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Colchicine, serotobenine, and kinobeon A: novel therapeutic compounds in Carthamus tinctorius L. for the management of diabetes 秋水仙碱、蛇床子碱和金诺贝酮 A:用于治疗糖尿病的新型荠菜治疗化合物
IF 2.3 3区 农林科学 Q3 FOOD SCIENCE & TECHNOLOGY Pub Date : 2024-09-27 DOI: 10.1186/s13765-024-00939-x
Samina Hanif, Zainab Shahzadi, Irfan Anjum, Zubaida Yousaf, Arusa Aftab, Sana Javed, Zainab Maqboo, Riaz Ullah, Zafar Iqbal, Muhammad Ahmer Raza

Diabetes, a global health concern, poses increasing mortality risks. The pathogenesis of diabetes involves multiple mechanisms, with oxidative stress being one of the key contributors. As synthetic drugs have various side effects, which can be minimized by using herbal plants. This study focuses on the In vitro antioxidant potential, α-amylase inhibition potential, identification of bioactive compounds, and hub genes in diabetes treatment mechanism by using C. tinctorius Extraction of C. tinctorious lead and flower was performed using different solvents (Distilled water, methanol, chloroform, and Dimethyl ether). After extraction different concentrations range from 25–200 mg/mL) was made and checked against activities. The antioxidant potential was assessed using 2, 2-diphenyl-1-picrylhydrazyl (DPPH), total phenolic contents (TPC), and total antioxidant capacity (TAC) assays, while antidiabetic activity was evaluated through α-amylase inhibition assay. Phytochemicals was identified by GC–MS analysis, followed by ADMET screening and network pharmacology analysis using Swiss Target Prediction, Gene Card, DesGeNet, DAVID, STRING, Cytoscape, and drug revitalization databases. Results revealed positive correlations with DPPH, TAC, and TPC. Methanol extract exhibited the highest inhibitory concentration. Screening of 46 compounds was performed by studying their pharmacokinetic properties which revealed 9 compounds effective against 204 diabetes targets. Moreover, their network analysis identified four hub genes, including AKT1, JUN, EGFR, and MMP9. These genes found highly associated with drugs like Colchicine and Serotobenine. Revitalization analysis also highlighted four genes (EGFR, PTGS2, AKT1, and MMP9) strongly correlated with FDA-approved drugs. The study suggests C. tinctorius methanol extract is a potential source for novel drugs.

