Pub Date : 2022-03-04DOI: 10.1080/22311866.2022.2032828
H. Abdallah, R. Ahmed, A. Elshamy
Abstract Salvia officinalis, a native plant to the Mediterranean and Middle East, is familiar cookery and traditional herb. Herein, in vivo anticonvulsant and analgesic effects of sclareol isolated from S. officinalis were reported. Sclareol (50 mg/kg) decreased tonic convulsions from 100% (positive control) to 33.33% with 16.66% mortality using MES protocol. Also, 100 mg/kg decreased convulsions to 16.66%, with no mortality. In MEST test, sclareol protected against gradually increased electric shock in a dose-dependent manner comparable to phenytoin. Pentylenetetrazole injection induced generalized clonic seizures and 100% mortality. Sclareol pretreatment exhibited a prolonged latency to 1-3 stages of clonic convulsions with significant incidence reduction of lethality. Sclareol at both doses was not neurotoxic in rotarod test. In the hot-plate test, sclareol showed analgesic effect at 60 and 90 min after drug administration. Finally, in addition to its central anti-nociceptive effect, sclareol also protected against chemically- and electrically-induced seizures with no central nervous system side effects. Our findings suggest that sclareol could be a leading compound for a potential new antiepileptic and analgesic drug. Graphical abstract
{"title":"In-vivo Anticonvulsant and Analgesic Activities of Sclareol Isolated from Salvia officinalis L","authors":"H. Abdallah, R. Ahmed, A. Elshamy","doi":"10.1080/22311866.2022.2032828","DOIUrl":"https://doi.org/10.1080/22311866.2022.2032828","url":null,"abstract":"Abstract Salvia officinalis, a native plant to the Mediterranean and Middle East, is familiar cookery and traditional herb. Herein, in vivo anticonvulsant and analgesic effects of sclareol isolated from S. officinalis were reported. Sclareol (50 mg/kg) decreased tonic convulsions from 100% (positive control) to 33.33% with 16.66% mortality using MES protocol. Also, 100 mg/kg decreased convulsions to 16.66%, with no mortality. In MEST test, sclareol protected against gradually increased electric shock in a dose-dependent manner comparable to phenytoin. Pentylenetetrazole injection induced generalized clonic seizures and 100% mortality. Sclareol pretreatment exhibited a prolonged latency to 1-3 stages of clonic convulsions with significant incidence reduction of lethality. Sclareol at both doses was not neurotoxic in rotarod test. In the hot-plate test, sclareol showed analgesic effect at 60 and 90 min after drug administration. Finally, in addition to its central anti-nociceptive effect, sclareol also protected against chemically- and electrically-induced seizures with no central nervous system side effects. Our findings suggest that sclareol could be a leading compound for a potential new antiepileptic and analgesic drug. Graphical abstract","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47114483","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 : 2022-01-02DOI: 10.1080/22311866.2021.2016485
M. Maqbool, Aisha Ashaq, Amara Maryam, Muhammad Khan, Muhammad Akhtar Ali, H. A. Shakir, Sameena Gul, F. Shakoori, M. Irfan, C. Ara
Abstract Centipeda minima (C. minima), is a medicinally important herb commonly called “Sneeze Weed” and widely distributed in humid areas. In China, Malaysia, and Nepal, it is used in folk medicines for the treatment of rhinitis, nasopharyngeal carcinoma, and respiratory disorders, it also exhibits antibacterial, antioxidant and antiprotozoal activity. Recently it is discovered that various bioactive molecule of C. minima has strong potential to be used in the treatment of various neoplasms. Thus, in this review, we aim to summarize and discuss various cellular targets and anticancer mechanisms of different bioactive components of C. minima. The pool of multiple studies suggested that various components of C. minima reduce cell growth, arrest cell cycle at various checkpoints and thereby induce apoptosis in different cancer cells via intrinsic and extrinsic apoptotic pathways. Moreover, these bioactive molecules also modulate different signaling pathways implicated in tumorigenesis including STAT3, NF-κB, ERK1/2, MMPs and AKT. In parallel to antiproliferative effect of C. minima, it also has antimetastatic and antineoplastic activities. A pile of literature clearly supported the anticancer activity of various components of C. minima against multiple human cancer cell lines. Thus, this review will be a milestone in the design and conduct of future research for the development of novel plant-based chemotherapeutics from C. minima.
