Pub Date : 2023-03-04DOI: 10.1080/22311866.2023.2225482
Ana Paula de Araújo Boleti, Pedro Hernique de Oliveira Cardoso, Breno Frihling, Zaira da Rosa Guterres, Ana Francisca Gomes da Silva, A. A. A. de Rezende, F. Garcez, W. Garcez, U. Graf, M. Spanó, Lillian May Grespan Estodutto da Silva, L. Migliolo
Abstract Ocotea minarum (Nees & Mart.) Mez is a tree belonging to the Lauraceae family and found in the Brazilian Cerrado ecosystem. Although the chemical composition of this species has already been described, little is known about the biological activities of one of the constituents of its fruits-the alkaloid tryptophol-5-O-β-D-glucopyranoside. In the present study, we assessed the anti-neuroinflammatory, mutagenic and recombinogenic properties of this indole alkaloid. Cytotoxicity and anti-inflammatory activities were performed using a model of LPS-stimulated microglia BV-2. Mutation detection and somatic recombination were performed in Drosophila melanogaster wing cells. The results showed that tryptophol-5-O-β-D-glucopyranoside was not cytotoxic to BV-2 cells at the concentrations tested. The results also showed that this alkaloid inhibited by 75% the inflammatory response induced by LPS at the concentration of 189 μM with IC50 = 12.07±0.35 μM. The analysis of the MH offspring showed that different concentrations of the alkaloid did not induce statistically significant increases in the frequencies of mutant spots when compared to those observed in the negative control. With these results, we can conclude that tryptophol-5-O-β-D-glucopyranoside presents therapeutic potential for the treatment of neurodegenerative diseases with no mutagenic effects. GRAPHICAL ABSTRACT
{"title":"Evaluation of in vitro and in vivo Anti-neuroinflammatory and Genotoxic Activities of the Alkaloid Tryptophol-5-O-β-D-glucopyranoside from Ocotea minarum","authors":"Ana Paula de Araújo Boleti, Pedro Hernique de Oliveira Cardoso, Breno Frihling, Zaira da Rosa Guterres, Ana Francisca Gomes da Silva, A. A. A. de Rezende, F. Garcez, W. Garcez, U. Graf, M. Spanó, Lillian May Grespan Estodutto da Silva, L. Migliolo","doi":"10.1080/22311866.2023.2225482","DOIUrl":"https://doi.org/10.1080/22311866.2023.2225482","url":null,"abstract":"Abstract Ocotea minarum (Nees & Mart.) Mez is a tree belonging to the Lauraceae family and found in the Brazilian Cerrado ecosystem. Although the chemical composition of this species has already been described, little is known about the biological activities of one of the constituents of its fruits-the alkaloid tryptophol-5-O-β-D-glucopyranoside. In the present study, we assessed the anti-neuroinflammatory, mutagenic and recombinogenic properties of this indole alkaloid. Cytotoxicity and anti-inflammatory activities were performed using a model of LPS-stimulated microglia BV-2. Mutation detection and somatic recombination were performed in Drosophila melanogaster wing cells. The results showed that tryptophol-5-O-β-D-glucopyranoside was not cytotoxic to BV-2 cells at the concentrations tested. The results also showed that this alkaloid inhibited by 75% the inflammatory response induced by LPS at the concentration of 189 μM with IC50 = 12.07±0.35 μM. The analysis of the MH offspring showed that different concentrations of the alkaloid did not induce statistically significant increases in the frequencies of mutant spots when compared to those observed in the negative control. With these results, we can conclude that tryptophol-5-O-β-D-glucopyranoside presents therapeutic potential for the treatment of neurodegenerative diseases with no mutagenic effects. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41701248","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 : 2023-03-04DOI: 10.1080/22311866.2023.2224286
Hieu Tran-Trung, L. Giang, D. Duc, Nguyen Thi Giang An, D. Van Son, Danh C. Vu, Nguyễn Thị Kim Anh, Hien Nguyen-Thi-Thu, Kh Tam, Trang H. D. Nguyen
