{"title":"Natural benzofuran derivatives as promising scaffold for alleviating Alzheimer symptoms: acetylcholinesterase inhibition, structure activity relationship and <i>in silico</i> studies.","authors":"Ahmed A M A Selim, Marwa A Ibrahim","doi":"10.1080/14786419.2024.2431998","DOIUrl":"https://doi.org/10.1080/14786419.2024.2431998","url":null,"abstract":"<p><p>Three isolated natural benzofuran compounds <b>1a-c</b> and four semi-synthesized benzofuran derivatives <b>2a,b</b> and <b>3a,b</b> were evaluated for their <i>in vitro</i> acetylcholinesterase inhibition assay. Most of the tested compounds showed moderate activity with IC<sub>50</sub> ranged from 102.4 ± 5.72 µM to 565.75 ± 4.17 µM, the most potent compound was kellin <b>1a</b> with IC<sub>50</sub> 102.4 ± 5.72 µM. The kellin derivatives <b>1a, 2a</b> and <b>3a</b> bearing additional methoxyl group showed more inhibition activity than its analogues of visnagin derivatives <b>1b,c</b>, <b>2b</b> and <b>3b</b>. The <i>in silico</i> investigation on the seven benzofuran derivatives matched our <i>in vitro</i> acetylcholinesterase results and explains the similarity in structures between the benzofuran compounds and donepezil drug. khellin had the best pharmacophore features among the studied compounds, the best fit score 1.862 and best dock score -9.135. In addition, our <i>in silico</i> study showed clearly that compounds carrying additional hydrophobic group had more potent activity through matched more ligand features.</p>","PeriodicalId":18990,"journal":{"name":"Natural Product Research","volume":" ","pages":"1-7"},"PeriodicalIF":1.9,"publicationDate":"2024-11-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142682113","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Raquel Anacleto Dos Anjos, Juliana Teixeira Araújo Gonçalves da Silva, Bruno Mançano Class, Lucas Oliveira da Silva, Lavinia Ferreira Leal, Sarah Bitler Delatorre Rosa, Francisco Paiva Machado, Hildegardo Seibert França, Andréa Monte Alto Costa, Leandro Machado Rocha, Gleyce Moreno Barbosa
{"title":"<i>Hypericum brasiliense:</i> assessment of the antioxidant potential in UVA-induced <i>in vitro</i> phototoxicity.","authors":"Raquel Anacleto Dos Anjos, Juliana Teixeira Araújo Gonçalves da Silva, Bruno Mançano Class, Lucas Oliveira da Silva, Lavinia Ferreira Leal, Sarah Bitler Delatorre Rosa, Francisco Paiva Machado, Hildegardo Seibert França, Andréa Monte Alto Costa, Leandro Machado Rocha, Gleyce Moreno Barbosa","doi":"10.1080/14786419.2024.2427808","DOIUrl":"https://doi.org/10.1080/14786419.2024.2427808","url":null,"abstract":"<p><p>Photoaging induced by ultraviolet A (UVA) radiation is mainly caused by the reactive oxygen species (ROS) increase, which trigger undesirable changes in the skin, such as inflammatory reactions, wrinkles, hyperpigmentation, and loss of elasticity. In this context, plant ingredients have been highlighted in recent decades due to their antioxidant mechanisms. This study investigated the potential of <i>Hypericum brasiliense</i> ethanolic extract against UVA-induced damage in 3T3 fibroblasts. Cells exposed to a single UVA dose (4 J/cm<sup>2</sup>, 30 min) were treated with different extract concentrations. The results showed that <i>H. brasiliense</i> extract has antioxidant potential, mitigating UVA-induced stress by reducing ROS and lipid peroxidation. Furthermore, the extract stimulated fibroblast proliferation, suggesting its potential to restore cell viability after radiation-induced damage. The search for replacing synthetic actives with natural ones reinforces the importance of these findings on the antioxidant and regenerative properties of <i>H. brasiliense</i> extract, making it a promising anti-aging ingredient or a sunscreen adjuvant.</p>","PeriodicalId":18990,"journal":{"name":"Natural Product Research","volume":" ","pages":"1-7"},"PeriodicalIF":1.9,"publicationDate":"2024-11-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142682108","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Congcong Wang, Rui Chen, Lingxiao Gong, Hong Xu, Jie Liu, Huijuan Zhang