{"title":"Unraveling the Anticancer Components of Centipeda minima and their Cellular Targets in Human Cancers","authors":"M. Maqbool, Aisha Ashaq, Amara Maryam, Muhammad Khan, Muhammad Akhtar Ali, H. A. Shakir, Sameena Gul, F. Shakoori, M. Irfan, C. Ara","doi":"10.1080/22311866.2021.2016485","DOIUrl":"https://doi.org/10.1080/22311866.2021.2016485","url":null,"abstract":"Abstract Centipeda minima (C. minima), is a medicinally important herb commonly called “Sneeze Weed” and widely distributed in humid areas. In China, Malaysia, and Nepal, it is used in folk medicines for the treatment of rhinitis, nasopharyngeal carcinoma, and respiratory disorders, it also exhibits antibacterial, antioxidant and antiprotozoal activity. Recently it is discovered that various bioactive molecule of C. minima has strong potential to be used in the treatment of various neoplasms. Thus, in this review, we aim to summarize and discuss various cellular targets and anticancer mechanisms of different bioactive components of C. minima. The pool of multiple studies suggested that various components of C. minima reduce cell growth, arrest cell cycle at various checkpoints and thereby induce apoptosis in different cancer cells via intrinsic and extrinsic apoptotic pathways. Moreover, these bioactive molecules also modulate different signaling pathways implicated in tumorigenesis including STAT3, NF-κB, ERK1/2, MMPs and AKT. In parallel to antiproliferative effect of C. minima, it also has antimetastatic and antineoplastic activities. A pile of literature clearly supported the anticancer activity of various components of C. minima against multiple human cancer cell lines. Thus, this review will be a milestone in the design and conduct of future research for the development of novel plant-based chemotherapeutics from C. minima.","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47329322","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 : 2022-01-02DOI: 10.1080/22311866.2021.2021986
A. S. Nugraha, Ikhar Ridho Dayli, Chintya Permata Zahky Sukrisno Putri, Lilla Nur Firli, A. N. Widhi Pratama, Bawon Triatmoko, L. Untari, H. Wongso, P. Keller, P. Wangchuk
Abstract There is an urgent need for novel drug leads, especially for microbial infections due to continuing emergence of drug resistance. Natural products are the backbone of modern medicine and the lichens have an important role to play in the discovery of novel drugs. Indonesia is gifted with a diverse array of lichens, which remain underexplored for medicinal applications. In this study, we have collected a lichen, Candelaria fibrosa, and conducted phytochemical and bioactivity studies. Using high performance liquid chromatography, mass spectrometry, and nuclear magnetic resonance spectroscopy, we have isolated and characterised two depside compounds, atraric acid (7) and methyl 3-hydroxy orsellinate (8). These two depsides were reported from this lichen species for the first time. The evaluation of the crude methanol extract against Gram-positive bacteria, Staphylococcus aureus, indicated insignificant activity. However, the isolated compounds have been previously reported to possess low antimicrobial activity against common pathogenic bacteria (Staphylococcus aureus, Bacillus cereus and Pseudomonas aeruginosa) but to show significant anti-legionellosis. Graphical abstract
