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Two new prenyl-substituted natural products from the endophytic fungus Talaromyces sp. XSJC-F4. 内生真菌Talaromyces sp. XSJC-F4的两个新戊烯基取代天然产物。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-23 DOI: 10.1080/14786419.2025.2605673
Shangfeng Gao, Yiqing Shi, Haidi Li, Hongping Long, Kangping Xu, Xia Yu

Two new prenyl-substituted natural products, 10-(3'-methyl-2'-butenyl)-9-methylguanine (1) and 12-ketone-colletorin B (2), along with three known prenylated compounds-12-ketone-colletochlorin B (3), colletorin B (4), and colletochlorin B (5)-were isolated from the endophytic fungus Talaromyces sp. XSJC-F4. The structures of isolated compounds were identified by HRESIMS, NMR analysis, and compared with data from the literature. In addition, all compounds were evaluated for their antibacterial activities in vitro. All five compounds (1-5) exhibited good antibacterial activity against Bacillus subtilis with MIC values ranging from 8 to 64 μg/mL.

从内生真菌Talaromyces sp. XSJC-F4中分离到两个新的戊烯基取代天然产物10-(3′-甲基-2′-丁烯基)-9-甲基鸟嘌呤(1)和12-酮-colletorin B(2),以及3个已知的戊烯基化化合物12-酮-colletochlorin B(3)、colletorin B(4)和colletochlorin B(5)。分离得到的化合物通过hresms、NMR分析进行了结构鉴定,并与文献数据进行了比较。此外,对所有化合物的体外抗菌活性进行了评价。5种化合物(1 ~ 5)对枯草芽孢杆菌均表现出良好的抑菌活性,MIC值在8 ~ 64 μg/mL之间。
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引用次数: 0
Cytotoxic effect of a cyclic nonapeptide from Agrostemma githago L. against non-small cell lung carcinoma H460 cells. 藤草环状非肽对非小细胞肺癌H460细胞的细胞毒作用。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-23 DOI: 10.1080/14786419.2025.2598833
Chong Yu, Yun-Xi Yang, Jia-Hang Deng, Yi Yang, Jun Yin, Zhi-Hui Liu

One new cyclic nonapeptide, named agroscyclopeptide A (1), was isolated from Agrostemma githago L. The planar structure of agroscyclopeptide A was determined using spectroscopic techniques and MS analyses. The amino acids absolute configurations were identified by advanced Marfey's method. The potential anti-lung-cancer activity of compound 1 was evaluated using CCK-8 assay, through which its cytotoxic effects on NCl-H460 cells were analysed by assessing cellular viability. The results revealed that the compound 1 exhibited dose-dependent inhibition of NCL-H460 cells with a calculated IC50 value of 4.6  μM, demonstrating efficacy comparable to that of cisplatin under identical experimental condition.

从Agrostemma githago L.中分离到一个新的环状非肽,命名为agroscyclopeptide A(1)。利用波谱技术和质谱分析对其进行了平面结构鉴定。用先进的Marfey法确定了氨基酸的绝对构型。采用CCK-8法评估化合物1的潜在抗肺癌活性,通过评估细胞活力分析化合物1对NCl-H460细胞的细胞毒作用。结果表明,化合物1对NCL-H460细胞具有剂量依赖性的抑制作用,其IC50值为4.6 μM,与顺铂在相同实验条件下的抑制作用相当。
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引用次数: 0
Impact of glycomacropeptide on growth, adhesion, and biofilm formation of the probiotic Lacticaseibacillus rhamnosus GG. 糖大肽对鼠李糖乳杆菌生长、粘附和生物膜形成的影响。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-23 DOI: 10.1080/14786419.2025.2596359
Diana Reyes-Pavón, Mariela Jiménez, Anahí Rodríguez-Campos, Daniel Cervantes-García, Laura Elena Córdova-Dávalos, Julien Deschamps, Romain Briandet, Luis G Bermúdez-Humarán, Eva Salinas