{"title":"Inhibiting hydrolytic enzyme activity and slowing carbohydrate digestion using lotus seed epicarp phenolic extracts.","authors":"Congcong Wang, Rui Chen, Lingxiao Gong, Hong Xu, Jie Liu, Huijuan Zhang","doi":"10.1080/14786419.2024.2426066","DOIUrl":"https://doi.org/10.1080/14786419.2024.2426066","url":null,"abstract":"<p><p>This study investigated the hypoglycaemic activity of lotus seed epicarp phenolic extract (LSEPE) by inhibiting starch hydrolytic enzyme activity and slowing down carbohydrate digestion. Total phenolic and flavonoid contents in LSEPE were 620.37 ± 10.45 mg GAE/g DW and 422.69 ± 23.57 mg RE/g DW, respectively. A total of 57 phenolic compounds were first identified in LSEPE. The IC<sub>50</sub> of LSEPE for inhibiting α-amylase and α-glucosidase were 124.44 ± 2.89 μg/mL and 0.99 ± 0.02 μg/mL, approximately 3.28 to 1.61 times that of acarbose. LSEPE acted as a mixed-type inhibitor of α-amylase and an anti-competitive-type inhibitor of α-glucosidase. UV spectroscopy, fluorescence quenching, and CD analysis showed that LSEPE could change the enzymes' microenvironment and hydrophobicity. Moreover, LSEPE slowed the starch hydrolysis rate <i>in vitro</i> and increased the proportions of slowly digestible starch (SDS) and resistant starch (RS) by 60.51% and 19.98%. Therefore, the lotus seed epicarppolyphenols could be the potential natural ingredients for developing anti-hyperglycemic functional foods.</p>","PeriodicalId":18990,"journal":{"name":"Natural Product Research","volume":" ","pages":"1-12"},"PeriodicalIF":1.9,"publicationDate":"2024-11-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142687601","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Comparative study of phytochemical content, antioxidant, and anti-inflammatory properties of <i>Merremia hirta</i> Merr. mature plant and microgreen.","authors":"Dian Kurniati, Rahma Naifa Septiany, Elazmanawati Lembong, Indira Lanti Kayaputri, Gemilang Lara Utama","doi":"10.1080/14786419.2024.2425795","DOIUrl":"https://doi.org/10.1080/14786419.2024.2425795","url":null,"abstract":"<p><p><i>Merremia hirta</i> Merr. is a plant belonging to the Convolvulaceae family, commonly used as a vegetable in Southeast Asia. The plant harbours diverse bioactive constituents, including polyphenols and flavonoids. Microgreens have gained popularity as a cultivation trend. They are referred to as superfoods due to their high bioactive content, which is estimated to be up to 10 times greater than mature plants. <i>M. hirta</i> Merr. microgreen and mature plant were investigated to determine their total phenol content using the Folin Ciocalteu method, total flavonoid content using AlCl<sub>3</sub>, antioxidant activity using 2,2-diphenyl-1- picrylhydrazyl and ferric reducing antioxidant power, and anti-inflammatory activity by protein denaturation inhibition <i>in vitro</i>. Microgreen demonstrated greater total phenolic content, directly associated with its high antioxidant activity compared to mature plants. However, the mature stage of <i>M. hirta</i> Merr. remains superior in terms of overall flavonoid content and anti-inflammatory activity.</p>","PeriodicalId":18990,"journal":{"name":"Natural Product Research","volume":" ","pages":"1-9"},"PeriodicalIF":1.9,"publicationDate":"2024-11-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142687597","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Isoquinoline alkaloids with bioactive constituents from the roots and rhizomes of <i>Hylomecon japonica</i>.","authors":"Zhen Cao, Shang-Jun Zhu, Zhao-Wei Xue, Lu-Ye Yao, Xin-Xin Zhang, Zeng-Jun Guo","doi":"10.1080/14786419.2024.2429122","DOIUrl":"https://doi.org/10.1080/14786419.2024.2429122","url":null,"abstract":"<p><p>Isoquinoline alkaloids are important effective chemical components separated from the <i>Hylomecon japonica</i>, which were mostly reported as planar structures. By using chiral HPLC, we have concluded that some natural isoquinoline alkaloids exist as enantiomeric mixtures, providing a novel direction for future research on isoquinoline alkaloids. Finally, three pairs of enantiomeric isoquinoline alkaloids (<b>1-3</b>, including five undescribed compounds-<b>1a/1b</b>, <b>3a/3b</b> and <b>2b</b>), together with another eight known isoquinoline alkaloids (<b>4-9</b>) were isolated from the roots and rhizomes of <i>Hylomecon japonica</i>. Their structures were elucidated by NMR, HRESIMS, UV, IR, and their absolute configurations were further defined by quantum chemical calculations of ECD spectra. The cytotoxic activities of these isolated compounds in MCF-7 cells were evaluated by MTT methods. Among them, the alkaloids <b>1a</b>, <b>1b</b>, <b>2b</b>, <b>3b</b> and other known alkaloids <b>5a</b> and <b>5b</b> had good inhibitory effects on MCF-7 cells of breast cancer <i>in vitro</i>, with an IC<sub>50</sub> lower than 20 μM.