{"title":"Isolation of Antibacterial Depside Constituents from Indonesian Folious Lichen, Candelaria fibrosa","authors":"A. S. Nugraha, Ikhar Ridho Dayli, Chintya Permata Zahky Sukrisno Putri, Lilla Nur Firli, A. N. Widhi Pratama, Bawon Triatmoko, L. Untari, H. Wongso, P. Keller, P. Wangchuk","doi":"10.1080/22311866.2021.2021986","DOIUrl":"https://doi.org/10.1080/22311866.2021.2021986","url":null,"abstract":"Abstract There is an urgent need for novel drug leads, especially for microbial infections due to continuing emergence of drug resistance. Natural products are the backbone of modern medicine and the lichens have an important role to play in the discovery of novel drugs. Indonesia is gifted with a diverse array of lichens, which remain underexplored for medicinal applications. In this study, we have collected a lichen, Candelaria fibrosa, and conducted phytochemical and bioactivity studies. Using high performance liquid chromatography, mass spectrometry, and nuclear magnetic resonance spectroscopy, we have isolated and characterised two depside compounds, atraric acid (7) and methyl 3-hydroxy orsellinate (8). These two depsides were reported from this lichen species for the first time. The evaluation of the crude methanol extract against Gram-positive bacteria, Staphylococcus aureus, indicated insignificant activity. However, the isolated compounds have been previously reported to possess low antimicrobial activity against common pathogenic bacteria (Staphylococcus aureus, Bacillus cereus and Pseudomonas aeruginosa) but to show significant anti-legionellosis. Graphical abstract","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42478607","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 : 2022-01-02DOI: 10.1080/22311866.2021.2023046
N. Kerebba, A. Oyedeji, R. Byamukama, S. Kuria, O. Oyedeji
Abstract Using bioactivity-guided isolation of bioactive compounds; deacetylviguiestenin, 4-O-caffeoyl-2-methyloxirane-2-carboxylic acid and sandaracopimaradiene-1α,9α-diol were obtained from Tithonia diversifolia (Hemsl.) A. Gray leaves and identified using spectroscopic methods. Their feeding deterrence activity against Sitophilus zeamais (Motsch.) including those of methanol crude extract, fractions, and the essential oil was determined. Results showed that the essential oil of T. diversifolia could not show significant anti-feedant activity at a dose of ˂0.29 μL/mg of flour disks. The solvent crude extract, some fractions and the isolated compounds, however, demonstrated feeding deterrence against S. zeamais. The feeding deterrence index of sandaracopimaradiene-1α,9α-diol was 81.19 ± 5.94% at 0.1% w/w (1 mg/g food) compared to 97.45 ± 0.43% for neemazal extract (10% azadirachtin) (positive control) at 10%w/w (100 mg/g food). The EC50 of deacetylviguiestin, 4-O-caffeoyl-2-methyloxirane-2-carboxylic acid and azadirachtin (commercial antifeedant) against S. zeamais were 22140.23 ± 9103.29, 3654.28 ± 2715.09 and 14.59 ± 5.59 ppm respectively. Although these compounds showed less activity against S. zeamais compared to azadirachtin, their anti-feedant activity was significant and are valuable alternatives.
