JOURNAL OF ASIA-PACIFIC ENTOMOLOGY
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2024
·
IF 1.1
Zhenni Ji,Chang Liu,Fa Xu,Yi Wang,Dongyu Gu,Yun Huang,Yi Yang
Blaps rynchopetera Fairmaire is a medicinal insect with a wide range of biological activities. Some of its activities, including anti-cancer and anti-inflammatory activities, are closely related to antioxidant capacity. In this study, a method was established to investigate components and theoretical mechanism of antioxidant from B. rynchopetera . As a result, two antioxidants were obtained by bioassay-guided separation and identified as 4-(2-hydroxyethyl)-1,2-benzenediol and 4-ethylbenzol-1,3-diol. Their EC 50 were 20.20 ± 0.30 μM and 22.90 ± 1.30 μM for ABTS· + scavenging, and 153.00 ± 2.00 μM and 301.00 ± 3.00 μM for DPPH· scavenging, respectively. The thermodynamic investigation indicated that the 2-OH of 4-(2-hydroxyethyl)-1,2-benzenediol and the 1-OH of 4-ethylbenzol-1,3-diol were more susceptible to be attacked by free radicals. They tended to exert antioxidant effects via the sequential proton loss electron transfer mechanism in polar media, whereas the hydrogen atom transfer mechanism was more likely to occur in non-polar media. In addition, frontier molecular orbital theory and energy barrier analysis suggested that 4-(2-hydroxyethyl)-1,2-benzenediol was more likely to react with DPPH·. These results confirmed that 4-(2-hydroxyethyl)-1,2-benzenediol had better antioxidant potential.
研究领域:
昆虫学
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药理学
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生物化学
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产品关联
DOI
高影响因子
Phytochemistry Letters
·
2023
·
IF 1.7
Yu-Chen Chen,Qiong Zheng,Hui Lu,Yi-Xin Zhuang,Ting-Ting Gong,Lie-Feng Ma,Zha-Jun Zhan
A new flavonoid glycoside bearing an unusual furan ring, epimedokoreanin F ( 1 ), was isolated from Epimedium brevicornu , along with 17 known flavonoids ( 2−18 ). The structures of these flavonoids were identified based on interpretation of spectroscopic data and comparison with literature data. Biologically, compounds 1−4 exhibited significant neuroprotective effects on the model of RSL3-induced ferroptosis in HT22 cells. Among them, compound 1 displayed the best activity with EC 50 values of 0.95 μ M, and can be used as lead compound for the development of neuroprotective agent to treat neurological diseases .
研究领域:
药理学
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神经科学
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生物化学
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植物化学
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产品关联
DOI
高影响因子
3 Biotech
·
2021
·Vol. 12
·期 1
·1-12
·
IF 2.406
Zhang Dong,Ma Zhi,Chen Hanchi,Ma Weilin,Zhou Jiawei,Wang Qing,Min Chan,Lu Yuele,Chen Xiaolong
A novel strain with antifungal activity against Sclerotinia sclerotiorum was isolated from soil, and identified as Streptomyces sp. ZJUT-IFE-354 using morphological and 16S rDNA sequence analysis. The bioactive metabolite produced by strain ZJUT-IFE-354 was identified and characterized as valinomycin by spectroscopic and chemical methods. The yield of valinomycin was 191.26 mg/L from the culture of Streptomyces sp. ZJUT-IFE-354, which was the highest yield to our knowledge. The in vitro antifungal activity of valinomycin against S. sclerotiorum was investigated as 0.056 ± 0.012 (EC 50 ) and 0.121 ± 0.023 μg/mL (EC 95 ), respectively, which was approximately 10.696- and 30.960-fold more active than that of carbendazim. The results from scanning electron microscopy, cell membrane permeability, and D -sorbitol and ergosterol assay indicated that valinomycin exerted the antifungal activity probably by increasing permeability of fungal cell membrane, leading to mycelial electrolyte leakage, and eventually resulting in the death of S. sclerotiorum . Thus, valinomycin may be a promising antifungal agent to control S. sclerotiorum .
