jppres23.1695_11.6.926","DOIUrl":"https://doi.org/10.56499/jppres23.1695_11.6.926","url":null,"abstract":"Context: Locally advanced breast cancers (LABC) are the most common women malignant tumors. Appropriate vasculature is required for tumor growth support, formed by involving protein signaling, including matrix metalloprotein 9 (MMP9) and C-X-C chemokine receptor type 4 (CXCR4). Neoadjuvant chemotherapy (NAC) administration to inoperable LABC commonly exhibits a positive response, although recurrences may be encountered in a few cases. Aims: To evaluate the MMP9 and CXCR4 expression shifting after the NAC procedure to establish evidence of the anti-angiogenic effect of NAC, which encourages knowledge of tumor size reduction pathways in LABC. Methods: Observational designs were conducted in this study. Tissue specimens before and after NAC were collected from 45 LABC-enrolled subjects. The targeted protein expression was analyzed by immunohistochemistry, and stained sections were classified according to the percentage of nuclear-stained tumor cells. Clinicopathological features of LABC were recorded. Tumor size was measured by Vernier caliper before and after NAC. Results: The results showed the nuclear expression of MMP9 and CXCR4 protein were observed in all tissue specimens. The expression of MMP9 and CXCR4 tended to decrease after the NAC but was not statistically significant for MMP9. There was a significant correlation between expression levels of CXCR4 and tumor size reduction (p<0.001) but not for MMP9. Conclusions: The results of this study demonstrate the anti-angiogenic effect of NAC by inhibiting MMP9 and CXCR4, which may be integrated with tumor size reduction in LABC. Further studies are required to highlight the possibility of recurrence following inhibition of MMP9 and CXCR4 by NAC.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"134957524","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-11-01DOI: 10.56499/jppres23.1684_11.6.1017
Karthick Vasudevan, Raghavendra B, Mithun A, Dhanushkumar T, Fazil Ahmad, Manoj Goyal, Monika Bansal, Tasneem Mohammed, Riyaz Ahmed Khan, Gayathri Pandurangam, George Priya Doss, Balu Kamaraj, Gurudeeban Selvaraj
Context: Gastric cancer is one of the most prevalent types of cancer in developing countries and ranks fourth in terms of death causes. Helicobacter pylori infection is a significant contributor to the emergence of gastric cancer. Lack of early diagnosis of gastric cancer is a leading cause of death. Aims: To identify the key genes and pathways involved in gastric cancer. Methods: This study performed a comprehensive analysis of RNA-Seq data from human gastric cancer and adjacent normal tissues. Raw data passed quality checks with FastQC and were aligned to GRCh38 using HISAT2. Subread's FeatureCounts handled transcript assembly and quantification. DESeq2 pinpointed significant genes, while ClueGO explored gene ontology and KEGG pathways. Protein-protein interaction networks, constructed with StringApp, aided in identifying hub genes through CytoHubba. This holistic approach yields insights into the molecular mechanisms underpinning gastric cancer. Results: This study detected 711 differentially expressed genes (DEGs) between normal and gastric samples. A total of 594 genes were identified as upregulated and 117 as downregulated. Major DEGs are enriched in signal transduction, stimulus-response regulation, transmembrane signaling receptor activity, and signal transduction pathways involving cytokines. In addition, 20 hub genes from the PPI network were identified based on MCC rank analysis from the CytoHubba plugin, contributing to the progression of gastric cancer. Conclusions: The top six hub genes, CD4, CTLA4, CD28, CD80, CD27, and SELL, are expected to regulate several pathways and may serve as potential biomarkers for the early detection and treatment of gastric cancer patients.