Abstract Siliquamomum oreodoxa and Curcuma thorelii in the family Zingiberaceae are two new species native to Vietnam. In the present work, volatile composition of essential oils (EOs) from leaves of the two plant species and their antimicrobial activities were reported for the first time. The gas chromatography-mass spectrometry analytical results revealed that the major constituents of the S. oreodoxa leaf EO were α-pinene (39.23%), β-pinene (26.34%), myrtenyl acetate (8.24%), and limonene (7.85%). The results also showed the C. thorelii EO was predominantly composed of β-pinene (21.58%) and caryophyllene (14.26%). In the antimicrobial assay, the two EOs were found to possess strong antimicrobial activities against multiple pathogenic bacterial and fungal strains, with minimum inhibitory concentrations ranging between 32 and 128 μg/mL. GRAPHICAL ABSTRACT
{"title":"Volatile Constituents and In vitro Antimicrobial Activities of Essential Oils from Leaves of Siliquamomum oreodoxa N.S. Lý & Škorničk and Curcuma thorelii Gagnep. (Zingiberaceae) Growing in Vietnam","authors":"Hieu Tran-Trung, L. Giang, D. Duc, Nguyen Thi Giang An, D. Van Son, Danh C. Vu, Nguyễn Thị Kim Anh, Hien Nguyen-Thi-Thu, Kh Tam, Trang H. D. Nguyen","doi":"10.1080/22311866.2023.2224286","DOIUrl":"https://doi.org/10.1080/22311866.2023.2224286","url":null,"abstract":"Abstract Siliquamomum oreodoxa and Curcuma thorelii in the family Zingiberaceae are two new species native to Vietnam. In the present work, volatile composition of essential oils (EOs) from leaves of the two plant species and their antimicrobial activities were reported for the first time. The gas chromatography-mass spectrometry analytical results revealed that the major constituents of the S. oreodoxa leaf EO were α-pinene (39.23%), β-pinene (26.34%), myrtenyl acetate (8.24%), and limonene (7.85%). The results also showed the C. thorelii EO was predominantly composed of β-pinene (21.58%) and caryophyllene (14.26%). In the antimicrobial assay, the two EOs were found to possess strong antimicrobial activities against multiple pathogenic bacterial and fungal strains, with minimum inhibitory concentrations ranging between 32 and 128 μg/mL. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41353420","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 : 2023-03-04DOI: 10.1080/22311866.2023.2220312
Ozaira Qadri, N. Hilal, K. Fazili
Abstract Bergenia ciliata (haw.) Sternb, a well-known medicinal plant, has traditionally been used to treat various ailments, such as diabetes, microbial infections, and kidney stones, owing to its anti-inflammatory and anti-tussive properties. Here we aimed to evaluate the anti-cancer potential of the plant extract and deduce the molecular pathways involved. To investigate this, we used the MTT assay to determine the IC50 values of the methanolic extract of B. ciliata (BcME) in MDA-MB-231 and C6-Glioma cell lines. After treating the cancer cell lines with BcME for 18 hours, we evaluated the UPR signalling markers, including pIRE1, Xbp1, ATF6, eIF2α, ATF4, and CHOP, using Immunoblotting. We also used RT-PCR to determine the mRNA levels of ATF4 and performed enzyme assays using Spectrophotometric techniques to measure ROS levels. Our results indicate that B. ciliata has potent anti-cancer properties due to its ability to modulate UPR and ROS pathways. Specifically, the plant extract effectively repressed the cytoprotective UPR by blocking IRE1-Xbp1 and ATF6 pathways while enhancing the PERK-ATF4-CHOP pathway, which is known to switch UPR towards apoptosis. Furthermore, our study revealed that B. ciliata significantly caused the accumulation of ROS in cancer cells and inhibited the antioxidant enzymes catalase and superoxide dismutase. These results conclusively suggest that BcME works synergistically on both UPR and ROS pathways to promote apoptosis and eliminate cancerous cells and thus serves as a potential primary source for bioactive molecules, selectively targeting cancer cells. GRAPHICAL ABSTRACT