Graphical Abstract

糖尿病是全球关注的健康问题,其造成的死亡风险与日俱增。糖尿病的发病机制涉及多个方面,氧化应激是其中一个重要因素。由于合成药物有各种副作用,使用草本植物可将副作用降至最低。本研究的重点是利用洋二仙草对体外抗氧化潜力、α-淀粉酶抑制潜力、生物活性化合物的鉴定以及糖尿病治疗机制中的枢纽基因进行研究。萃取后制成不同浓度(25-200 毫克/毫升)的产品,并检查其活性。抗氧化潜力采用 2,2-二苯基-1-苦基肼(DPPH)、总酚含量(TPC)和总抗氧化能力(TAC)测定法进行评估,抗糖尿病活性则通过α-淀粉酶抑制测定法进行评估。通过气相色谱-质谱分析鉴定了植物化学成分,然后利用瑞士靶点预测、Gene Card、DesGeNet、DAVID、STRING、Cytoscape 和药物振兴数据库进行了 ADMET 筛选和网络药理学分析。结果表明,它们与 DPPH、TAC 和 TPC 呈正相关。甲醇提取物的抑制浓度最高。通过研究 46 种化合物的药代动力学特性对其进行了筛选,结果发现 9 种化合物对 204 个糖尿病靶点有效。此外,他们还通过网络分析发现了四个枢纽基因,包括 AKT1、JUN、表皮生长因子受体和 MMP9。这些基因与秋水仙碱和丝裂霉素等药物高度相关。活化分析还强调了四个基因(表皮生长因子受体、PTGS2、AKT1 和 MMP9)与 FDA 批准的药物密切相关。研究表明,洋二仙草甲醇提取物是新型药物的潜在来源。
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引用次数: 0
Correction: Inhibitory effect of human indoleamine 2,3-dioxygenase 1 (hIDO1) by kazinols of 1,3-diphenylpropane derivatives 更正:1,3-二苯基丙烷衍生物嗪醇对人类吲哚胺 2,3-二氧合酶 1 (hIDO1) 的抑制作用
IF 2.3 3区 农林科学 Q3 FOOD SCIENCE & TECHNOLOGY Pub Date : 2024-09-27 DOI: 10.1186/s13765-024-00943-1
Taehoon Oh, Sunin Jung, Seon Min Oh, Mi Hyeon Park, Hyoung-Geun Kim, Su-Yeon Lee, Sung-Kyun Ko, Hyung Won Ryu
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引用次数: 0
Phytochemical composition and green insecticides from Citrus aurantifolia fruit peels against whitefly, Bemisia tabaci 枳壳果皮中的植物化学成分和绿色杀虫剂对粉虱(Bemisia tabaci)的防治作用
IF 2.3 3区 农林科学 Q3 FOOD SCIENCE & TECHNOLOGY Pub Date : 2024-09-23 DOI: 10.1186/s13765-024-00916-4
Mariam S. El-Alfy, Mohamed E. Mostafa, Abelaziz M. Dawidar, Mamdouh Abdel-Mogib

Insecticidal potential of extracts of Citrus aurantifolia, family Rutaceae, was evaluated to control whiteflies, Bemisia tabaci. Biocidal activity directed chromatographic separation of chloroform and butanol fractions, with spectral identification (1D-NMR, 2D-NMR, ESIMS) of the active fractions have been resulted in separation and structural elucidation of for previously described coumarins (bergapten 1, limettin 2, isopimpinellin 3, oxypeucedanin hydrate 4) in addition to a new dimeric coumarin (12R, 12’R)-aurantifolin 5, two known limonoids; 21,23-dihydro-23-methoxy-21-oxolimonin 6, 21,23-dihydro-23-methoxy-21-oxonomilin 7, and two known flavonoid glycosides; scoparin 8, and narcissin 9. Amongst these compounds, narcissin 9 was the most effective after 24 h. of treatment while, (12R, 12’R)-aurantifolin 5 was the most potent against B. tabaci, 3rd instar nymphs after 72 h. of treatment and under laboratory conditions, with LC50 values of 33.31and 15.92 ppm, respectively comparing with the positive control azadirachtin.

评估了芸香科柑橘属植物枳的提取物在控制烟粉虱方面的杀虫潜力。通过对氯仿和丁醇馏分进行杀虫活性定向色谱分离,并对活性馏分进行光谱鉴定(1D-NMR、2D-NMR、ESIMS),除了一种新的二聚香豆素(12R、12'R)-aurantifolin 5 外,还分离并阐明了以前描述的香豆素(bergapten 1、limettin 2、isopimpinellin 3、oxypeucedanin hydrate 4)和两种已知的柠檬醛类化合物的结构;21,23-二氢-23-甲氧基-21-oxolimonin 6、21,23-二氢-23-甲氧基-21-oxonomilin 7,以及两种已知的黄酮苷:莨菪苷 8 和水仙苷 9。在这些化合物中,水仙素 9 在处理 24 小时后效果最好,而(12R, 12'R)-aurantifolin 5 在处理 72 小时后,在实验室条件下,与阳性对照阿扎菌素相比,对塔巴氏线虫第三龄若虫的半数致死浓度分别为 33.31 和 15.92 ppm。
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引用次数: 0
Preparation of chitosan oligosaccharides from chitosan of tenebrio molitor and its prebiotic activity 甲壳素寡糖的制备及其益生元活性
IF 2.3 3区 农林科学 Q3 FOOD SCIENCE & TECHNOLOGY Pub Date : 2024-09-18 DOI: 10.1186/s13765-024-00937-z
Hyemi Kim, Ga Yeong Cheon, Jae Hee Kim, Ra-Yeong Choi, In-Woo Kim, Hyung Joo Suh, Ki-Bae Hong, Sung Hee Han