Glycomacropeptide (GMP) is a milk-derived bioactive peptide with demonstrated prebiotic properties. It is composed of a 64-amino acid framework and different carbohydrate molecules, which may serve as carbon sources for beneficial bacteria. Lacticaseibacillus rhamnosus GG (LGG) is a widely used probiotic strain that promotes intestinal barrier function, prevents pathogen colonisation and exerts anti-inflammatory and immunomodulatory activities. In this study, we explored the effect of GMP supplementation to LGG cultures on growth, adhesion and biofilm-forming properties of the bacterium. Prebiotic GMP promoted LGG growth and acidifying activities, mainly under anaerobiosis, without modifying the binding-mucus ability. GMP supplementation also increased LGG-biofilm biomass 3.8- and 3.4-fold under aerobic and anaerobic conditions. Besides, GMP treatment increased LGG-biofilm volume 4.7-fold, thickness by 39% and roughness by 110%. Thus, incorporating GMP into food or nutraceutical formulations might represent a viable strategy to enhance the probiotic efficacy of LGG strain, potentially improving its performance in functional products.

糖宏肽(GMP)是一种乳源性生物活性肽,具有益生元特性。它由64个氨基酸的框架和不同的碳水化合物分子组成,可能是有益菌的碳源。鼠李糖乳杆菌GG (lactoaseibacillus rhamnosus GG, LGG)是一种被广泛应用的益生菌菌株,具有促进肠道屏障功能、阻止病原体定植、发挥抗炎和免疫调节作用。在这项研究中,我们探讨了在LGG培养物中添加GMP对细菌生长、粘附和生物膜形成特性的影响。益生元GMP促进LGG生长和酸化活性,主要是在厌氧条件下,但不改变黏液结合能力。在好氧和厌氧条件下,添加GMP也使lgg生物膜的生物量增加了3.8倍和3.4倍。此外,GMP处理使lgg -生物膜体积增加4.7倍,厚度增加39%,粗糙度增加110%。因此,将GMP纳入食品或营养保健品配方可能是提高LGG菌株益生菌功效的可行策略,有可能提高其在功能性产品中的性能。
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引用次数: 0
Three unusual norlignans with anti-inflammatory from the resin of Styrax tonkinensis (Pierre) Craib ex Hart. 从东洋Styrax tonkinensis (Pierre) crab ex Hart树脂中提取三种具有抗炎作用的去脂素。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-23 DOI: 10.1080/14786419.2025.2605667
Xian-Fei Duan, Chun-Yu Ai, Qin Chen, Wang Feng, Lie-Hua Deng, Zhen-Feng Fang

Three unusual phenylisopentane norlignans, designated styraxolanes A-C (1-3), alongside three known analogues (4-6), were obtained from the Styrax tonkinensis resin. Structural assignment was achieved through comprehensive spectroscopic analysis (IR, HRESIMS, 1D- and 2D-NMR). With IC50 values of 7.51 and 8.99 µM, compounds 3 and 4 correspondingly exhibited significant suppression of nitric oxide (NO) production in LPS-stimulated macrophages. In contrast, compounds 1 and 2 displayed considerably weak activity (IC50 = 23.47 and 24.78 μM, respectively). These results suggest a clear structure-dependent bioactivity. This study expands the chemical diversity of bioactive constituents in Styrax species and provides potential candidates for anti-inflammatory agent development.

从Styrax tonkinensis树脂中获得了三个不寻常的苯异戊烷去脂素,命名为styraxolanes A-C(1-3),以及三个已知的类似物(4-6)。通过全面的光谱分析(IR, hresms, 1D-和2D-NMR)实现了结构分配。化合物3和化合物4的IC50值分别为7.51和8.99µM,对lps刺激的巨噬细胞产生一氧化氮(NO)有显著抑制作用。化合物1和2的IC50分别为23.47 μM和24.78 μM,活性较弱。这些结果表明其具有明显的结构依赖性生物活性。该研究扩大了Styrax物种生物活性成分的化学多样性,并为抗炎药的开发提供了潜在的候选药物。
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引用次数: 0
Four new glycoside compounds from Sinapis alba L. and their cytotoxic activity. 白刺中4个新的苷类化合物及其细胞毒活性研究。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-23 DOI: 10.1080/14786419.2025.2602196
Degang Kong, Xinyu Shi, Linlin Ni, Xiaoni Kong, Meichao Cai, Honglei Zhou, Xiaoyu Wang

Four novel compounds, 4-hydroxybenzyl-7-S-β-glucopyranoside (1), 4-hydroxybenzyl-7-S-S-β-glucopyranoside (2), 1-S-(4'-hydroxybenzyl)-6-(4''-hydroxybenzoyl)-β-glucopyranoside (3), and 1-O-(4'-hydroxybenzoyl)-2-O-Z-sinapoyl-β-glucopyranoside (4) were used to isolate from Sinapis alba L. seeds. The structures were accomplished through spectroscopic analysis (NMR and MS) corroborated by chemical studies. Three human cancer cell lines were employed to detect the cytotoxic effects of the compounds.