{"title":"Unveiling the Anti-cancer Potential of Bergenia ciliata (haw.) Sternb: A Mechanistic Study on UPR Modulation and ROS Generation","authors":"Ozaira Qadri, N. Hilal, K. Fazili","doi":"10.1080/22311866.2023.2220312","DOIUrl":"https://doi.org/10.1080/22311866.2023.2220312","url":null,"abstract":"Abstract Bergenia ciliata (haw.) Sternb, a well-known medicinal plant, has traditionally been used to treat various ailments, such as diabetes, microbial infections, and kidney stones, owing to its anti-inflammatory and anti-tussive properties. Here we aimed to evaluate the anti-cancer potential of the plant extract and deduce the molecular pathways involved. To investigate this, we used the MTT assay to determine the IC50 values of the methanolic extract of B. ciliata (BcME) in MDA-MB-231 and C6-Glioma cell lines. After treating the cancer cell lines with BcME for 18 hours, we evaluated the UPR signalling markers, including pIRE1, Xbp1, ATF6, eIF2α, ATF4, and CHOP, using Immunoblotting. We also used RT-PCR to determine the mRNA levels of ATF4 and performed enzyme assays using Spectrophotometric techniques to measure ROS levels. Our results indicate that B. ciliata has potent anti-cancer properties due to its ability to modulate UPR and ROS pathways. Specifically, the plant extract effectively repressed the cytoprotective UPR by blocking IRE1-Xbp1 and ATF6 pathways while enhancing the PERK-ATF4-CHOP pathway, which is known to switch UPR towards apoptosis. Furthermore, our study revealed that B. ciliata significantly caused the accumulation of ROS in cancer cells and inhibited the antioxidant enzymes catalase and superoxide dismutase. These results conclusively suggest that BcME works synergistically on both UPR and ROS pathways to promote apoptosis and eliminate cancerous cells and thus serves as a potential primary source for bioactive molecules, selectively targeting cancer cells. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46539026","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 : 2023-03-04DOI: 10.1080/22311866.2023.2225480
Weslley Guimarães Bovi, C. S. Desidério, R. O. Trevisan, M. M. Santos, Mariana de Oliveira Silva, M. V. da Silva, V. R. Júnior, E. U. Bucek, C. J. Oliveira
Abstract Noni, also known as Morinda citrifolia, is a plant that has been widely used for treating various pathologies due to its allegedly anti-inflammatory and immunomodulating properties. Macrophages and monocytes are critical immune cells that initiate inflammation and generate an immune response against various aggressors, regardless of their causative agent. However, it is not well investigated how noni fruit components affect the behavior or phenotype of these cells. Hence, studies in this direction could potentially demonstrate the therapeutic effects of this fruit, which is consumed worldwide. This study aimed to investigate the therapeutic properties of noni fruit juice in modulating the behavior and phenotype of human monocytes and macrophage cells in vitro. The results show that noni fruit juice inhibited the production of nitric oxide (NO) and inflammatory cytokines such as tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-4, while stimulating the production of the anti-inflammatory cytokine IL-10 in monocytes. In addition, it negatively modulated the expression of toll-like receptor 4 (TLR4). In macrophages, noni fruit juice enhanced the secretion of all cytokines and NO, and inhibited the expression of TLR4. The contrasting results observed could be attributed to the joint stimuli of PMA (Phorbol 12-myristate 13-acetate), which was used to induce macrophage differentiation and noni Juice. Overall, the data indicate that noni may act as an anti-inflammatory agent and may aid in the treatment of uncontrolled inflammatory diseases as a complementary treatment to conventional therapies, under medical supervision. GRAPHICAL ABSTRACT
{"title":"Exploring the Potential Immunomodulatory Properties of Noni Juice on Human Monocytes and Macrophages","authors":"Weslley Guimarães Bovi, C. S. Desidério, R. O. Trevisan, M. M. Santos, Mariana de Oliveira Silva, M. V. da Silva, V. R. Júnior, E. U. Bucek, C. J. Oliveira","doi":"10.1080/22311866.2023.2225480","DOIUrl":"https://doi.org/10.1080/22311866.2023.2225480","url":null,"abstract":"Abstract Noni, also known as Morinda citrifolia, is a plant that has been widely used for treating various pathologies due to its allegedly anti-inflammatory and immunomodulating properties. Macrophages and monocytes are critical immune cells that initiate inflammation and generate an immune response against various aggressors, regardless of their causative agent. However, it is not well