This study aimed to establish the optimal production conditions for mealworm chitosan oligosaccharides (MCOS) using the response surface methodology and measure the prebiotic effect of MCOS prepared on cecal microbiota through in vitro anaerobic fermentation. The optimal conditions for MCOS production using chitosanase were 2.5% substrate, 30 mg/g enzyme, and 6 h reaction time. Matrix-assisted laser desorption ionization-time of flight mass spectrometry, Fourier transform infrared spectroscopy, and in vitro assays to confirm that the chemical structure and physicochemical properties of MCOS are similar to those of commercially available chitosan oligosaccharides. The growth of Lactobacillus acidophilus, Lacticaseibacillus casei, and Bifidobacterium bifidum was increased by MOCS and confirmed that the prebiotic effect of MCOS was significant in a concentration-dependent manner. The addition of 1% and 2% MCOS to in vitro anaerobic fermentation resulted in changes in the content of short-chain fatty acids (SCFAs) and an increase in Verrucomicrobiota abundance compared with the control. In the case of Romboutsia, Turicibacter, and Akkermansia, a significant increase was confirmed in the MCOS-containing groups compared to that in the control group. Compared to 2% MCOS, 1% MCOS more significantly affected Lactobacillus levels. MCOS produced by chitosanase under optimal conditions contains oligosaccharides with 2–6 degree of polymerization and exerts a prebiotic effect that affects changes in the SCFA content and microbiota composition in the cecum.

本研究旨在利用响应面方法确定黄粉虫壳聚糖寡糖(MCOS)的最佳生产条件,并通过体外厌氧发酵测定制备的 MCOS 对盲肠微生物群的益生作用。使用壳聚糖酶生产 MCOS 的最佳条件是 2.5% 的底物、30 mg/g 的酶和 6 小时的反应时间。基质辅助激光解吸电离飞行时间质谱法、傅立叶变换红外光谱法和体外试验证实 MCOS 的化学结构和理化性质与市售壳聚糖低聚物相似。MOCS 增加了嗜酸乳杆菌、酪酸乳杆菌和双歧杆菌的生长,并证实 MCOS 的益生效应显著,且呈浓度依赖性。与对照组相比,在体外厌氧发酵中添加 1%和 2%的 MCOS 会导致短链脂肪酸(SCFAs)含量的变化和 Verrucomicrobiota 丰度的增加。与对照组相比,含 MCOS 组的 Romboutsia、Toricibacter 和 Akkermansia 的数量显著增加。与 2% 的 MCOS 相比,1% 的 MCOS 对乳酸菌水平的影响更为明显。壳聚糖酶在最佳条件下产生的 MCOS 含有聚合度为 2-6 的低聚糖,具有益生作用,可影响盲肠中 SCFA 含量和微生物群组成的变化。
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引用次数: 0
Effects of high solid content and straw proportion on volatile fatty acids production from straw, sludge and food wastes: performance and microbial community characteristics 高固体含量和秸秆比例对从秸秆、污泥和食物垃圾中产生挥发性脂肪酸的影响:性能和微生物群落特征
IF 2.3 3区 农林科学 Q3 FOOD SCIENCE & TECHNOLOGY Pub Date : 2024-09-17 DOI: 10.1186/s13765-024-00935-1
Yu-Wei Chen, Gao Feng, Xia Hong, Meng Wang, Quan Zhang, Zhao-Yong Sun, Ya-Ting Chen, Yue-Qin Tang