研究领域:
微生物学
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药理学
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植物病理学
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DOI
PubMed
高影响因子
AQUACULTURE
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2021
·
IF 4.242
Xiaoping Tan,Yang Hu,Shenye Qu,Gaoxue Wang,Tianqiang Liu
Noxious pathogens always lead to high rates of mortality, which results in severe economic losses in aquaculture. Currently, gyrodactylosis treatments mainly rely on unapproved chemicals, which are not always satisfactory. According to the previous study, arctigenin is an efficient natural product for controlling gyrodactylosis. For the sake of seeking high-efficiency compounds, a new arctigenin derivative (CCA) was synthesized. Next, we evaluated the anthelmintic activity of CCA in vitro and in vivo , and studied the mechanism of action. The number of Gyrodactylus kobayashii significantly reduced as compared with the control group, the EC 50 value at 24 and 48-h after CCA treatment was 0.616 and 0.451 mg/L, respectively, with EC 100 at CCA concentration of 3 mg/L after 1 h bath treatment. In vitro results showed that CCA can rapidly reduce the amount of G. kobayashii and inhibit its mobility that could normally lead to death. The concentration and duration of CCA were positively correlated with the mortality of G. kobayashii . In addition, CCA displayed 100% efficacy against G. kobayashii at 4.0 mg/L after only 20 min exposure. Acute toxicity assay demonstrated that the LC 50 of CCA against goldfish was 5.012 mg/L, which was 8.13 times higher than that of the EC 50 . Furthermore, the results of confocal microscope study revealed that CCA leaded to the epidermal structure and dissolved muscles of worms. Moreover, the ATP level of worms were decreased sharply after both in vitro and in vivo exposures with CCA. The anthelminthic mechanism of CCA against gyrodactylids was related to epidermal structure damages and energy insufficient. From the previous study, the EC 50 of CCA against G. kobayashii (0.616 mg/L) was much lower than the EC 50 (1.85 mg/L) of arctigenin ( Tu et al., 2018 ). In summary, CCA is more effective than arctigenin and has great potential in control of Gyrodactylus infections.
研究领域:
水产养殖
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寄生虫学
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药理学
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兽医学
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DOI
高影响因子
Foods
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2023
·Vol. 12
·期 2
·392
·
IF 5.2
Yue Peng,Qian Wang,Kaixiang Zhu,Wu Ding
Pseudomonas aeruginosa(P. aeruginosa) is a typical Gram-negative bacterium that can cause the spoilage of catered food products. Using a luminescent reporter gene (luxCDABE), this study sought to construct a cell-based biosensor (PAO1-CE) to rapidly screen antibacterial substances againstP. aeruginosa. A total of six antibiotics belonging to five categories were used as the model test substances. The results of the bioluminescence detection method were verified using traditional antibacterial research assessments. The correlation coefficient of the regression equation fitting the data generated using this method was greater than 0.98, supporting the credibility of this approach. Additionally, the EC50of each of the antibiotics assessed in this study was lower than the 1/2 MIC determined by conventional means. All six of the antibiotics caused varying degrees of damage to the cell membrane and cell wall ofP. aeruginosa. Importantly, this novel method helped shorten the time necessary for active-compound detection and could be used for high-throughput detection, which would also help improve the detection efficiency. The application of this method towards the discovery of novel antibacterial compounds targetingP. aeruginosaholds substantial promise for greatly improving the efficiency of compound discovery.Keywords:luxCDABE;Pseudomonas aeruginosa;bacteriostatic substances;rapid
研究领域:
微生物学
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生物技术
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药学
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产品关联
DOI
PubMed
高影响因子
FOOD CHEMISTRY
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2023
·
IF 8.8
Yumei Qin,Yufei Zhou,Xue Yan,Zihan Qin,Yuezhong Mao,Shiyi Tian
Sweetness is a crucial indicator for identifying sweeteners used for flavor regulation and nutritional matching of foods. This study established a new quantitative sweetness evaluation method based on a combination of transiently transfected sweet taste receptor cells (STRs) and human sensory evaluation. Here, nine different sweeteners were evaluated and 10 sensory difference intensities and their corresponding concentrations were obtained through sensory evaluation. Using the same concentration solution as in the sensory evaluation, the dosage-response curve and EC 50 of the nine sweeteners were obtained by analyzing the intracellular calcium signal fluctuation of STRs. Data analysis revealed that the calcium signal intensity and sweetness intensity under the same concentration of sweetener presented a strong linear correlation (R 2 > 0.9). Additionally, we found a favorable correlation (R 2 = 0.8746) between the relative sweetness and EC 50 . These findings indicate that the quantitative evaluation of sweetness based on STRs could be a potential alternative to human sensory evaluation.
