Journal of Biologically Active Products from Nature最新文献

Evaluation of Cytotoxicity, Cell-Cycle Arrest, and Apoptotic Induction of Three Ruellia tuberosa Leaf Extracts in MCF-7 Cells 三种麻风叶提取物对MCF-7细胞的细胞毒性、细胞周期阻滞和诱导凋亡的研究

Journal of Biologically Active Products from Nature Pub Date : 2023-11-08 DOI: 10.1080/22311866.2023.2278726

P.L. Teoh, F.F. Lem, B.E. Cheong

{"title":"Evaluation of Cytotoxicity, Cell-Cycle Arrest, and Apoptotic Induction of Three <i>Ruellia tuberosa</i> Leaf Extracts in MCF-7 Cells","authors":"P.L. Teoh, F.F. Lem, B.E. Cheong","doi":"10.1080/22311866.2023.2278726","DOIUrl":"https://doi.org/10.1080/22311866.2023.2278726","url":null,"abstract":"AbstractThis study investigated the mechanisms responsible for the antiproliferative activities of three Ruellia tuberosa (RT) leaf extracts against MCF-7 cells after liquid-liquid partitioning. Among these extracts, methanol leaf extract exhibited the greatest inhibition of cell growth compared to water and hexane extracts. Results from JC-1 staining and apoptosis assay demonstrated that these leaf extracts induced apoptosis via caspase or mitochondrial independent manner as only substantial apoptotic cells with no obvious loss of mitochondrial membrane potential were found. However, the decrease in the BCL-2/BAX ratio is due to upregulated BAX expression, implying cells undergoing apoptosis. The expression of caspase 9 was unaltered except for cells treated with hexane leaf extract. Additionally, perturbation of cell cycle progression mainly at G1 or S phases was noticeable in treated cells and concentration-dependent. The distinct effect of different leaf extracts on the cell cycle was also reflected by the dysregulation of cyclins (A2 or E1) and cyclin-dependent kinase (CDK6). These findings have unveiled the therapeutical value of RT leaf extracts in breast cancer.Key words: Breast cancerApoptosisCell cycleRuellia tuberosa","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":"31 S104","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135343222","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}

引用次数: 0

Procyanidin Dimer from the Stem Bark of Moringa oleifera (Lam.) Attenuates Insulin Resistance in Rats 辣木茎皮原花青素二聚体的研究减轻大鼠胰岛素抵抗

Journal of Biologically Active Products from Nature Pub Date : 2023-11-08 DOI: 10.1080/22311866.2023.2277897

Hasanpasha N. Sholapur, Basanagouda M. Patil, Fatima Sanjeri Dasankoppa

引用次数: 0

Anti-hyperlipidemic and Antioxidant Potential of Phenolic Monoterpenes Rich Thymus satureioides Coss. Volatile Oil 富含酚类单萜的胸腺草抗高脂血症和抗氧化潜力。挥发油

Journal of Biologically Active Products from Nature Pub Date : 2023-11-08 DOI: 10.1080/22311866.2023.2277899

Hamza Elbouny, Brahim Ouahzizi, Mohamed Bammou, Khalid Sellam, Chakib Alem

{"title":"Anti-hyperlipidemic and Antioxidant Potential of Phenolic Monoterpenes Rich <i>Thymus satureioides</i> Coss. Volatile Oil","authors":"Hamza Elbouny, Brahim Ouahzizi, Mohamed Bammou, Khalid Sellam, Chakib Alem","doi":"10.1080/22311866.2023.2277899","DOIUrl":"https://doi.org/10.1080/22311866.2023.2277899","url":null,"abstract":"AbstractThis work aims to evaluate the antioxidant and lipid-lowering effects of the essential oil of Thymus satureioides and its main compounds. The profile of volatile phytochemicals was determined by gas chromatography-mass spectrometry (GC/MS). Total phenolic compounds estimation and antioxidant activity assessment have been evaluated according to the literature models and the anti-hyperlipidemic activity was evaluated using triton wr-1339 induced hyperlipidemic rats model. Our findings revealed that thymol (26.6%) and carvacrol (25.9%) were the most abundant volatile constituents. Furthermore, the essential oil was found to be rich in phenolic components (6.50 ±0.14 GAE mg/g EO) and exhibits significant antioxidant potential (DPPH IC50=25.02 mg/mL; ABTS IC50=0.87 mg/mL). Additionally, the volatile oil displayed a potent lipid-lowering potential by reducing the levels of triglycerides (-68.78%), cholesterol (-36.34%), and non-HDL-C (-38.44%). This effect can be explained by its richness in thymol and carvacrol, which demonstrated a comparable anti-hyperlipidemic effect to that of simvastatin. We conclude that Thymus satureioides is a natural producer of lipid-lowering agents that can be used as a potential natural alternative treatment for managing hyperlipidemia.Keywords: Thymus satureioidesvolatile oilthymolcarvacrolhyperlipidemia","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":"57 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135392898","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}