Anaerobic digestion (AD) is an efficient technology for treating organic solid wastes, and the volatile fatty acids (VFAs) produced during AD have significant value due to their wide range of applications and higher added value compared to methane. This study investigated the long-term effects of high solid content and straw proportion in mixed substrates (straw, sludge, and food wastes) on VFAs production through semi-continuous reactors under thermophilic and mesophilic conditions. Results showed that both reactors achieved a maximum VFAs concentration of ~ 22 g/L as the straw proportion increased to 50%. Acetate (48.3 – 64.5%) was the main component of produced VFAs in both reactors, while butyrate and propionate production in thermophilic temperature were superior compared to mesophilic conditions. Microbial community analysis revealed that Defluviitoga plays a pivotal role in acidogenesis within both reactors; besides, unclassified Hungateiclostridiaceae and Caproiciproducen were found to be dominant in thermophilic reactor, while Lachnospiraceae_NK3A20_group and Rikenellaceae_RC9_gut_group were essential for VFAs production under mesophilic conditions. These findings provide valuable insights for the biotechnological exploration of acidogenic fermentation for large-scale mechanized production of VFAs from agricultural wastes.

厌氧消化(AD)是一种处理有机固体废物的高效技术,在厌氧消化过程中产生的挥发性脂肪酸(VFAs)具有广泛的应用价值,而且与甲烷相比具有更高的附加值。本研究调查了在嗜热和中嗜热条件下,通过半连续反应器处理混合基质(秸秆、污泥和食物垃圾)时,高固体含量和秸秆比例对挥发性脂肪酸产量的长期影响。结果表明,当秸秆比例增加到 50%时,两种反应器的最大 VFAs 浓度都达到了约 22 克/升。乙酸盐(48.3%-64.5%)是两种反应器产生的 VFAs 的主要成分,而嗜热条件下的丁酸盐和丙酸盐产量比中嗜热条件下高。微生物群落分析表明,Defluviitoga 在两个反应器的产酸过程中都起着关键作用;此外,未分类的 Hungateiclostridiaceae 和 Caproiciproducen 在嗜热反应器中占优势,而 Lachnospiraceae_NK3A20_group 和 Rikenellaceae_RC9_gut_group 在中嗜热条件下对 VFAs 的产生至关重要。这些发现为从农业废弃物中大规模机械化生产 VFAs 的产酸发酵生物技术探索提供了宝贵的启示。
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引用次数: 0
AI-guided investigation of biochar’s efficacy in Pb immobilization for remediation of Pb contaminated agricultural land 以人工智能为指导,研究生物炭在固定铅以修复受铅污染的农田方面的功效
IF 2.3 3区 农林科学 Q3 FOOD SCIENCE & TECHNOLOGY Pub Date : 2024-09-16 DOI: 10.1186/s13765-024-00933-3
Yoora Cho, Juin Yau Lim, Avanthi Deshani Igalavithana, Geonwook Hwang, Mee Kyung Sang, Ondřej Mašek, Yong Sik Ok

This study evaluated the lead (Pb) immobilization efficiency of biochar in contaminated agricultural soil. The biochar was produced from a range of major biomass residues and pyrolyzed under well-controlled conditions. Ten different types of standard biochar samples were derived from five different feedstocks (i.e., softwood, miscanthus straw, rice husk, oilseed rape straw, wheat straw) and pyrolyzed at 550 ℃ and 700 ℃. Pb-contaminated soil near an abandoned mine was incubated with 2.5% (w w− 1) of biochar. Incubation was conducted for various durations at room temperature under both short-term (21 days) and long-term (214 days) conditions. This variation explicitly accounted for the simulated microplastic contamination during the long-term incubation period. A novel framework has been developed to predict the long-term immobilization effect of various biochar types using a machine-learning approach, following the successful identification of optimal biochar implementations. This prediction method utilizes a small on-field dataset by employing a data augmentation approach, showcasing an innovative approach to forecasting the effects of different biochar types over time. After the incubation period, soil samples were analyzed for their chemical properties. As a result, oil seed rape biochar was the highest in pH, EC, exchangeable Ca2+, Mg2+, and K+, total nitrogen content, soil organic matter content, and available phosphate. In return, OSR 700 treated soils showed the highest content of exchangeable cations and the lowest content of available Pb after the incubation period. The most efficient biochar for immobilizing lead (Pb) in soil appears to be OSR 700, based on the available evidence.