从白sinapba种子中分离得到4-羟基苯基-7- s -β-葡萄糖苷(1)、4-羟基苯基-7- s -s -β-葡萄糖苷(2)、1- s -(4′-羟基苯基)-6-(4′-羟基苯基)-β-葡萄糖苷(3)和1- o -(4′-羟基苯基)-2- o - z -sinapoyl-β-葡萄糖苷(4)四个新化合物。结构是通过光谱分析(核磁共振和质谱)完成的,并得到了化学研究的证实。采用三种人类癌细胞系检测化合物的细胞毒性作用。
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引用次数: 0
Unveiling the pharmacological potential of Ophiorrhiza radicans Gardner ex Thwaites: first report on its antioxidant, anti-inflammatory, antidiabetic, and cytotoxic activities. 揭示蛇根根的药理潜力:首次报道其抗氧化、抗炎、抗糖尿病和细胞毒性活性。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-23 DOI: 10.1080/14786419.2025.2605669
Jinu Mathew, Majid Sharifi-Rad, Krishnaraj M V, Mity Thambi

Ophiorrhiza species are traditionally used to treat inflammation, pain, wounds, and snake bites due to their bioactive compounds; however, Ophiorrhiza radicans Gardner ex Thwaites, from the Western Ghats, remains underexplored. This study analysed extracts of hexane, chloroform, ethyl acetate, ethanol, and methanol for their antioxidant, anti-inflammatory, antidiabetic, and cytotoxic activities. The ethanol extract showed the highest saponins (0.7404 µg/mL), tannins (0.619 mg/mL), and lignin (14.13%) content, and potent antioxidant activity (ABTS IC50 = 6.962 µg/mL; FRAP value = 43.84 mg Trolox equivalents/gdw). The ethyl acetate extract was richest in terpenoids (0.512 mg/mL) and showed the strongest α-amylase (IC50 = 1.39 ± 0.021 µg/mL) and α-glucosidase (IC50 = 0.30 ± 0.028 µg/mL) inhibition. The chloroform extract, rich in quinone (0.485 µg/mL), showed significant anti-inflammatory activity (IC50 = 0.39 ± 0.012 µg/mL). The methanol extract had the highest glycoside(0.8230 µg/mL) and coumarin (0.9390 µg/mL) content and was non-toxic to HepG2 cells (IC50 of 38.91 µg/mL).

由于其生物活性化合物,传统上用于治疗炎症、疼痛、伤口和蛇咬伤;然而,来自西高止山脉的蛇根草(Ophiorrhiza radicans Gardner ex Thwaites)仍未被充分发掘。本研究分析了己烷、氯仿、乙酸乙酯、乙醇和甲醇提取物的抗氧化、抗炎、抗糖尿病和细胞毒活性。乙醇提取物皂苷含量最高(0.7404µg/mL),单宁含量最高(0.619 mg/mL),木质素含量最高(14.13%),具有较强的抗氧化活性(ABTS IC50 = 6.962µg/mL, FRAP值= 43.84 mg Trolox equivalents/gdw)。乙酸乙酯提取物中萜类化合物含量最高(0.512 mg/mL),对α-淀粉酶(IC50 = 1.39±0.021µg/mL)和α-葡萄糖苷酶(IC50 = 0.30±0.028µg/mL)的抑制作用最强。氯仿提取物含有丰富的醌(0.485µg/mL),具有显著的抗炎活性(IC50 = 0.39±0.012µg/mL)。甲醇提取物中糖苷含量最高(0.8230µg/mL),香豆素含量最高(0.9390µg/mL),对HepG2细胞无毒(IC50为38.91µg/mL)。
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引用次数: 0
A novel plastocyanin-like protein from Strobilanthes schomburgkii (Craib) J.R.I.Wood leaves: isolation and anti-inflammatory activity through MAPK signalling. 一种新的从石南花(Strobilanthes schomburgkii, Craib)木材叶片中提取的质体青素样蛋白:通过MAPK信号的分离和抗炎活性。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-23 DOI: 10.1080/14786419.2025.2605672
Hoai Bac Vo, Thi Thu Hong Le, Tat Cuong Trinh, Yaroslav Andreev, Van Truong Le, Ba Trung Ngo, Thi Bich Thuy Ly, Andreas Koschella