investigated how noni fruit components affect the behavior or phenotype of these cells. Hence, studies in this direction could potentially demonstrate the therapeutic effects of this fruit, which is consumed worldwide. This study aimed to investigate the therapeutic properties of noni fruit juice in modulating the behavior and phenotype of human monocytes and macrophage cells in vitro. The results show that noni fruit juice inhibited the production of nitric oxide (NO) and inflammatory cytokines such as tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-4, while stimulating the production of the anti-inflammatory cytokine IL-10 in monocytes. In addition, it negatively modulated the expression of toll-like receptor 4 (TLR4). In macrophages, noni fruit juice enhanced the secretion of all cytokines and NO, and inhibited the expression of TLR4. The contrasting results observed could be attributed to the joint stimuli of PMA (Phorbol 12-myristate 13-acetate), which was used to induce macrophage differentiation and noni Juice. Overall, the data indicate that noni may act as an anti-inflammatory agent and may aid in the treatment of uncontrolled inflammatory diseases as a complementary treatment to conventional therapies, under medical supervision. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41886976","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 : 2023-03-04DOI: 10.1080/22311866.2023.2211043
Nonthalert Lertnitikul, R. Suttisri, Supotchana Sitthigool, C. Pattamadilok, Kanyanat Piewpong, Ariya Khanboon, Jatupol Liangsakul, Cherdsak Boonyong
Abstract Four amides, namely, piperine (1), pellitorine (2), piperiline (5) and N-trans-p-coumaroyltyramine (7), and three aristolactams, i.e., piperolactams D (3), B (4) and A (6), were isolated from the methanol extract of Piper wallichii stems. Piperiline, piperolactams B and D were obtained from this plant for the first time. Compounds 1, 3, 5, 6 and 7 were evaluated for their antioxidant, antimicrobial and cytotoxic activities. Piperine (1) displayed the highest antioxidant activity in scavenging DPPH radicals with an IC50 value of 94.51 ± 11.91 μM. Piperolactams D (3) and A (6) showed antibacterial activity against Gram-positive bacteria (B. subtilis and S. aureus) with MICs of between 500-1000 μM. All test compounds were cytotoxic to breast cancer (MCF-7) cells, while the aristolactams were more toxic to colon cancer (Caco-2) cells than the amides. Compounds 1, 3, 6 and 7 were moderately cytotoxic to the doxorubicin-resistant MCF-7 subline (MCF-7/DOX). All compounds were non-toxic to normal human fibroblast (NIH/3T3) cells. GRAPHICAL ABSTRACT
{"title":"Antioxidant, Antimicrobial and Cytotoxic Activities of Amides and Aristolactams from Piper wallichii (Miq.) Hand.-Mazz. Stems","authors":"Nonthalert Lertnitikul, R. Suttisri, Supotchana Sitthigool, C. Pattamadilok, Kanyanat Piewpong, Ariya Khanboon, Jatupol Liangsakul, Cherdsak Boonyong","doi":"10.1080/22311866.2023.2211043","DOIUrl":"https://doi.org/10.1080/22311866.2023.2211043","url":null,"abstract":"Abstract Four amides, namely, piperine (1), pellitorine (2), piperiline (5) and N-trans-p-coumaroyltyramine (7), and three aristolactams, i.e., piperolactams D (3), B (4) and A (6), were isolated from the methanol extract of Piper wallichii stems. Piperiline, piperolactams B and D were obtained from this plant for the first time. Compounds 1, 3, 5, 6 and 7 were evaluated for their antioxidant, antimicrobial and cytotoxic activities. Piperine (1) displayed the highest antioxidant activity in scavenging DPPH radicals with an IC50 value of 94.51 ± 11.91 μM. Piperolactams D (3) and A (6) showed antibacterial activity against Gram-positive bacteria (B. subtilis and S. aureus) with MICs of between 500-1000 μM. All test compounds were cytotoxic to breast cancer (MCF-7) cells, while the aristolactams were more toxic to colon cancer (Caco-2) cells than the amides. Compounds 1, 3, 6 and 7 were moderately cytotoxic to the doxorubicin-resistant MCF-7 subline (MCF-7/DOX). All compounds were non-toxic to normal human fibroblast (NIH/3T3) cells. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43901505","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 : 2023-03-04DOI: 10.1080/22311866.2023.2224283