引用次数: 0

Chemical profile and antiproliferative activity of essential oil of Centella asiatica from Mebo, Pasighat in Arunachal Pradesh, India 印度阿鲁纳恰尔邦帕西哈特梅博百岁草精油的化学成分和抗增殖活性

Journal of Biologically Active Products from Nature Pub Date : 2023-09-03 DOI: 10.1080/22311866.2023.2287113

Rajani Kurup Sukumaryamma Remadevi, Ajikumaran Nair Sadasivan Nair, Sabulal Baby

{"title":"Chemical profile and antiproliferative activity of essential oil of Centella asiatica from Mebo, Pasighat in Arunachal Pradesh, India","authors":"Rajani Kurup Sukumaryamma Remadevi, Ajikumaran Nair Sadasivan Nair, Sabulal Baby","doi":"10.1080/22311866.2023.2287113","DOIUrl":"https://doi.org/10.1080/22311866.2023.2287113","url":null,"abstract":"Abstract Centella asiatica (CA) is a perennial herb with critical uses in traditional medicines. This study reports the chemical composition of the essential oil of C. asiatica (CAEO) collected from Mebo, a high altitude location in Arunachal Pradesh in India, and its antiproliferative activity. Hydrodistillation yielded pale yellow coloured essential oil (0.2 mL, 0.14% v/w). Twenty-five compounds were identified in CAEO by gas chromatographic analysis of which sesquiterpene hydrocarbons constituted 87.82%, followed by oxygenated sesquiterpenes (2.57%), monoterpene hydrocarbons (1.38%) and other miscellaneous compounds (2.28%). Sesquiterpenes, α-humulene (41.31% ± 0.03), E-caryophyllene (19.72% ± 0.01), α-copaene (7.98% ± 0.00), β-elemene (5.56% ± 0.08) and γ-muurolene (5.18% ± 0.01), were the major constituents in CAEO. In MTT assay CAEO displayed significant cytotoxicity against SKBr3 and DLA cells with CD50 values of 4.7 µg/mL and 9.2 µg/mL, respectively. The major components of CAEO, α-humulene and (E)-caryophyllene, displayed cytotoxicity on SKBr3 and DLA cells, whereas (E)-caryophyllene demonstrated higher toxicity than α-humulene. CD50 values of (E)-caryophyllene on SKBr3 and DLA cells were 51.6 and 47.2 µg/mL, respectively. The antiproliferative activity of CAEO is due to the synergistic effects of its terpenoid constituents, and it supports the nutritional and medicinal uses of CA. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":"68 1","pages":"460 - 468"},"PeriodicalIF":0.0,"publicationDate":"2023-09-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139343060","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}

引用次数: 0

Isolation of new bibenzyl derivatives from Bulbophyllum auricomum and evaluation of their α-glucosidase inhibitory activity 从牛肝菌中分离出新的苄基衍生物并评估其α-葡萄糖苷酶抑制活性

Journal of Biologically Active Products from Nature Pub Date : 2023-09-03 DOI: 10.1080/22311866.2023.2286246

Hoo Tint San, Ne Yi Hla, Ei Mon Hla, C. Chansriniyom, B. Sritularak, K. Likhitwitayawuid