{"title":"Evaluation for Feeding Deterrents Against Sitophilus zeamais (Motsch.) from Tithonia diversifolia (Hemsl.) A. Gray","authors":"N. Kerebba, A. Oyedeji, R. Byamukama, S. Kuria, O. Oyedeji","doi":"10.1080/22311866.2021.2023046","DOIUrl":"https://doi.org/10.1080/22311866.2021.2023046","url":null,"abstract":"Abstract Using bioactivity-guided isolation of bioactive compounds; deacetylviguiestenin, 4-O-caffeoyl-2-methyloxirane-2-carboxylic acid and sandaracopimaradiene-1α,9α-diol were obtained from Tithonia diversifolia (Hemsl.) A. Gray leaves and identified using spectroscopic methods. Their feeding deterrence activity against Sitophilus zeamais (Motsch.) including those of methanol crude extract, fractions, and the essential oil was determined. Results showed that the essential oil of T. diversifolia could not show significant anti-feedant activity at a dose of ˂0.29 μL/mg of flour disks. The solvent crude extract, some fractions and the isolated compounds, however, demonstrated feeding deterrence against S. zeamais. The feeding deterrence index of sandaracopimaradiene-1α,9α-diol was 81.19 ± 5.94% at 0.1% w/w (1 mg/g food) compared to 97.45 ± 0.43% for neemazal extract (10% azadirachtin) (positive control) at 10%w/w (100 mg/g food). The EC50 of deacetylviguiestin, 4-O-caffeoyl-2-methyloxirane-2-carboxylic acid and azadirachtin (commercial antifeedant) against S. zeamais were 22140.23 ± 9103.29, 3654.28 ± 2715.09 and 14.59 ± 5.59 ppm respectively. Although these compounds showed less activity against S. zeamais compared to azadirachtin, their anti-feedant activity was significant and are valuable alternatives.","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45674445","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 : 2022-01-02DOI: 10.1080/22311866.2021.2013943
Hagar Ashraf, Ashaimaa Y. Moussa, O. Eldahshan, A. Singab
Abstract Gleditsia species were widely used traditionally for the treatment of GIT problems and skin diseases, especially in Chinese traditional medicine. Gleditsia species isolated compounds and biological activities were summarized in a previous review published in 2015. This work aims to review the isolated chemical compounds from Gleditsia species and their biological activities during the period from 2015 to 2021. More than eighty compounds belonging to flavonoids, triterpenoidal saponins, alkaloids, lignans or coumarins were isolated from Gleditsia triacanthos L., Gleditsia sinensis Lam., Gleditsia capsica Desf., Gleditsia aquatic Marshal, and Gleditsia japonica Miq. during this period. Triterpenoidal saponins and flavonoids were the most abundant constituents of Gleditsia species. Crude extracts, fractions and isolated compounds showed diverse cytotoxic, antimicrobial, antihyperlipidemic, analgesic, antioxidant and hypoglycemic activities. Some of the possible mechanisms of actions are reported in this review such as causing apoptosis, affecting adhesion, migration and size of cancer cells and decreasing the expression of cyclooxygenase, prostaglandin E2, tumor necrosis factor-α and interleukin (IL)-1β. According to this review, new compounds are still being isolated from Gleditsia species with promising biological activities. Further studies can be conducted to explore more bioactive compounds responsible for the pharmacological activities of genus Gleditsia and elucidate their mechanisms of action. Graphical abstract
{"title":"Genus Gleditsia: A Phytochemical and Biological Review (2015-2020)","authors":"Hagar Ashraf, Ashaimaa Y. Moussa, O. Eldahshan, A. Singab","doi":"10.1080/22311866.2021.2013943","DOIUrl":"https://doi.org/10.1080/22311866.2021.2013943","url":null,"abstract":"Abstract Gleditsia species were widely used traditionally for the treatment of GIT problems and skin diseases, especially in Chinese traditional medicine. Gleditsia species isolated compounds and biological activities were summarized in a previous review published in 2015. This work aims to review the isolated chemical compounds from Gleditsia species and their biological activities during the period from 2015 to 2021. More than eighty compounds belonging to flavonoids, triterpenoidal saponins, alkaloids, lignans or coumarins were isolated from Gleditsia triacanthos L., Gleditsia sinensis Lam., Gleditsia capsica Desf., Gleditsia aquatic Marshal, and Gleditsia japonica Miq. during this period. Triterpenoidal saponins and flavonoids were the most abundant constituents of Gleditsia species. Crude extracts, fractions and isolated compounds showed diverse cytotoxic, antimicrobial, antihyperlipidemic, analgesic, antioxidant and hypoglycemic activities. Some of the possible mechanisms of actions