Jhalnath Dhungel, B. Marasini, Erendra Manandhar, R. Rathnayaka, S. Samarakoon, S. Shyaula
Abstract From the caudex of Stephania glandulifera Miers, five alkaloids were isolated using a cold percolation method with 90% methanol. The methanol extract was fractionated into three different fractions from where the alkaloids were purified using preparative HPLC. Structure elucidations were performed by modern spectral analysis including Mass and 1D and 2D-NMR spectroscopy. The purified compounds were tested against the LN-229 human brain glioblastoma cell line by performing a Sulforhodamine B assay (SRB). The isolated compounds were confirmed to be tetrahydropalmatine (1), palmatine (2), stepharanine (3), stepholidine (4), and stepharine (5). Compound 5 showed anticancer activity in the LN-229 human brain glioblastoma cell line with an IC50 value of 8.1 μg/mL. In this study, five alkaloids belonging to three classes namely proaporphine, protoberberine, and tetrahydroprotoberberine were isolated for the first time from Stephania glandulifera Miers. Among them, stepharine showed anticancer activity in the LN-229 human brain glioblastoma cell line which can be further developed as a potential anticancer agent. GRAPHICAL ABSTRACT
摘要采用90%甲醇冷渗法制备了金假藤(Stephania glandulifera Miers)的5种生物碱。甲醇提取物被分成三个不同的部分，其中生物碱被纯化使用制备高效液相色谱。通过现代光谱分析(包括质谱、一维和二维核磁共振谱)对其结构进行了分析。用硫代丹B实验(Sulforhodamine B assay, SRB)检测纯化的化合物对LN-229人脑胶质母细胞瘤细胞系的作用。分离得到的化合物分别为四氢巴马汀(1)、巴马汀(2)、皂素(3)、皂素碱(4)和皂素(5)。化合物5对LN-229人脑胶质母细胞瘤细胞具有抗肿瘤活性，IC50值为8.1 μg/mL。本研究首次从菝葜属植物中分离到原阿啡、原小檗碱和四氢原小檗碱3大类5种生物碱。其中，凡士林在LN-229人脑胶质母细胞瘤细胞系中显示出抗癌活性，可作为一种潜在的抗癌药物进一步开发。图形抽象
{"title":"Cytotoxic Activity of Alkaloids Isolated from Stephania glandulifera Miers","authors":"Jhalnath Dhungel, B. Marasini, Erendra Manandhar, R. Rathnayaka, S. Samarakoon, S. Shyaula","doi":"10.1080/22311866.2023.2224283","DOIUrl":"https://doi.org/10.1080/22311866.2023.2224283","url":null,"abstract":"Abstract From the caudex of Stephania glandulifera Miers, five alkaloids were isolated using a cold percolation method with 90% methanol. The methanol extract was fractionated into three different fractions from where the alkaloids were purified using preparative HPLC. Structure elucidations were performed by modern spectral analysis including Mass and 1D and 2D-NMR spectroscopy. The purified compounds were tested against the LN-229 human brain glioblastoma cell line by performing a Sulforhodamine B assay (SRB). The isolated compounds were confirmed to be tetrahydropalmatine (1), palmatine (2), stepharanine (3), stepholidine (4), and stepharine (5). Compound 5 showed anticancer activity in the LN-229 human brain glioblastoma cell line with an IC50 value of 8.1 μg/mL. In this study, five alkaloids belonging to three classes namely proaporphine, protoberberine, and tetrahydroprotoberberine were isolated for the first time from Stephania glandulifera Miers. Among them, stepharine showed anticancer activity in the LN-229 human brain glioblastoma cell line which can be further developed as a potential anticancer agent. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45202806","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 : 2023-03-04DOI: 10.1080/22311866.2023.2211046
S. A. Nair, Rajani Kurup Sukumaryamma Remadevi, Smrithi S. Lal, R. Raju, R. Antony, Sabulal Baby
Abstract Anemia schimperiana C.Presl subsp. wightiana (Gardener) Fraser-Jenkins is a rhizomatous fern endemic to south India. Its rhizome and frond (leaf) essential oils (EOs) were isolated and characterized by gas chromatographic techniques. Thirty compounds (99.1%) of the rhizome EO were characterized, with myrtenyl acetate (50.6%), α-pinene (26.0%), myrtenol (7.3%) and trans-pinocarveol (5.6%) as its major constituents. Twenty-four compounds (97.8%), with trans-pinocarveol (43.0%), pinocarvone (17.3%) and myrtenyl acetate (15.8%), were identified in the frond EO. In MTT assay, rhizome EO showed prominent cytotoxicity against C6 (CD50 86.0 µg/mL) and DLA (CD50 6.1 µg/mL) cells. Fluorescent microscopic and caspase-3 activity assays demonstrated apoptotic cell death induced by the rhizome EO in DLA cells. MTT assay of myrtenyl acetate, α-pinene and myrtenol against DLA cells displayed CD50s of 7.4, 0.9 and 20.5 µg/mL, respectively, revealing α-pinene as the prominent constituent causing antiproliferative activity of the rhizome EO. This is the first report on the chemistry and antiproliferative activity of this rare aromatic fern endemic to south India. GRAPHICAL ABSTRACT