本研究评估了生物炭在受污染农业土壤中的铅固定效率。生物炭由一系列主要生物质残留物制成,并在控制良好的条件下进行热解。从五种不同的原料(即软木、马齿苋秸秆、稻壳、油菜秸秆和小麦秸秆)中提取了十种不同类型的标准生物炭样品,并在 550 ℃ 和 700 ℃ 下进行热解。在废弃矿山附近受铅污染的土壤中加入 2.5%(体积分数-1)的生物炭进行培养。在室温下,在短期(21 天)和长期(214 天)条件下进行了不同持续时间的培养。这种变化明确考虑了长期培养期间的模拟微塑料污染。在成功确定最佳生物炭实施方案后,开发了一个新的框架,利用机器学习方法预测各种生物炭类型的长期固定效果。这种预测方法通过采用数据增强方法,利用了一个小型现场数据集,展示了一种预测不同生物炭类型随时间变化的效果的创新方法。培养期结束后,对土壤样本进行了化学特性分析。结果显示,油菜生物炭的 pH 值、EC 值、可交换 Ca2+、Mg2+ 和 K+、全氮含量、土壤有机质含量和可利用磷酸盐含量最高。反过来,经 OSR 700 处理的土壤在培养期后显示出最高的可交换阳离子含量和最低的可利用铅含量。根据现有证据,OSR 700 似乎是土壤中固定铅(Pb)最有效的生物炭。
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引用次数: 0
Optimization of fermentation conditions, physicochemical profile and sensory quality analysis of seedless wampee wine 优化无籽芒皮酒的发酵条件、理化特征和感官质量分析
IF 2.3 3区 农林科学 Q3 FOOD SCIENCE & TECHNOLOGY Pub Date : 2024-09-13 DOI: 10.1186/s13765-024-00938-y
Hong Wang, Xiang Liao, Chunyao Lin, Weidong Bai, Gengsheng Xiao, Xingyuan Huang, Gongliang Liu

The aims of the present stud were to optimize fermentation parameters of seedless wampee wine using response surface methodology (RSM) and evaluate the changes in flavor metabolites during fermentation. Seedless wampee wine of optimal sensory quality was produced using an inoculum concentration of 0.6%, initial sugar levels of 200 g/L, a fermentation temperature of 22 °C, and a fermentation period of 9 days. Then the flavor compound profiles (amino acids, organic acids and volatile aroma compounds) of seedless wampee wine during the fermentation under optimal conditions were analyzed using high performance liquid chromatography (HPLC) and gas chromatography–mass spectrometr (GC-MS). The main fermented phase of fermentation resulted in fluctuations in both total amino acids and organic acids, with stabilization occurring later on. A total of 54 volatile components, including esters, alcohols, terpenes, and acids, were putatively identified. Terpenes were the primary drivers of the flavor characteristics of seedless wampee. The rise of esters and decline of terpenes have the potential to significantly alter the flavor of wine during fermentation. These results would contribute to the further development of seedless wampee wine.