Strobilanthes schomburgkii (Craib) J.R.I. Wood, a member of the Acanthaceae family, is a traditional medicinal plant with a wide range of therapeutic uses. Extracts of this plant have been employed for wound healing, as well as to treat and prevent various diseases, including inflammation, acute and chronic colitis, digestive disorders, bloating, diarrhoea, hemostasis, and cancer. In this study, plastocyanin-like protein (SSW) from the leaves of S. schomburgkii was isolated and evaluated for its anti-inflammatory activity. The SSW protein showed an approximate molecular mass of 15 kDa according to Tricine-SDS-PAGE. N-terminal sequence of the protein (FEVLMGSDVGELVFXP) shared 70-80% similarity with plastocyanin-like proteins from plants. Our results suggest that SSW represents a novel member of the plastocyanin-like protein family. SSW inhibited bovine serum albumin (BSA) denaturation with an IC50 of 0.399 mg/mL, exhibiting activity similar to diclofenac, a non-steroidal anti-inflammatory drug. At a concentration of 40 µg/mL, the SSW did not exhibit any cytotoxic effects and suppressed cytokine production on macrophages in vitro as effectively as dexamethasone. A strong anti-inflammatory activity of SSW (40 µg/mL) was associated with inhibition of mitogen-activated protein kinase (MAPK) signalling pathways in macrophages, that lead to the significant decrease of the extracellular signal-regulated kinase (P-ERK) and p38 phosphorylation. Therefore anti-inflammatory properties of S. schomburgkii leaves, revealed by Vietnam folk medicine, are at least partially mediated by plastocyanin-like protein of this plant.

Strobilanthes schomburgkii (Craib) J.R.I. Wood是棘科植物,是一种具有广泛治疗用途的传统药用植物。这种植物的提取物已被用于伤口愈合,以及治疗和预防各种疾病,包括炎症、急性和慢性结肠炎、消化系统紊乱、腹胀、腹泻、止血和癌症。本研究从schomburgkii叶片中分离得到了质体青素样蛋白(plasocyanin -like protein, SSW),并对其抗炎活性进行了评价。根据Tricine-SDS-PAGE, SSW蛋白的分子量约为15 kDa。该蛋白的n端序列(FEVLMGSDVGELVFXP)与来自植物的质体青素样蛋白具有70-80%的相似性。我们的研究结果表明,SSW代表了质体青素样蛋白家族的一个新成员。SSW抑制牛血清白蛋白(BSA)变性的IC50为0.399 mg/mL,其活性与非甾体抗炎药双氯芬酸相似。在浓度为40 μ g/mL时,SSW没有表现出任何细胞毒作用,并且在体外与地塞米松一样有效地抑制巨噬细胞的细胞因子产生。SSW的强抗炎活性(40µg/mL)与巨噬细胞中丝裂原活化蛋白激酶(MAPK)信号通路的抑制相关,导致细胞外信号调节激酶(P-ERK)和p38磷酸化的显著降低。因此,越南民间医学所揭示的schomburgkii叶片的抗炎特性,至少部分是由该植物的质体青素样蛋白介导的。
{"title":"A novel plastocyanin-like protein from <i>Strobilanthes schomburgkii</i> (Craib) J.R.I.Wood leaves: isolation and anti-inflammatory activity through MAPK signalling.","authors":"Hoai Bac Vo, Thi Thu Hong Le, Tat Cuong Trinh, Yaroslav Andreev, Van Truong Le, Ba Trung Ngo, Thi Bich Thuy Ly, Andreas Koschella","doi":"10.1080/14786419.2025.2605672","DOIUrl":"https://doi.org/10.1080/14786419.2025.2605672","url":null,"abstract":"<p><p><i>Strobilanthes schomburgkii</i> (Craib) J.R.I. Wood, a member of the Acanthaceae family, is a traditional medicinal plant with a wide range of therapeutic uses. Extracts of this plant have been employed for wound healing, as well as to treat and prevent various diseases, including inflammation, acute and chronic colitis, digestive disorders, bloating, diarrhoea, hemostasis, and cancer. In this study, plastocyanin-like protein (<b>SSW</b>) from the leaves of <i>S. schomburgkii</i> was isolated and evaluated for its anti-inflammatory activity. The <b>SSW</b> protein showed an approximate molecular mass of 15 kDa according to Tricine-SDS-PAGE. N-terminal sequence of the protein (<b>FEVLMGSDVGELVFXP</b>) shared 70-80% similarity with plastocyanin-like proteins from plants. Our results suggest that <b>SSW</b> represents a novel member of the plastocyanin-like protein family. <b>SSW</b> inhibited bovine serum albumin (BSA) denaturation with an IC<sub>50</sub> of 0.399 mg/mL, exhibiting activity similar to diclofenac, a non-steroidal anti-inflammatory drug. At a concentration of 40 µg/mL, the <b>SSW</b> did not exhibit any cytotoxic effects and suppressed cytokine production on macrophages <i>in vitro</i> as effectively as dexamethasone. A strong anti-inflammatory activity of <b>SSW (</b>40 µg/mL) was associated with inhibition of mitogen-activated protein kinase (MAPK) signalling pathways in macrophages, that lead to the significant decrease of the extracellular signal-regulated kinase (P-ERK) and p38 phosphorylation. Therefore anti-inflammatory properties of <i>S. schomburgkii</i> leaves, revealed by Vietnam folk medicine, are at least partially mediated by plastocyanin-like protein of this plant.</p>","PeriodicalId":18990,"journal":{"name":"Natural Product Research","volume":" ","pages":"1-8"},"PeriodicalIF":1.6,"publicationDate":"2025-12-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145820395","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}
引用次数: 0
Pioneering study on phytochemical, nutritional, antioxidant, and antidiabetic potential of Xanthosoma brasiliense (Desf.) Engl.: a key plant species from Kerala, India. 巴西黄病菌(Xanthosoma brasiliense, Desf.)植物化学、营养、抗氧化和抗糖尿病潜能的开创性研究心血管病。:一种来自印度喀拉拉邦的重要植物。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-22 DOI: 10.1080/14786419.2025.2602915
Parvathy Chandran, J Lohidas