are reported in this review such as causing apoptosis, affecting adhesion, migration and size of cancer cells and decreasing the expression of cyclooxygenase, prostaglandin E2, tumor necrosis factor-α and interleukin (IL)-1β. According to this review, new compounds are still being isolated from Gleditsia species with promising biological activities. Further studies can be conducted to explore more bioactive compounds responsible for the pharmacological activities of genus Gleditsia and elucidate their mechanisms of action. Graphical abstract","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46642547","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 : 2022-01-02DOI: 10.1080/22311866.2021.2021985
P. Saravana Kumar, Yu Li, Meijun He, P. Yuvaraj, K. Balakrishna, S. Ignacimuthu
Abstract The present study introduces an effective and rapid method for isolation of antifungal compound ricinine from Ricinus communis (L.). In this respect, the tender leaves of R. communis were extracted using methanol and tested for antifungal activity against a panel of dermatophytes and plant pathogenic fungi. Primarily, the total extract exhibited broad-spectrum antifungal activity with the zones of inhibition ranging from 12 ± 1.00 to 18.66 ± 1.52 mm. Further, investigation of chemical constituents led to the isolation of a cyano-pyridone alkaloid, ricinine using acid-base extraction. The compound exhibited significant antifungal activity with MIC values ranging from 6.25-250 µg/mL against the tested pathogenic fungi. Particularly, antifungal activity was recorded against A. flavus with the MIC value of 7.81 µg/mL followed by B. cinerea and A. niger with 15.62 µg/mL, respectively; T. mentagrophytes and T. rubrum with 62.5 µg/mL, respectively and it showed weak activity against Scopulariopsis sp. with 250 µg/mL. This efficient result provide new insights on large-scale isolation and identification of 4-methoxy-1-methyl-2-oxo-1,2-dihydropyridine-3-carbonitrile (Ricinine) which possess potent antifungal activity. In conclusion, the compound ricinine can be used as potential antifungal agent for controlling plant pathogenic fungi as well dermatophytes. Further, this potentially useful technique is operationally simple, safe, time-saving and inexpensive, and can be applied by medicinal, pharmaceutical and scientific research for the isolation of other potentially useful alkaloids in the drug discovery programs. Graphical abstract
{"title":"Rapid Isolation of Ricinine, a Pyridone Alkaloid from Ricinus communis (L.) with Antifungal Properties","authors":"P. Saravana Kumar, Yu Li, Meijun He, P. Yuvaraj, K. Balakrishna, S. Ignacimuthu","doi":"10.1080/22311866.2021.2021985","DOIUrl":"https://doi.org/10.1080/22311866.2021.2021985","url":null,"abstract":"Abstract The present study introduces an effective and rapid method for isolation of antifungal compound ricinine from Ricinus communis (L.). In this respect, the tender leaves of R. communis were extracted using methanol and tested for antifungal activity against a panel of dermatophytes and plant pathogenic fungi. Primarily, the total extract exhibited broad-spectrum antifungal activity with the zones of inhibition ranging from 12 ± 1.00 to 18.66 ± 1.52 mm. Further, investigation of chemical constituents led to the isolation of a cyano-pyridone alkaloid, ricinine using acid-base extraction. The compound exhibited significant antifungal activity with MIC values ranging from 6.25-250 µg/mL against the tested pathogenic fungi. Particularly, antifungal activity was recorded against A. flavus with the MIC value of 7.81 µg/mL followed by B. cinerea and A. niger with 15.62 µg/mL, respectively; T. mentagrophytes and T. rubrum with 62.5 µg/mL, respectively and it showed weak activity against Scopulariopsis sp. with 250 µg/mL. This efficient result provide new insights on large-scale isolation and identification of 4-methoxy-1-methyl-2-oxo-1,2-dihydropyridine-3-carbonitrile (Ricinine) which possess potent antifungal activity. In conclusion, the compound ricinine can be used as potential antifungal agent for controlling plant pathogenic fungi as well dermatophytes. Further, this potentially useful technique is operationally simple, safe, time-saving and inexpensive, and can be applied by medicinal, pharmaceutical and scientific research for the isolation of other potentially useful alkaloids in the drug discovery programs. Graphical abstract","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46475568","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 : 2022-01-02DOI: 10.1080/22311866.2021.2008269
C. Chandran, P. Smitha, D. Gayathri Devi