Graphical Abstract

本研究的目的是利用响应面方法(RSM)优化无籽黄皮酒的发酵参数,并评估发酵过程中风味代谢物的变化。在接种物浓度为 0.6%、初始糖度为 200 克/升、发酵温度为 22 °C、发酵期为 9 天的条件下,生产出感官质量最佳的无籽芒皮酒。然后用高效液相色谱法(HPLC)和气相色谱-质谱法(GC-MS)分析了无籽芒皮酒在最佳条件下发酵过程中的风味化合物特征(氨基酸、有机酸和挥发性芳香化合物)。发酵的主要发酵阶段导致氨基酸总量和有机酸总量波动,随后趋于稳定。共鉴定出 54 种挥发性成分,包括酯类、醇类、萜烯类和酸类。萜烯类化合物是无籽黄皮风味特征的主要驱动因素。酯类的增加和萜烯类的减少有可能在发酵过程中显著改变葡萄酒的风味。这些结果将有助于无籽芒皮酒的进一步发展。
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引用次数: 0
Characterization of acidogenic phase metabolism in Clostridium acetobutylicum ATCC 824 (pCD07239) under different culture conditions 不同培养条件下乙酰丁酸梭菌 ATCC 824(pCD07239)的产酸期代谢特征
IF 2.3 3区 农林科学 Q3 FOOD SCIENCE & TECHNOLOGY Pub Date : 2024-09-12 DOI: 10.1186/s13765-024-00936-0
Haeng Lim Lee, Selim Ashoor, Zhuang Yao, Yu-Sin Jang

In this study, we investigated the metabolic behavior of the engineered Clostridium acetobutylicum ATCC 824 (pCD07239) strain during the acidogenic phase under varying glucose concentrations and pH conditions. Unlike the wild-type C. acetobutylicum ATCC 824, the engineered strain exhibited negligible butyrate production and simultaneous butanol production during the acidogenic phase under limited glucose condition of 25 g/L. Specifically, batch fermentations of the engineered strain with 25 g/L glucose at a pH of around 5.0 (initially uncontrolled) demonstrated butanol production of 2.99 g/L, while butyrate remained below 0.30 g/L. Separately, in batch fermentations at pH 6.0 with 90 g/L glucose, acetate production nearly doubled compared to fermentations at pH 5.0 with the same glucose concentrations, reaching a maximum concentration of 11.43 g/L, while butyrate production remained relatively low at 4.04 g/L. Under these pH 6.0 and 90 g/L glucose conditions, butanol production reached 9.86 g/L. These findings indicate that C. acetobutylicum ATCC 824 (pCD07239) maintained low butyrate production, even under conditions favoring acidogenesis, and consistently produced butanol. Additionally, the negligible production of acetone at pH 6.0 further indicates that the traditional phase transition was not prominent, suggesting altered regulation mechanisms in the engineered strain. These findings highlight C. acetobutylicum ATCC 824 (pCD07239) strain’s unique metabolic profile and its potential for efficient biobutanol production under diverse conditions.

在本研究中,我们研究了乙酰丁酸梭菌 ATCC 824(pCD07239)工程菌株在不同葡萄糖浓度和 pH 条件下的产酸阶段的代谢行为。与野生型乙酰丁酸梭菌 ATCC 824 不同的是,工程菌株在 25 克/升的有限葡萄糖条件下的产酸阶段表现出可忽略不计的丁酸产量,并同时产生丁醇。具体来说,在 pH 值为 5.0 左右(最初不受控制)、25 克/升葡萄糖条件下对工程菌株进行批量发酵时,丁醇产量为 2.99 克/升,而丁酸盐产量仍低于 0.30 克/升。另外,在 pH 值为 6.0、葡萄糖浓度为 90 克/升的批量发酵中,乙酸酯的产量比 pH 值为 5.0、葡萄糖浓度相同的发酵几乎翻了一番,达到 11.43 克/升的最大浓度,而丁酸盐的产量仍然相对较低,为 4.04 克/升。在 pH 值为 6.0、葡萄糖浓度为 90 克/升的条件下,丁醇产量达到 9.86 克/升。这些研究结果表明,即使在有利于酸生成的条件下,C. acetobutylicum ATCC 824(pCD07239)的丁酸产量也很低,但却能持续产生丁醇。此外,pH 值为 6.0 时丙酮的产量微乎其微,这进一步表明传统的相变并不突出,表明工程菌株的调节机制发生了改变。这些发现凸显了 C. acetobutylicum ATCC 824(pCD07239)菌株独特的代谢特征及其在不同条件下高效生产生物丁醇的潜力。
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引用次数: 0
Chikusetsusaponin IVa from Dolichos lablab Linne attenuates UVB-induced skin photoaging in mice by suppressing MAPK/AP-1 signaling 来自 Dolichos lablab Linne 的 Chikusetsusaponin IVa 通过抑制 MAPK/AP-1 信号传导,减轻紫外线诱导的小鼠皮肤光老化现象
IF 2.3 3区 农林科学 Q3 FOOD SCIENCE & TECHNOLOGY Pub Date : 2024-09-11 DOI: 10.1186/s13765-024-00934-2
Ki Mo Kim, A.-Rang Im, Ki-Shuk Shim, Chang-Seob Seo, Yongnam Lee, Jonghun Lee, Ji Seok Yoo, Sunga Choi, Sungwook Chae