Xanthosoma brasiliense (Desf.) Engl. (Araceae) is a leafy vegetable with nutritional and therapeutic potential. This study evaluated its nutritional composition, phytochemicals, High-Performance Liquid Chromatography (HPLC) profile, antioxidant, and antidiabetic activity. Proximate analysis showed carbohydrate 0.41 ± 0.01 mg glucose equivalents per gram dry weight (mg glucose Eq./g DW), protein 0.55 ± 0.02 mg bovine serum albumin equivalents per gram dry weight (mg BSA Eq./g DW), fibre 12.0 ± 0.4 mg/g DW, fat 0.16 ± 0.01% DW, ash 12.3 ± 0.4% DW, and moisture 62.0 ± 1.1% fresh weight. HPLC identified gallic, caffeic, rutin, quercetin, and ferulic acid. Antioxidant assays showed half-maximal inhibitory concentration (IC50) of 1.818 mg/mL for 2,2-diphenyl-1-picrylhydrazyl (DPPH), 0.506 mg/mL for 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and Ferric Reducing Antioxidant Power (FRAP) of 41.21 μg Trolox equivalents per gram dry weight (μg TE/g DW).α-Amylase (IC50 = 0.979 mg/mL) and α-glucosidase (IC50 = 1.904 mg/mL) inhibition matched acarbose, confirming antidiabetic potential.

巴西黄病菌心血管病。天南星科植物是一种具有营养和治疗价值的多叶蔬菜。本研究评估了其营养成分、植物化学成分、高效液相色谱(HPLC)分析、抗氧化和抗糖尿病活性。碳水化合物每克干重0.41±0.01 mg葡萄糖当量(mg葡萄糖当量/g DW),蛋白质每克干重0.55±0.02 mg牛血清白蛋白当量(mg BSA当量/g DW),纤维12.0±0.4 mg/g DW,脂肪0.16±0.01% DW,灰分12.3±0.4% DW,水分62.0±1.1%鲜重。HPLC鉴定没食子、咖啡、芦丁、槲皮素和阿魏酸。抗氧化实验显示,2,2-二苯基-1-吡啶肼(DPPH)的半最大抑制浓度(IC50)为1.818 mg/mL, 2,2'-氮基-二(3-乙基苯并噻唑-6-磺酸)(ABTS)的半最大抑制浓度(IC50)为0.506 mg/mL,铁还原抗氧化能力(FRAP)为41.21 μg Trolox当量/克干重(μg TE/g DW)。α-淀粉酶(IC50 = 0.979 mg/mL)和α-葡萄糖苷酶(IC50 = 1.904 mg/mL)抑制作用与阿卡波糖匹配,证实了降糖潜力。
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引用次数: 0
Valorisation of mediterranean basin fruit by-products: bioactive composition, applications, and future research directions. 地中海盆地水果副产品的增值:生物活性成分、应用和未来的研究方向。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-21 DOI: 10.1080/14786419.2025.2602197
Diana Vanacore, Sara Beltrami, Antonella Gori, Francesca Alderotti, Ermes Lo Piccolo, Cassandra Detti, Andrea Baptista, Francesco Ferrini, Cecilia Brunetti