{"title":"Isolation of new bibenzyl derivatives from Bulbophyllum auricomum and evaluation of their α-glucosidase inhibitory activity","authors":"Hoo Tint San, Ne Yi Hla, Ei Mon Hla, C. Chansriniyom, B. Sritularak, K. Likhitwitayawuid","doi":"10.1080/22311866.2023.2286246","DOIUrl":"https://doi.org/10.1080/22311866.2023.2286246","url":null,"abstract":"Abstract Bulbophyllum auricomum Lindl., commonly referred to as the 'Royal Thazin' in Myanmar, holds the esteemed status of being the national flower of the country. In our research, we delved into the ethyl acetate extract derived from the pseudobulbs and roots of this plant. This extract exhibited significant inhibitory activity against the α-glucosidase enzyme, prompting a detailed investigation into its active compounds. Our study resulted in the isolation and characterization of several compounds, including a novel natural product named 2-(4-hydroxyphenyl) ethyl 3-(2-hydroxyphenyl) propanoate. Additionally, we identified two previously unreported inseparable isomeric bibenzyls, namely 7-hydroxybatatasin III and 8-hydroxybatatasin III. Furthermore, we isolated six known compounds, including batatasin III, lusianthridin, tristin, phochinenin G, phoyunnanin E, and phoyunnanin C. Significantly, our study unveiled that phochinenin G acts as a reversible noncompetitive inhibitor of the α-glucosidase enzyme. This compound displayed greater inhibitory activity than the standard drug acarbose. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":"11 1","pages":"437 - 447"},"PeriodicalIF":0.0,"publicationDate":"2023-09-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139343038","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}

引用次数: 0

Conservation of endangered medicinal plant Oroxylum indicum Vent. by substitution of roots with small branches via comparative chemo-profiling 通过比较化学分析，用小枝替代根部，保护濒危药用植物 Oroxylum indicum Vent.

Journal of Biologically Active Products from Nature Pub Date : 2023-09-03 DOI: 10.1080/22311866.2023.2283467

Himanshu Sharma, Bhavana Srivastava, Ravindra Singh

{"title":"Conservation of endangered medicinal plant Oroxylum indicum Vent. by substitution of roots with small branches via comparative chemo-profiling","authors":"Himanshu Sharma, Bhavana Srivastava, Ravindra Singh","doi":"10.1080/22311866.2023.2283467","DOIUrl":"https://doi.org/10.1080/22311866.2023.2283467","url":null,"abstract":"Abstract Oroxylum indicum Vent. is an endangered medicinal plant due to the overexploitation of roots in the herbal market. The study proposed the substitution of its roots with small branches on a phytochemical basis for plant sustainability and the exploration of the medicinal potential of alternative plant parts. The comparative phytochemical profiles of roots and small branches of O. indicum were examined through physicochemical, spectrophotometric, and HPTLC analysis. Analogous HPTLC profiles indicated phytochemical similarities in different extracts of roots and small branches, along with higher concentrations of total phenolics and flavonoids found in the aerial part than in the roots. Equality in the phytoconstituent pattern demonstrates the possibility of using small branches over the roots. The study advocates the substitution of roots for small branches of O. indicum, substituent may be used alternatively in place of roots in medicinal applications and to conserve such threatened medicinal plants for future sustainability. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":"25 1","pages":"490 - 503"},"PeriodicalIF":0.0,"publicationDate":"2023-09-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139343067","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}

引用次数: 0

Potential and Prospective of Traditional Indian Medicinal Plants for the Treatment of Diabetes 印度传统药用植物治疗糖尿病的潜力和前景

Journal of Biologically Active Products from Nature Pub Date : 2023-07-04 DOI: 10.1080/22311866.2023.2262964