</p>","PeriodicalId":18990,"journal":{"name":"Natural Product Research","volume":" ","pages":"1-9"},"PeriodicalIF":1.9,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142676442","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Extended-spectrum β - lactamase inhibitory potential of <i>Dichrocephala integrifolia</i>: an <i>in vitro</i> and computational studies.","authors":"Anupama Moirangthem, Taranga Jyoti Baruah, Mridusmita Paul, Birson Ingti, Amitabha Bhattacharjee, Anand Prakash Maurya, Susmita Paul, Bhaskar Jyoti Das","doi":"10.1080/14786419.2024.2429529","DOIUrl":"https://doi.org/10.1080/14786419.2024.2429529","url":null,"abstract":"<p><p>Extended-spectrum β-lactamases (ESBL) producing enterobacteriales are a major global health concern since they often result in the ineffectiveness of empirical antibiotic therapy with β-lactams. This study aims to identify potential medicinal plants that can inhibit β-lactamase and subsequently enhance the activity of the β-lactams against resistant bacterial strains. A synergistic study of <i>Dichrocephala integrifolia</i> extract exhibited good synergistic activity against a CTX-M-producing organism, which was confirmed using an agar-based diffusion bioassay method. Further validation was done by Molecular docking in which, the phytocompound Propanamide, N-[4-(4-chlorophenyl)-2-thiazolyl]-3-(1-pyrrolidinyl)-/NSC339591, obtained from the GC-MS study showed a good binding affinity with favourable hydrogen bond interactions with the active sites of CTX-M-14. This phytocompound was further selected for a Molecular Dynamic Simulation (MD) study with CTX-M-14, where the complex exhibited good stability and maintained a consistent conformation throughout the simulation. NSC339591 cleared the drug-likeness filters.</p>","PeriodicalId":18990,"journal":{"name":"Natural Product Research","volume":" ","pages":"1-9"},"PeriodicalIF":1.9,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142676299","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Fauzia Anjum, Urvashi Bhardwaj, Sayeed A H Patel, Salesh Kumar Jindal, Ramandeep Kaur, Neena Chawla
{"title":"Portraying phytochemical and genetic components of elite cultivated chilli (<i>Capsicum annuum</i> L.) genotypes.","authors":"Fauzia Anjum, Urvashi Bhardwaj, Sayeed A H Patel, Salesh Kumar Jindal, Ramandeep Kaur, Neena Chawla","doi":"10.1080/14786419.2024.2429129","DOIUrl":"https://doi.org/10.1080/14786419.2024.2429129","url":null,"abstract":"<p><p>Chilli has numerous bioactive components and served since ages in global cuisine and therapeutics. To meet demands of food and various industries, potential genotypes with finest bioactive components is needed. Hence, the objective was to unravel the natural phytochemical variation of 25 chilli genotypes available from the northwestern region of India. The genotypes PT (1.28%), PAU-114 (1.17%) and PL (1.16%) contain high capsaicin, while PL (8.9%), PS (8.2%) and HM-242 (7.8%) have high oleoresin content. PC-431, SB-493 and SM-481 were identified as promising genotypes exhibiting potential antioxidant properties. The correlation matrix depicted a significant association between traits that assist in breeding program. Oleoresin has a negative association with total phenolics. The genetic components revealed less influence of environmental factors and thus improvement through pure line selection method is possible. Phytochemically enriched genotypes can be utilised in diverse areas, <i>viz</i>. nutritional, food processing, therapeutics, cosmetics and in breeding programmes.