Peels, seeds, shells, cores and pomace are major by-products of fruit processing, whose improper disposal poses critical environmental and economic challenges. Currently, there is a growing need to find strategies for recycling and valorising these by-products, now recognised as valuable sources of bioactive compounds for nutraceutical, cosmetic and agrochemical applications. This review explores the by-products of the most important Mediterranean fruits and nuts, examining their bioactive composition and potential applications to identify understudied matrices and compounds, thus determining research gaps and priorities for their valorisation. Among waste matrices, pome cores, stone fruit pomace, seeds and internal layers of citrus, pomegranate pulp, and nut shells and skins were the most overlooked. Furthermore, some classes of phytochemicals, including phytosterols of stone fruits and triterpenes of pomes, emerged as the least investigated. This evidence underscores the need for targeted research to address knowledge gaps and fully leverage the functional potential of these by-products.

果皮、种子、果壳、果核和果渣是水果加工的主要副产品,它们的不当处理给环境和经济带来了严峻的挑战。目前,越来越需要找到回收和估价这些副产品的策略,这些副产品现在被认为是营养品、化妆品和农用化学品应用的生物活性化合物的宝贵来源。这篇综述探讨了最重要的地中海水果和坚果的副产品,研究了它们的生物活性成分和潜在的应用,以识别未被充分研究的基质和化合物,从而确定研究空白和优先事项。在废弃物基质中,最容易被忽视的是梨核、核果渣、柑橘种子和内层、石榴果肉、坚果壳和果皮。此外,某些种类的植物化学物质,包括核果中的植物甾醇和石榴树中的三萜,是研究最少的。这一证据强调需要进行有针对性的研究,以解决知识差距并充分利用这些副产品的功能潜力。
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引用次数: 0
Synthetic derivatives of gibberellin A3 with selective antiproliferative activity against human renal carcinoma 786-O cells. 对人肾癌786-O细胞具有选择性抗增殖活性的赤霉素A3衍生物的合成。
IF 1.6 3区 化学 Q3 CHEMISTRY, APPLIED Pub Date : 2025-12-21 DOI: 10.1080/14786419.2025.2600509
Jia-Hao Pang, Ke Wang, Xiao-Ping Peng, Gang Li

Gibberellin A3 (GA3, 1), a well-known member of the ent-kaurene tetracyclic diterpenoid family, exhibits diverse bioactivities. It serves as a lead compound in medicinal chemistry. In this study, inspired by the chemical structure of anticancer vorinostat and the bioactive α,β-unsaturated ketone unit in gibberellins, five new GA3-based derivatives (2-6) were designed and synthesised. Their antiproliferative activity against five cancer cells was evaluated. Compound 4 and 5 with a ketone group at C-3 exhibited selective cytotoxicity against human renal carcinoma 786-O cells. Specifically, compound 4 displayed the most potent antiproliferative effect on 786-O cells with an IC50 value of 12.93 μM.

赤霉素A3 (giberellin A3, GA3, 1)是一种众所周知的对烯四环二萜家族成员,具有多种生物活性。它在药物化学中充当先导化合物。本研究以抗癌伏立诺他的化学结构和赤霉素中具有生物活性的α,β-不饱和酮单元为灵感,设计并合成了5个新的ga3衍生物(2-6)。评价了它们对5种癌细胞的抗增殖活性。化合物4和5在C-3上具有酮基,对人肾癌786-O细胞具有选择性细胞毒性。其中,化合物4对786-O细胞的抑制作用最强,IC50值为12.93 μM。
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引用次数: 0
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Natural Product Research
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