{"title":"Chemical Composition and Antiproliferative Activity of Rhizome and Frond Essential Oils of Anemia schimperiana subsp. wightiana, a Rare Fern Endemic to South India","authors":"S. A. Nair, Rajani Kurup Sukumaryamma Remadevi, Smrithi S. Lal, R. Raju, R. Antony, Sabulal Baby","doi":"10.1080/22311866.2023.2211046","DOIUrl":"https://doi.org/10.1080/22311866.2023.2211046","url":null,"abstract":"Abstract Anemia schimperiana C.Presl subsp. wightiana (Gardener) Fraser-Jenkins is a rhizomatous fern endemic to south India. Its rhizome and frond (leaf) essential oils (EOs) were isolated and characterized by gas chromatographic techniques. Thirty compounds (99.1%) of the rhizome EO were characterized, with myrtenyl acetate (50.6%), α-pinene (26.0%), myrtenol (7.3%) and trans-pinocarveol (5.6%) as its major constituents. Twenty-four compounds (97.8%), with trans-pinocarveol (43.0%), pinocarvone (17.3%) and myrtenyl acetate (15.8%), were identified in the frond EO. In MTT assay, rhizome EO showed prominent cytotoxicity against C6 (CD50 86.0 µg/mL) and DLA (CD50 6.1 µg/mL) cells. Fluorescent microscopic and caspase-3 activity assays demonstrated apoptotic cell death induced by the rhizome EO in DLA cells. MTT assay of myrtenyl acetate, α-pinene and myrtenol against DLA cells displayed CD50s of 7.4, 0.9 and 20.5 µg/mL, respectively, revealing α-pinene as the prominent constituent causing antiproliferative activity of the rhizome EO. This is the first report on the chemistry and antiproliferative activity of this rare aromatic fern endemic to south India. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42983442","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 : 2023-01-02DOI: 10.1080/22311866.2023.2185681
S. Sankaran, R. Dubey, S. Lohidasan
Abstract The potential of Indian propolis as a suitable therapeutic agent is still to be explored to the fullest. As variation in the chemical composition across different geographical regions has been a major concern, it is, therefore, worthwhile to systematically investigate, and assess the quality of Indian propolis and set nationalized standards. The propolis collected from three different regions were authenticated for the major plant source, followed by the evaluation of physicochemical properties. Different extraction methods were compared, with their influence on balsam content, polyphenol, and flavonoid content. The sample coded HAR using ultrasonication gave the highest extraction yield of 71.87%. Further, the process variables in the ultrasonication method (i.e. Amplitude, extraction time, the concentration of ethanol) at three levels were optimized using the Box-Behnken response design. The model was found significant with the concentration of ethanol having a maximum influence on the responses. The model was successfully verified by setting the amplitude at 48%, extraction time to 5.6 mins, and ethanol concentration to 87% v/v. The extraction efficiency of 83.86±1.17% was achieved with a substantial diminution of extraction time. The total phenolic, total flavonol, and total flavanone content of the optimized batch were 28.74±0.13 mgGAE/g, 4.66±0.78 mgQE/g, and 3.16±0.14 mgPE/g of propolis respectively. Further HPTLC fingerprint image of the optimized extract revealed the presence of quercetin, p-coumaric acid, kaempferol, chrysin, pinocembrin, and galangin. GRAPHICAL ABSTRACT