{"title":"Integrated RNA-sequencing and network analysis approach to identify the Hub genes and vital pathways associated with gastric cancer","authors":"Karthick Vasudevan, Raghavendra B, Mithun A, Dhanushkumar T, Fazil Ahmad, Manoj Goyal, Monika Bansal, Tasneem Mohammed, Riyaz Ahmed Khan, Gayathri Pandurangam, George Priya Doss, Balu Kamaraj, Gurudeeban Selvaraj","doi":"10.56499/jppres23.1684_11.6.1017","DOIUrl":"https://doi.org/10.56499/jppres23.1684_11.6.1017","url":null,"abstract":"Context: Gastric cancer is one of the most prevalent types of cancer in developing countries and ranks fourth in terms of death causes. Helicobacter pylori infection is a significant contributor to the emergence of gastric cancer. Lack of early diagnosis of gastric cancer is a leading cause of death. Aims: To identify the key genes and pathways involved in gastric cancer. Methods: This study performed a comprehensive analysis of RNA-Seq data from human gastric cancer and adjacent normal tissues. Raw data passed quality checks with FastQC and were aligned to GRCh38 using HISAT2. Subread's FeatureCounts handled transcript assembly and quantification. DESeq2 pinpointed significant genes, while ClueGO explored gene ontology and KEGG pathways. Protein-protein interaction networks, constructed with StringApp, aided in identifying hub genes through CytoHubba. This holistic approach yields insights into the molecular mechanisms underpinning gastric cancer. Results: This study detected 711 differentially expressed genes (DEGs) between normal and gastric samples. A total of 594 genes were identified as upregulated and 117 as downregulated. Major DEGs are enriched in signal transduction, stimulus-response regulation, transmembrane signaling receptor activity, and signal transduction pathways involving cytokines. In addition, 20 hub genes from the PPI network were identified based on MCC rank analysis from the CytoHubba plugin, contributing to the progression of gastric cancer. Conclusions: The top six hub genes, CD4, CTLA4, CD28, CD80, CD27, and SELL, are expected to regulate several pathways and may serve as potential biomarkers for the early detection and treatment of gastric cancer patients.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135012148","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-11-01DOI: 10.56499/jppres23.1671_11.6.1079
Patricia Azócar, Marisela Valdés-González, Bárbara B. Garrido-Suárez, Maria S. Fernández-Alfonso, Gabino Garrido
Context: Self-medication is a self-care practice. It is a frequent and widespread habit in all societies and does not distinguish between sex and age. Therefore, students are not exempt from using this practice. Aims: To carry out a systematic review of scientific articles published between 2010 and 2020 on self-medication in university students of careers related to medical and biological sciences with PRISMA guidelines. Methods: A standardized search was performed in four databases with the following terms: Automedicación (in Spanish), Self-medication, Automedication, University Student, and Students. For the selection of studies, the Rayyan® tool was used. The most relevant information on self-medication of university students was collected. Results: Fourteen articles were included and evaluated as high, medium, and low quality with the AXIS tool. The results of the study reflected a high self-medication in university students of careers related to medical and biological sciences, with a higher prevalence of self-medication in women than in men. The more knowledge these students have, the greater their self-medication and, thus, they always maintain this practice, being the most indicated causes for it the problems in the respiratory tract, headaches, and gastrointestinal problems. The main reasons for these students to practice self-medication are the knowledge they have acquired in their curricula, due to past experiences with the same symptoms and minor illnesses. Pharmacies, through friends, relatives or neighbors and home medicine cabinets are the most common places for the acquisition of medications by these students, indicating that analgesics/anti-inflammatories, antibiotics, and antipyretics are the most used medications among them. Conclusions: These students practice self-medication because they consider they have sufficient knowledge about diseases and their treatments, which gives them more confidence in making the decision to self-medicate. Subsequently, self-knowledge is a decisive reason for self-medication. Moreover, self-medication patterns regarding the use of drugs from various therapeutic categories vary among medical and biological sciences university students from different countries.
{"title":"Systematic review of self-medication in students of medical and biological sciences careers","authors":"Patricia Azócar, Marisela Valdés-González, Bárbara B. Garrido-Suárez, Maria S. Fernández-Alfonso, Gabino Garrido","doi":"10.56499/jppres23.1671_11.6.1079","DOIUrl":"https://doi.org/10.56499/jppres23.1671_11.6.1079","url":null,"abstract":"Context: Self-medication is a self-care practice. It is a frequent and widespread habit in all societies and does not distinguish between sex and age. Therefore, students are not exempt from using this practice. Aims: To carry out a systematic review of scientific articles published between 2010 and 2020 on self-medication in university students of careers related to medical and biological sciences with PRISMA guidelines. Methods: A standardized search was performed in four databases with the following terms: Automedicación (in Spanish), Self-medication, Automedication, University Student, and Students. For the selection of studies, the Rayyan® tool was used. The most relevant information on self-medication of university students was collected. Results: Fourteen articles were included and evaluated as high, medium, and low quality with the AXIS tool. The results of the study reflected a high self-medication in university students of careers related to medical and biological sciences, with a higher prevalence of self-medication in women than in men. The more knowledge these students have, the greater their self-medication and, thus, they always maintain this practice, being the most indicated causes for it the problems in the respiratory tract, headaches, and gastrointestinal problems. The main reasons for these students to practice self-medication are the knowledge they have acquired in their curricula, due to past experiences with the same symptoms and minor illnesses. Pharmacies, through friends, relatives or neighbors and home medicine cabinets are the most common places for the acquisition of medications by these students, indicating that analgesics/anti-inflammatories, antibiotics, and antipyretics are the most used medications among them. Conclusions: These students practice self-medication because they consider they have sufficient knowledge about diseases and their treatments, which gives them more confidence in making the decision to self-medicate. Subsequently, self-knowledge is a decisive reason for self-medication. Moreover, self-medication patterns regarding the use of drugs from various therapeutic categories vary among medical and biological sciences university students from different countries.","PeriodicalId":43917,"journal":{"name":"Journal of Pharmacy & Pharmacognosy Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135012465","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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