</p>","PeriodicalId":18990,"journal":{"name":"Natural Product Research","volume":" ","pages":"1-7"},"PeriodicalIF":1.9,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142676453","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Investigating the neuroprotective effects of alkaloids from Galanthus woronowii as a potential treatment for Alzheimer's disease.","authors":"Priyadharsan Arumugam","doi":"10.1080/14786419.2024.2431124","DOIUrl":"https://doi.org/10.1080/14786419.2024.2431124","url":null,"abstract":"","PeriodicalId":18990,"journal":{"name":"Natural Product Research","volume":" ","pages":"1-2"},"PeriodicalIF":1.9,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142676330","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Francisco Paiva Machado, Guilherme Freimann Wermelinger, Alex de Souza Cruz Lopes Canuto, Anna Carolina Carvalho da Fonseca, Diogo Folly, Afonso Thales Sousa Arruda, Leandro Rocha, Bruno Kaufmann Robbs
{"title":"Antitumoral effect thought ROS production of the sesquiterpene lactone centratherin isolated from <i>Eremanthus crotonoides</i>, an endemic plant from Brazil.","authors":"Francisco Paiva Machado, Guilherme Freimann Wermelinger, Alex de Souza Cruz Lopes Canuto, Anna Carolina Carvalho da Fonseca, Diogo Folly, Afonso Thales Sousa Arruda, Leandro Rocha, Bruno Kaufmann Robbs","doi":"10.1080/14786419.2024.2427812","DOIUrl":"https://doi.org/10.1080/14786419.2024.2427812","url":null,"abstract":"<p><p>Cancer is a global public health problem, requiring the development of new and more effective drugs for treatment. <i>Eremanthus crotonoides</i>, is a common plant found in the Brazilian Cerrado and Atlantic Forest and is used as a traditional medicinal plant in some regions. This study evaluated the potential antitumor effect of centratherin, a compound isolated from <i>E. crotonoides</i> leaves, against cancer cells. In colorectal cancer cells, centratherin showed greater toxicity than carboplatin while maintaining comparable selectivity to the control. Although centratherin did not induce classical apoptotic phenotypes and was not inhibited by Zvad, it did induce elevated levels of reactive oxygen species (ROS) that was responsible for cell death explaining its toxicity. <i>in silico</i> analysis, showed that this substance has high oral bioavailability and intestinal absorption. Centratherin was found to be selective against colon cancer cells and, therefore may be considered for future studies on colorectal cancer (CRC) studies.</p>","PeriodicalId":18990,"journal":{"name":"Natural Product Research","volume":" ","pages":"1-8"},"PeriodicalIF":1.9,"publicationDate":"2024-11-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142676389","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Li-Qi Liang, Xian-Hua He, Chun-Yan Wei, Jing-Xian Zhao, Qian Wu, Min Liang, Jun Li, Yan Luo, Wei-Feng Xu, Rui-Yun Yang
{"title":"Antimicrobial polyketides from an endophytic fungus <i>Arcopilus aureus</i> HJ-7 from <i>Ardisia mamillata</i> Hance.","authors":"Li-Qi Liang, Xian-Hua He, Chun-Yan Wei, Jing-Xian Zhao, Qian Wu, Min Liang, Jun Li, Yan Luo, Wei-Feng Xu, Rui-Yun Yang","doi":"10.1080/14786419.2024.2429119","DOIUrl":"10.1080/14786419.2024.2429119","url":null,"abstract":"<p><p>Eleven polyketide derivatives, including two new compounds, xanthoradone D (<b>1</b>) and arisochromophilone (<b>2</b>), were isolated from <i>Arcopilus aureus</i> HJ-7, a Chinese medicinal plant <i>Ardisia mamillata</i> Hance-associated fungus. Their structures were elucidated on the basis of spectroscopic analysis and ECD (Electronic Circular Dichroism) calculations. The antibacterial and antifungal activities of the compounds were evaluated. Compound <b>1</b> showed the significant inhibitory activity against <i>Staphylococcus aureus</i> and <i>Xanthomonas axonopodis pv.</i> citri (Hasse) Dye with the MIC (Minimum Inhibitory Concentration) value of 6.25 μg/mL, and <b>1</b> also showed strong antifungal activities against <i>Cochliobolus miyabeanus</i> and <i>Ceratocystis paradoxa</i> with the MIC value of 3.125 μg/mL.</p>","PeriodicalId":18990,"journal":{"name":"Natural Product Research","volume":" ","pages":"1-8"},"PeriodicalIF":1.9,"publicationDate":"2024-11-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142668262","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}