Abstract: Natural trypsin inhibitors are increasingly recognised as putative anticancer or antimicrobial therapeutics. In the present study, we isolated a proteinaceous trypsin inhibitor from the seeds of Artocarpus hirsutus to assess its anticancer, antioxidant and microbicidal effects. A trypsin inhibitory protein (AhTI) was isolated from the seeds of A. hirsutus using ion exchange and gel filtration chromatographic methods. The trypsin inhibitory activity of AhTI was confirmed by activity staining using Reverse Zymography. The effect of AhTI on human cancer cell lines (A431 and HT29) was studied by microscopic examination, MTT assay and LDH leakage analysis. Antioxidant activity of AhTI was analysed by ferric reducing power and DPPH radical scavenging assays. An agar well diffusion method was used to check the antimicrobial activity of AhTI. The purification protocols used in the study significantly increased the specific activity of the target protein from 72.65 ± 0.86 to 2048 ± 27.3. AhTI offers significant activity against the proliferation of the A431 and HT29 cancer cell lines. In vitro AhTI shows potent antioxidant activity and exhibits antimicrobial activity against all the bacteria and fungi isolates used in this study. Of particular note, AhTI was particularly effective against Staphylococcus aureus and Escherichia coli. This in vitro study shows that AhTIis a promising candidate for further development novel therapeutics targeting cancer, microbial infections and oxidative stress. Graphical abstract
{"title":"Seed Protein from Artocarpus hirsutus Lam. with Trypsin Inhibitory, Micro-bicidal and Antioxidant Activities Induces Depletion of Human Skin Cancer (A431) and Colon Cancer (HT29) Cells","authors":"C. Chandran, P. Smitha, D. Gayathri Devi","doi":"10.1080/22311866.2021.2008269","DOIUrl":"https://doi.org/10.1080/22311866.2021.2008269","url":null,"abstract":"Abstract: Natural trypsin inhibitors are increasingly recognised as putative anticancer or antimicrobial therapeutics. In the present study, we isolated a proteinaceous trypsin inhibitor from the seeds of Artocarpus hirsutus to assess its anticancer, antioxidant and microbicidal effects. A trypsin inhibitory protein (AhTI) was isolated from the seeds of A. hirsutus using ion exchange and gel filtration chromatographic methods. The trypsin inhibitory activity of AhTI was confirmed by activity staining using Reverse Zymography. The effect of AhTI on human cancer cell lines (A431 and HT29) was studied by microscopic examination, MTT assay and LDH leakage analysis. Antioxidant activity of AhTI was analysed by ferric reducing power and DPPH radical scavenging assays. An agar well diffusion method was used to check the antimicrobial activity of AhTI. The purification protocols used in the study significantly increased the specific activity of the target protein from 72.65 ± 0.86 to 2048 ± 27.3. AhTI offers significant activity against the proliferation of the A431 and HT29 cancer cell lines. In vitro AhTI shows potent antioxidant activity and exhibits antimicrobial activity against all the bacteria and fungi isolates used in this study. Of particular note, AhTI was particularly effective against Staphylococcus aureus and Escherichia coli. This in vitro study shows that AhTIis a promising candidate for further development novel therapeutics targeting cancer, microbial infections and oxidative stress. Graphical abstract","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46701922","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 : 2021-11-02DOI: 10.1080/22311866.2021.1944316
Varun Dhiman, D. Pant, T. Dhewa, Anita Padam
Abstract This article presents the pharmacological potential of numerous conopeptides as antidiabetic and anticancer agents. Different mechanisms, pharmacology with their peptide chemistry are also discussed. The study uses a comprehensive, transparent review approach with the analysis of available scientific literature focusing the medicinal applications. It involves the exploration of available literature using databases like Google Scholar, PubMed, Research Gate, and ISI web of knowledge. The relevant data and information were collected from different data sources including scientific databases, peer-review of previous and recently published research, and review articles. It has been found that limited research and comprehensive reviews have focused on investigating the possible antidiabetic and anticancer potential of different conopeptides. It is concluded that conopeptides are highly potent in the development of new generation medicines for diabetes and cancer cure which provide further possibilities in exploring drugs from the marine ecosystem.