Ultraviolet-B (UVB) radiation-induced photoaging of the skin is characterized by amplified expression of matrix metalloproteinase-1 (MMP-1) and reduced collagen fibers, both of which contribute to skin wrinkle formation. Edible natural products can protect against skin photoaging. Here, we investigate the protective effect of Dolichos lablab Linne (DLL) water extract against UVB radiation-prompted skin damage and attempt to uncover its fundamental mechanisms in human keratinocytes (HaCaT) and HR-1 hairless mouse. We found DLL extract rescued the reduction in cell viability associated with UVB exposure without any associated cytotoxic effects. It also protected against skin photoaging by inhibiting mitogen-activating protein kinase (MAPK) signaling, thereby preventing the UVB-associated increase in MMP-1 and -9 expression. DLL extract also increased the expression of both superoxide dismutase 1 (SOD1) and catalase (CAT). We identified chikusetsusaponin IVa, soyasaponin Bb, and sandosaponin A as bioactive components of DLL. Although we have not yet identified the mechanisms by which these compounds reduce the effects of photoaging, we have demonstrated that chikusetsusaponin IVa, soyasaponin Bb, and sandosaponin A reduce MMP-1, MMP-9, p–c-Fos, and p–c-Jun expression, while also avoiding any cytotoxicity. We found oral administration of DLL extract effectively alleviated dorsal epidermal thickening and skin dehydration in HR-1 hairless mouse visible to UVB. DLL extract also prevents UVB-induced activation of the MAPK/AP-1 signaling pathway, thereby reducing the expression of MMPs in dorsal mouse skin. Our results indicate that chikusetsusaponin IVa, soyasaponin Bb, and sandosaponin A are bioavailable components of DLL extract that can reduce UVB-induced skin damage via MMPs by deactivating the MAPK/AP-1 signaling pathway. These findings suggest DLL extract can be used as a skin anti-photoaging agent.