Chinmaya Panda, Parth Sharma, U. S. Dixit, L. Pandey

{"title":"Potential and Prospective of Traditional Indian Medicinal Plants for the Treatment of Diabetes","authors":"Chinmaya Panda, Parth Sharma, U. S. Dixit, L. Pandey","doi":"10.1080/22311866.2023.2262964","DOIUrl":"https://doi.org/10.1080/22311866.2023.2262964","url":null,"abstract":"Abstract The emergence of diabetes as a silent epidemic and the failure of conventional medicines to provide a safe, effective, and affordable stance has rendered scientists to go back to the ancient literature on traditional plant-based therapies. Though many spices and herbs are used for usual culinary purposes, organized research on the beneficial effect of such herbs in regard to diabetes is less explored. Traditionally, ayurvedic phyto-based polyherbal formulations have been described to reduce blood glucose levels and ease allied complications related to diabetes. The present review amasses nine ethnomedicinal plants (cinnamon, fenugreek, bitter gourd, neem, Indian bael, black myrobalan, Indian gooseberry, turmeric, and giloy) of the Indian subcontinent frequently mentioned in a traditional setting. Systematic assessment of different extraction methods, computational, in vitro, in vivo, and human trials for diabetes involving plants, is presented. A list of some of the commercially available polyherbal formulations for diabetes, along with their key constituents, is discussed. Finally, considering the concomitant use of herbs along with conventional drugs, a brief perspective on the possible herb-drug interactions, limitations, and future directions is provided. This review sheds light on the bioactive components of pharmaceutically relevant plants mentioned in traditional settings for hypoglycemic control. Subsequently, wider acceptance of complementary therapy for efficient management of diabetes would improve the quality of life of patients across the globe. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":"59 1","pages":"316 - 360"},"PeriodicalIF":0.0,"publicationDate":"2023-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139363194","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}

引用次数: 0

Antibacterial Activity of Isolated Compounds from Allophylus spicatus (Poir.) Radlk (Sapindacea) 从 Allophylus spicatus (Poir.) Radlk (Sapindacea) 分离出的化合物的抗菌活性

Journal of Biologically Active Products from Nature Pub Date : 2023-07-04 DOI: 10.1080/22311866.2023.2262951

E. O. Okpala, P. Onocha, Muhammad Shaiq Ali, O. Odeja, Michael Gabriel Ibok, Godfrey Okechukwu Eneogwe, M. Lateef

{"title":"Antibacterial Activity of Isolated Compounds from Allophylus spicatus (Poir.) Radlk (Sapindacea)","authors":"E. O. Okpala, P. Onocha, Muhammad Shaiq Ali, O. Odeja, Michael Gabriel Ibok, Godfrey Okechukwu Eneogwe, M. Lateef","doi":"10.1080/22311866.2023.2262951","DOIUrl":"https://doi.org/10.1080/22311866.2023.2262951","url":null,"abstract":"Abstract Phytochemical investigation on the roots of Allophylus spicatus (Sapindacea) led to the isolation of four compounds, namely cleomiscosin A (1), cleomiscosin C (2), scopoletin (3) and 3-oxotirucalla-7,24-dien-24-oic acid (4). The structures of the compounds were established by spectroscopic analysis: UV, IR, 1D and 2D NMR, EI-MS and HR-EI-MS and compared with the literature. These compounds are reported for the first time from the plant. The compounds showed potent antibacterial activity, marked inhibition against most of the tested bacterial strains: Pseudomonas aeruginosa (ATCC 27853), Escherichia coli (ATCC 25922), Salmonella typhi (ATCC 25923), Klebsiella pneumonia (ATCC 13883), Streptococcus faecalis (ATCC 29212) and Micrococcus luteus (ATCC 10240), with a zone of inhibition between 0.7±0.35 - 16±0.46 mm as compared with the zone of inhibition of Streptomycin (20±0.34 - 31±0.29 mm), a known antibacterial drug used as the standard. The antibacterial activity of the isolated phytochemicals could be responsible for the plant ethno-medicinal uses. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":"9 1","pages":"380 - 389"},"PeriodicalIF":0.0,"publicationDate":"2023-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139363396","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}

引用次数: 0

Indigestible Dextrin Alleviates the Intestinal Absorption of Alpha-linolenic Acid More Markedly Than That of Linoleic Acid in Obese Mice 难消化糊精对肥胖小鼠肠道吸收α-亚麻酸的作用比亚油酸更明显

Journal of Biologically Active Products from Nature Pub Date : 2023-07-04 DOI: 10.1080/22311866.2023.2256309