摘要:本文介绍了许多康多肽作为抗糖尿病和抗癌药物的药理潜力。不同的作用机制，药理学及其肽化学也进行了讨论。本研究采用全面、透明的审查方法，对现有科学文献进行分析，重点是医学应用。它包括使用谷歌Scholar、PubMed、Research Gate和ISI web of knowledge等数据库对可用文献进行探索。相关数据和信息收集自不同的数据来源，包括科学数据库、对以前和最近发表的研究的同行评审以及综述文章。目前对不同康诺多肽可能的抗糖尿病和抗癌作用的研究比较有限，综述也比较全面。由此可见，康多肽在糖尿病和癌症治疗新一代药物的开发中具有重要的应用价值，为从海洋生态系统中开发药物提供了进一步的可能性。
{"title":"A Review on the Antidiabetic and Anticancer Activities of Conus Venom Peptides","authors":"Varun Dhiman, D. Pant, T. Dhewa, Anita Padam","doi":"10.1080/22311866.2021.1944316","DOIUrl":"https://doi.org/10.1080/22311866.2021.1944316","url":null,"abstract":"Abstract This article presents the pharmacological potential of numerous conopeptides as antidiabetic and anticancer agents. Different mechanisms, pharmacology with their peptide chemistry are also discussed. The study uses a comprehensive, transparent review approach with the analysis of available scientific literature focusing the medicinal applications. It involves the exploration of available literature using databases like Google Scholar, PubMed, Research Gate, and ISI web of knowledge. The relevant data and information were collected from different data sources including scientific databases, peer-review of previous and recently published research, and review articles. It has been found that limited research and comprehensive reviews have focused on investigating the possible antidiabetic and anticancer potential of different conopeptides. It is concluded that conopeptides are highly potent in the development of new generation medicines for diabetes and cancer cure which provide further possibilities in exploring drugs from the marine ecosystem.","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2021-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47297543","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 : 2021-11-02DOI: 10.1080/22311866.2021.1970021
Rijo Rajeev, Shreedhanya D Marathe, V. Niranjan, Bhavya Sharma, Suma Sarojini
Abstract Improvements and advances in health care over the past few decades have increased life expectancy and quality of life. However, this has resulted in an increase in non-communicable diseases like dementia, Alzheimer’s Disease (AD), etc. AD most commonly affects the older population, but recent studies reveal that it can also affect people of any age group. As of now, there are no accessible treatments or therapies that reverse the progression of the disease. The few existing medications to treat AD include Donepezil (Aricept), Galantamine (Razadyne) and Rivastigmine (Exelon) provide only temporary relief and come with several side effects like diarrhoea, vomiting, nausea, fatigue, insomnia, loss of appetite, and weight loss. An effective and augmenting therapy with Cholinesterase inhibitors from natural products is gaining popularity among researchers. Plant sterols have been known to play roles in inhibiting proteins implicated in the development of AD. The present study highlights the significance and scope of Stigmasterol, a phytochemical in Saraca asoca in the alleviation of AD. Our study involving the use of QSAR, ADME, molecular interaction, and molecular docking has shown that Stigmasterol has the potential to be developed as a therapeutic drug to curb the progression of AD after thorough validation procedures. Graphical abstract
{"title":"In silico Analysis of Stigmasterol from Saraca asoca as a Potential Therapeutic Drug Against Alzheimer’s Disease","authors":"Rijo Rajeev, Shreedhanya D Marathe, V. Niranjan, Bhavya Sharma, Suma Sarojini","doi":"10.1080/22311866.2021.1970021","DOIUrl":"https://doi.org/10.1080/22311866.2021.1970021","url":null,"abstract":"Abstract Improvements and advances in health care over the past few decades have increased life expectancy and quality of life. However, this has resulted in an increase in non-communicable diseases like dementia, Alzheimer’s Disease (AD), etc. AD most commonly affects the older population, but recent studies reveal that it can also affect people of any age group. As of now, there are no accessible treatments or therapies that reverse the progression of the disease. The few existing medications to treat AD include Donepezil (Aricept), Galantamine (Razadyne) and Rivastigmine (Exelon) provide only temporary relief and come with several side effects like diarrhoea, vomiting, nausea, fatigue, insomnia, loss of appetite, and weight loss. An effective and augmenting therapy with Cholinesterase inhibitors from natural products is gaining popularity among researchers. Plant sterols have been known to play roles in inhibiting proteins implicated in the development of AD. The present study highlights the significance and scope of Stigmasterol, a phytochemical in Saraca asoca in the alleviation of AD. Our study involving the use of QSAR, ADME, molecular interaction, and molecular docking has shown that Stigmasterol has the potential to be developed as a therapeutic drug to curb the progression of AD after thorough validation procedures. Graphical abstract","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2021-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45291354","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 : 2021-11-02DOI: 10.1080/22311866.2021.1987323
M. S. So'aib, N. A. Latip, H. Tan
Abstract Carica papaya Linn. (papaya plant) is a ubiquitous crop in tropical regions which is mainly harvested for its sweet-tasting fruit. Various parts of the papaya plant are used in folklore medicines to treat various ailments. This work presented the toxic and teratogenic effects of fermented Carica papaya leaf (CPL) on zebrafish (Danio rerio) embryos. The eggs from the spawning of the adult male and female zebrafish were collected and exposed to different concentrations of fermented CPL; 250, 125, 62.5, 31.25, 15.625 and 0 µg/ mL for six to 72 h post fertilisation (hpf). The survival and sublethal effects of these treatments on zebrafish embryos such as mortality and hatchability were calculated using microscopic observation while the heartbeat rate was measured using DanioScope. The toxic effects of fermented CPL on zebrafish embryos was found to be concentration dependent. The median lethal concentration (LC50) was 133.1 µg/mL as calculated from the probit-log (concentration) regression model using Microsoft Excel. This value fell into the category of less than toxic according to OECD guideline. The total flavonoid content (TFC) of the fermented CPL was also higher at the end of the fermentation as compared to onset of fermentation.
{"title":"Lethal Concentration Determination of Fermented Carica papaya Leaf on Zebrafish (Danio rerio) Embryo Using Probit Regression with Arbitrary Slopes","authors":"M. S. So'aib, N. A. Latip, H. Tan","doi":"10.1080/22311866.2021.1987323","DOIUrl":"https://doi.org/10.1080/22311866.2021.1987323","url":null,"abstract":"Abstract Carica papaya Linn. (papaya plant) is a ubiquitous crop in tropical regions which is mainly harvested for its sweet-tasting fruit. Various parts of the papaya plant are used in folklore medicines to treat various ailments. This work presented the toxic and teratogenic effects of fermented Carica papaya leaf (CPL) on zebrafish (Danio rerio) embryos. The eggs from the spawning of the adult male and female zebrafish were collected and exposed to different concentrations of fermented CPL; 250, 125, 62.5, 31.25, 15.625 and 0 µg/ mL for six to 72 h post fertilisation (hpf). The survival and sublethal effects of these treatments on zebrafish embryos such as mortality and hatchability were calculated using microscopic observation while the heartbeat rate was measured using DanioScope. The toxic effects of fermented CPL on zebrafish embryos was found to be concentration dependent. The median lethal concentration (LC50) was 133.1 µg/mL as calculated from the probit-log (concentration) regression model using Microsoft Excel. This value fell into the category of less than toxic according to OECD guideline. The total flavonoid content (TFC) of the fermented CPL was also higher at the end of the fermentation as compared to onset of fermentation.","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2021-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44914859","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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