紫外线-B(UVB)辐射引起的皮肤光老化的特点是基质金属蛋白酶-1(MMP-1)的表达增大和胶原纤维减少,这两者都会导致皮肤皱纹的形成。食用天然产品可以防止皮肤光老化。在此,我们研究了Dolichos lablab Linne(DLL)水提取物对紫外线辐射引起的皮肤损伤的保护作用,并试图揭示其在人类角质细胞(HaCaT)和HR-1无毛小鼠中的基本机制。我们发现,DLL 水提取物能缓解紫外线照射导致的细胞活力下降,而不会产生任何相关的细胞毒性作用。它还能通过抑制有丝分裂原激活蛋白激酶(MAPK)信号传导,防止皮肤光老化,从而防止与 UVB 相关的 MMP-1 和 -9 表达增加。DLL 提取物还能增加超氧化物歧化酶 1(SOD1)和过氧化氢酶(CAT)的表达。我们发现 DLL 中的生物活性成分有菊苣皂苷 IVa、大豆皂苷 Bb 和山豆皂苷 A。虽然我们还没有确定这些化合物减少光老化影响的机制,但我们已经证明,菊苣皂苷 IVa、大豆皂苷 Bb 和山道皂苷 A 能减少 MMP-1、MMP-9、p-c-Fos 和 p-c-Jun 的表达,同时还能避免任何细胞毒性。我们发现,口服 DLL 提取物可有效缓解可见紫外线照射的 HR-1 无毛小鼠背侧表皮增厚和皮肤脱水现象。DLL 提取物还能防止紫外线诱导的 MAPK/AP-1 信号通路的激活,从而减少小鼠背侧皮肤中 MMPs 的表达。我们的研究结果表明,筑皂素 IVa、大豆皂素 Bb 和砂皂素 A 是 DLL 提取物中的生物可利用成分,它们能通过使 MAPK/AP-1 信号通路失活,减少紫外线诱导的皮肤损伤。这些研究结果表明,DLL 提取物可用作皮肤抗光老化剂。
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引用次数: 0
Inhibitory effect of human indoleamine 2,3-dioxygenase 1 (hIDO1) by kazinols of 1,3-diphenylpropane derivatives 1,3-二苯基丙烷衍生物卡嗪醇对人类吲哚胺 2,3-二氧合酶 1 (hIDO1) 的抑制作用
IF 2.3 3区 农林科学 Q3 FOOD SCIENCE & TECHNOLOGY Pub Date : 2024-09-04 DOI: 10.1186/s13765-024-00923-5
Taehoon Oh, Sunin Jung, Seon Min Oh, Mi Hyeon Park, Hyoung-Geun Kim, Su-Yeon Lee, Sung-Kyun Ko, Hyung Won Ryu

This study focused on identifying and characterizing 1,3-diphenylpropane derivatives from flavonoids that inhibit human indoleamine 2,3-dioxygenase 1 (hIDO1) enzymes, which play a role in immune regulation and are associated with various diseases. A series of isolated metabolites (1–7) demonstrated modest to high inhibition of hIDO1, with binding degree values ranging from 26.31 to 72.17%. In particular, during a target-based screening of natural products using hIDO1, kazinol J (6, a 1,3-diphenylpropane derivative) was found to potently inhibit hIDO1, with a binding degree of 72.17% at 1 ppm. Kazinol J (6) showed concentration-dependent and mixed inhibition kinetics and achieved slow and time-dependent inhibition of hIDO1. Additionally, docking simulations were performed to evaluate the inhibitory potential and binding interactions of the compounds with hIDO1. These findings suggest that these 1,3-diphenylpropane derivatives can serve as therapeutic agents for conditions involving hIDO1 dysregulation, such as cancer, autoimmune disorders, and infectious diseases.

这项研究的重点是从黄酮类化合物中鉴定和表征可抑制人类吲哚胺 2,3-二氧合酶 1(hIDO1)的 1,3-二苯基丙烷衍生物,这些酶在免疫调节中发挥作用,并与多种疾病相关。一系列分离出来的代谢物(1-7)对 hIDO1 的抑制作用从弱到强,结合度值从 26.31% 到 72.17%。其中,在利用 hIDO1 对天然产物进行靶向筛选的过程中,发现 kazinol J(6,一种 1,3-二苯基丙烷衍生物)对 hIDO1 具有强效抑制作用,在 1 ppm 时的结合度为 72.17%。Kazinol J (6) 显示出浓度依赖性和混合抑制动力学,并实现了对 hIDO1 的缓慢和时间依赖性抑制。此外,还进行了对接模拟,以评估化合物的抑制潜力以及与 hIDO1 的结合相互作用。这些研究结果表明,这些 1,3-二苯基丙烷衍生物可作为治疗药物,用于治疗涉及 hIDO1 失调的疾病,如癌症、自身免疫性疾病和传染性疾病。
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Applied Biological Chemistry
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