A. Sato, Kaito Matsumoto, Takahiro Fukase, K. Ebina

{"title":"Indigestible Dextrin Alleviates the Intestinal Absorption of Alpha-linolenic Acid More Markedly Than That of Linoleic Acid in Obese Mice","authors":"A. Sato, Kaito Matsumoto, Takahiro Fukase, K. Ebina","doi":"10.1080/22311866.2023.2256309","DOIUrl":"https://doi.org/10.1080/22311866.2023.2256309","url":null,"abstract":"Abstract Linoleic acid (LA) and alpha-linolenic acid (ALA) constitute the main dietary polyunsaturated fatty acids. Indigestible dextrin (DEX) is a dietary fiber that causes a beneficial decrease in lifestyle-related disease risk factors. We investigated the effects of DEX on intestinal absorption of LA and ALA in obese mice. KK-Ay/TaJcl obese mice were fed an ALA- or LA-abundant diet and provided with water in the absence and presence of 0.06 w/v% DEX for 4 weeks. The levels of lipids in serum samples and the lipase activity in serum and liver were analyzed. The effects of DEX on the intestinal absorption of LA and ALA were investigated using an in vitro model of the intestinal absorption process in the fed-state simulated intestinal fluid (FeSSIF) solution. ALA resulted in an increase in the serum triglyceride (TG) levels than those observed upon feeding an LA-abundant diet. DEX suppressed significantly the ALA-dependent increase in serum TG levels. Neither LA nor ALA affected the serum levels of total cholesterol and high-density lipoprotein cholesterol, as well as the serum and hepatic lipase activities. Moreover, ALA showed better solubility than LA in FeSSIF solution. The solubility of ALA in FeSSIF solution was significantly suppressed by DEX, whereas that of LA was not affected by DEX. ALA can be absorbed more easily than LA during the intestinal absorption process, probably leading to an increase in the serum TG levels and then DEX more selectively inhibits the intestinal absorption of ALA compared to that of LA. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":"7 1","pages":"410 - 423"},"PeriodicalIF":0.0,"publicationDate":"2023-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139362805","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}

引用次数: 0

A Clerodane Diterpene from Aquarius scaber (Rataj) Christenh. & Byng Leaves as Inhibitor of Leishmania mexicana Trypanosomatid Enzymes 水瓶座疮痂（Rataj）Christenh. & Byng 叶中的一种 Clerodane 二萜作为墨西哥利什曼原虫锥虫酶的抑制剂

Journal of Biologically Active Products from Nature Pub Date : 2023-07-04 DOI: 10.1080/22311866.2023.2256311

Kheytiany H.S. Lopes, Virgínia C.P. Silva, Marcos J. Jacinto, Aline A. de Souza, Camila G.D. Padovani, M. F. Machado, W. A. Judice, Paulo T. Sousa

{"title":"A Clerodane Diterpene from Aquarius scaber (Rataj) Christenh. & Byng Leaves as Inhibitor of Leishmania mexicana Trypanosomatid Enzymes","authors":"Kheytiany H.S. Lopes, Virgínia C.P. Silva, Marcos J. Jacinto, Aline A. de Souza, Camila G.D. Padovani, M. F. Machado, W. A. Judice, Paulo T. Sousa","doi":"10.1080/22311866.2023.2256311","DOIUrl":"https://doi.org/10.1080/22311866.2023.2256311","url":null,"abstract":"Abstract The clerodane diterpenoid 2-oxo-5α,8α-cleroda-3,13-dien-16,15-olide (1) isolated from the leaves of A. scaber was identified by IR, 1H and 13C NMR (1D and 2D) and HRESIMS spectrometric analysis. This is the first report of this diterpene in the Aquarius genus. The inhibitory potential of 1 has been determined against cysteine proteases from Leishmania mexicana rCPB2.8, rCPB3.0 and rH84Y. The inhibitory constants (Ki and αKi) as well as the mechanism of action were also investigated. Compound 1 was 7- and 18-fold more potent in the inhibition of rCPB3.0 (IC50 = 4.2 µM) than rCPB2.8 (IC50 = 20 µM) and rH84Y (IC50 = 75 µM). From the kinetic mechanisms of inhibitor binding, we found that compound 1 has a higher affinity to rCPB3.0 (K i = 7.5 µM and αK i = 7.4 µM) than rCPB2.8 (K i = 15.4 µM, αK i = 14.7 µM) and rH84Y (K i = 81.4, and αK i = 27.9 μM and βKi = 41.5 µM). Compound 1 also presented a non-competitive linear simple inhibition mechanism at both enzymes rCPB3.0 and rCPB2.8. On the other hand, 1 presented a positive cooperativity mechanism of inhibition at rH84Y. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":"11 1","pages":"369 - 379"},"PeriodicalIF":0.0,"publicationDate":"2023-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139363220","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}

引用次数: 0