{"title":"Optimization of Extraction Conditions using Response Surface Methodology and HPTLC Fingerprinting Analysis of Indian Propolis","authors":"S. Sankaran, R. Dubey, S. Lohidasan","doi":"10.1080/22311866.2023.2185681","DOIUrl":"https://doi.org/10.1080/22311866.2023.2185681","url":null,"abstract":"Abstract The potential of Indian propolis as a suitable therapeutic agent is still to be explored to the fullest. As variation in the chemical composition across different geographical regions has been a major concern, it is, therefore, worthwhile to systematically investigate, and assess the quality of Indian propolis and set nationalized standards. The propolis collected from three different regions were authenticated for the major plant source, followed by the evaluation of physicochemical properties. Different extraction methods were compared, with their influence on balsam content, polyphenol, and flavonoid content. The sample coded HAR using ultrasonication gave the highest extraction yield of 71.87%. Further, the process variables in the ultrasonication method (i.e. Amplitude, extraction time, the concentration of ethanol) at three levels were optimized using the Box-Behnken response design. The model was found significant with the concentration of ethanol having a maximum influence on the responses. The model was successfully verified by setting the amplitude at 48%, extraction time to 5.6 mins, and ethanol concentration to 87% v/v. The extraction efficiency of 83.86±1.17% was achieved with a substantial diminution of extraction time. The total phenolic, total flavonol, and total flavanone content of the optimized batch were 28.74±0.13 mgGAE/g, 4.66±0.78 mgQE/g, and 3.16±0.14 mgPE/g of propolis respectively. Further HPTLC fingerprint image of the optimized extract revealed the presence of quercetin, p-coumaric acid, kaempferol, chrysin, pinocembrin, and galangin. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47732979","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 : 2023-01-02DOI: 10.1080/22311866.2023.2172079
A. S. Nugraha, Lilla Nur Firli, R. Hendra, P. Keller, Reza Yuridian Purwoko, H. Idrus, Rien Ritawidya, M. B. Febrian, I. Mahendra, A. Kurniawan, Alfian M. Forentin, V. Y. Susilo, C. E. Kusumaningrum, Y. Setiadi, H. Wongso
Abstract This study describes the isolation of bioactive compounds and their in vitro anticancer activities from Melia azedarach L leaves from Karanglor, Karangan, Karanganom Klaten, Central Java-Indonesia. Isolated and characterised were the phenolics, kaempferol 7-O-rutinoside 1 and 4-methoxyresorcinol 3, The anticancer activity of the crude methanol extract of M. azedarach against a number cell lines (LNCaP, MDA-MB-231, and MCF-7) was found to be moderate; kaempferol derivatives were notable for their antiproliferative activities. Computational analysis, including molecular docking simulations and molecular dynamic studies, were used to investigate the feasibility of radiolabelled versions of 1 and 3 as theranostic agents targeting tyrosine kinase-type cell surface receptor HER2 in cancer - the iodinated derivatives 2 and 4, respectively, were used in this investigation as surrogates. The corresponding radioiodinated 2 and 4 were found to have high binding affinities of 10.1 and 5.7 kcal/mol, respectively, and have a good stability on the receptor. GRAPHICAL ABSTRACT
摘要本研究从印度尼西亚中爪哇Karanglor、Karanganom Klaten、Karanganom Klaten产苦楝叶中分离得到生物活性化合物及其体外抗癌活性。从苦楝粗甲醇提取物中分离鉴定出山奈酚7- o -芦丁苷1和4-甲氧基间苯二酚3，发现苦楝粗甲醇提取物对LNCaP、MDA-MB-231和MCF-7细胞的抗癌活性中等;山奈酚衍生物具有显著的抗增殖活性。计算分析，包括分子对接模拟和分子动力学研究，用于研究放射性标记版本的1和3作为靶向肿瘤酪氨酸激酶型细胞表面受体HER2的治疗药物的可行性-碘化衍生物2和4分别在本研究中作为替代品。相应的放射性碘化2和4分别具有10.1和5.7 kcal/mol的高结合亲和力，并且在受体上具有良好的稳定性。图形抽象
{"title":"Anticancer activity of Indonesian Melia azedarach L.: Phyto-chemistry, in vitro and in silico studies","authors":"A. S. Nugraha, Lilla Nur Firli, R. Hendra, P. Keller, Reza Yuridian Purwoko, H. Idrus, Rien Ritawidya, M. B. Febrian, I. Mahendra, A. Kurniawan, Alfian M. Forentin, V. Y. Susilo, C. E. Kusumaningrum, Y. Setiadi, H. Wongso","doi":"10.1080/22311866.2023.2172079","DOIUrl":"https://doi.org/10.1080/22311866.2023.2172079","url":null,"abstract":"Abstract This study describes the isolation of bioactive compounds and their in vitro anticancer activities from Melia azedarach L leaves from Karanglor, Karangan, Karanganom Klaten, Central Java-Indonesia. Isolated and characterised were the phenolics, kaempferol 7-O-rutinoside 1 and 4-methoxyresorcinol 3, The anticancer activity of the crude methanol extract of M. azedarach against a number cell lines (LNCaP, MDA-MB-231, and MCF-7) was found to be moderate; kaempferol derivatives were notable for their antiproliferative activities. Computational analysis, including molecular docking simulations and molecular dynamic studies, were used to investigate the feasibility of radiolabelled versions of 1 and 3 as theranostic agents targeting tyrosine kinase-type cell surface receptor HER2 in cancer - the iodinated derivatives 2 and 4, respectively, were used in this investigation as surrogates. The corresponding radioiodinated 2 and 4 were found to have high binding affinities of 10.1 and 5.7 kcal/mol, respectively, and have a good stability on the receptor. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47684035","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}
Abstract Breast cancer (BC) is a major type of cancer found in women worldwide, accounting for more than 25% of all females diagnosed as BC patients. The BC treatment still needs to be highly effective with few adverse effects on the rest of the body. This study's objective was to investigate how hispolon enhanced anticancer activities and examine the underlying processes in human breast cancer cells. Hispolon was used to treat the HTB-26 cell lines. We investigated cell viability, intracellular reactive oxygen species (ROS) production, immunofluorescence straining, MDC assay, and RT-PCR. According to the findings, hispolon inhibited HTB-26 cells from proliferating and caused them to undergo apoptosis. When the mechanism of action of hispolon was investigated, it was discovered that BCL-2 expression was downregulated while pro-apoptotic genes including caspase-3, caspase-9, and BAX were upregulated. The level of intracellular ROS was also shown to be increased by hispolon, and the expression of antioxidant genes including SOD, GPX, and Catalase was found to be downregulated. The increase in the confocal fluorescence image of LC3I/II and the identification of upregulated autophagy-related genes, such as LC3I/II, ATG5, ATG10, and ATG12, served as indicators of the activation of autophagy. Therefore, our findings showed that hispolon had great potential for being an effective therapeutic agent and could cause cell death in breast cancer cells. GRAPHICAL ABSTRACT
{"title":"Hispolon, A Bioactive Compound from Phellinus linteus, Induces Apoptosis of Human Breast Cancer Cells Through the Modulation of Oxidative Stress and Autophagy","authors":"Amorn Pangjantuk, Phongsakorn Chueaphromsri, Phongsakorn Kunhorm, Ruchee Phonchai, S. Chumkiew, Nipha Chaicharoenau-domrung, Parinya Noisa","doi":"10.1080/22311866.2023.2191994","DOIUrl":"https://doi.org/10.1080/22311866.2023.2191994","url":null,"abstract":"Abstract Breast cancer (BC) is a major type of cancer found in women worldwide, accounting for more than 25% of all females diagnosed as BC patients. The BC treatment still needs to be highly effective with few adverse effects on the rest of the body. This study's objective was to investigate how hispolon enhanced anticancer activities and examine the underlying processes in human breast cancer cells. Hispolon was used to treat the HTB-26 cell lines. We investigated cell viability, intracellular reactive oxygen species (ROS) production, immunofluorescence straining, MDC assay, and RT-PCR. According to the findings, hispolon inhibited HTB-26 cells from proliferating and caused them to undergo apoptosis. When the mechanism of action of hispolon was investigated, it was discovered that BCL-2 expression was downregulated while pro-apoptotic genes including caspase-3, caspase-9, and BAX were upregulated. The level of intracellular ROS was also shown to be increased by hispolon, and the expression of antioxidant genes including SOD, GPX, and Catalase was found to be downregulated. The increase in the confocal fluorescence image of LC3I/II and the identification of upregulated autophagy-related genes, such as LC3I/II, ATG5, ATG10, and ATG12, served as indicators of the activation of autophagy. Therefore, our findings showed that hispolon had great potential for being an effective therapeutic agent and could cause cell death in breast cancer cells. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49196331","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}
京公网安备 11010802042870号
京ICP备2023020795号-1
扫码关注我们
求助内容：
应助结果提醒方式：