研究领域:
食品科学
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感官科学
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细胞生物学
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生物化学
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产品关联
DOI
PubMed
高影响因子
ENVIRONMENTAL SCIENCE & TECHNOLOGY
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2022
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IF 11.357
Di Zhang,Tom Bond,Yang Pan,Mingli Li,Jiayi Luo,Rong Xiao,Wenhai Chu
Identifying disinfection byproducts (DBPs) with high health risk is an unresolved challenge. In this study, six members of a new class of aromatic nitrogenous DBPs─2-chloroaniline, 2-bromoaniline, 2,4-dichloroaniline, 2-chloro-4-bromoaniline, 4-chloro-3-nitroaniline, and 2-chloro-4-nitroaniline─are reported as DBPs in drinking water for the first time. Haloanilines completely degraded within 1 h in the presence of chlorine (1 mg/L), while about 20% remained in the presence of chloramine (1 mg/L) after 120 h. Haloanilines showed high stability in the absence of disinfectants, with <30% degradation at pH 5–9 over 120 h. Eight haloanilines were determined in chloraminated finished water and tap water at total concentrations of up to 443 ng/L. The most abundant was 2-bromoaniline, with a median concentration of 104 ng/L. The cytotoxicity of eight haloanilines and regulated trichloromethane and dichloroacetic acid (DCAA) was evaluated using Hep G2 cell assay. The EC50 values of eight haloanilines were 1–2 orders of magnitude lower than those of the regulated DBPs. The lowest toxic concentration of 2-chloro-4-nitroaniline was 1 μM, 500 times lower than that of DCAA. The formation and control of haloanilines in drinking water warrant further investigation.
研究领域:
环境科学
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水处理
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毒理学
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公共卫生
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产品关联
DOI
PubMed
高影响因子
CHEMISTRY & BIODIVERSITY
·
2023
·Vol. 20
·期 6
·e202300128
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IF 2.9
Delong Wang,Chunxia Yuan,Jing Li,Yali Fang,Zhijia Zhang
In an effort to exploit the natural antifungal pogostone, its simplified scaffold dehydroacetic acid (DHA) was used as a lead compound to semi-synthesize 56 DHA derivatives ( I1 – 48 , II , III , and IV1 – 6 ). Among them, compound IV4 exhibited the most potent antifungal activity with 11.0 μM EC 50 against mycelial growth of Sclerotinia sclerotiorum (Lib.) de Bary whose sclerotia production was also completely suppressed at this concentration. Furthermore, IV4 could completely inhibit infection cushion formation of S. sclerotiorum on rape leaves and achieved a preventive efficacy of 90.2 % at 500 μM, which was on the same level as that of commercial boscalid at 30 μM (88.7 %). The results of physiological and ultrastructural studies indicated that IV4 might disrupt the cell membrane permeability or induce the imbalance of mitochondrial membrane potential homeostasis to exert the antifungal mode of action. Besides, the robust and predicative three-dimensional quantitative structure-activity relationship (3D-QSAR) models were developed and discussed herein.
研究领域:
药物化学
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植物病理学
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分子生物学
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
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2024
·
IF 5.7
Ruo-Fei Bai,Yi-Wei Wang,Shan-Shan Yang,Yu-Hao Zhang,Bo-Hang Zhou,Cong-Wei Zhou,Le Zhou
As part of our continuing research on propiolic acid derivatives, a series of benzyl propiolate derivatives and analogues were designed, synthesized, and investigated for inhibition activity in vitro and in vivo on phytopathogenic fungi, structure–activity relationship (SAR) and action mechanism. The results showed that most of the compounds had potent and broad-spectrum antifungal activity in vitro at 50 μg/mL. Among the compounds, 2-bromobenzyl propiolate (3h) displayed the highest comprehensive activity with total activity index (TAI) of 4.57 against all the eight test fungi followed by 3-fluorobenzyl propiolate (3c) (TAI = 4.53), superior to positive fungicides thiabendazole (TAI < 4.12) and/or azoxystrobin (TAI < 2.90). Relative to the other fungi, Fusarium solani and Fusarium graminearum revealed higher total susceptibility indexes (TSI) of 11.1 and 8.98, respectively, for all compounds. 3h and 3g (4-chlorobenzyl propiolate) gave the smallest EC50 values of 0.86 and 0.67 μg/mL against F. solani and F. graminearum, respectively, superior or comparable with thiabendazole and azoxystrobin. As a representative, 3h at 200 μg/mL displayed 100% protection on F. solani infections on potatoes over 7 days and high safety for plant growth. In antifungal mechanism, 3h was able to change mycelial morphology, destroy the structures of both hypha and cell membrane, increase the intracellular ROS level, decrease the intracellular mitochondrial membrane potential level, and change the permeability of the cell membrane. The SAR showed that ethynyl is a key group for the activity, and the presence of halogen atoms at the 2-site of the benzene ring can significantly improve the activity in most cases. Thus, benzyl propiolate can be considered a novel antifungal lead compound, while 3h can be considered a promising fungicide candidate to develop new agricultural fungicides.
研究领域:
农业化学
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植物病理学
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药物化学
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DOI
PubMed
高影响因子
Frontiers in Microbiology
·
2019
·
IF 4.259
Zhang Shujing,Liu Qi,Han Yunfei,Han Jinghua,Yan Zhiqiang,Wang Yonghong,Zhang Xing
This study was conducted to purify and identify metabolites of antimicrobial activity against phytopathogens from Xenorhabdus nematophila YL001. Three dipeptide compounds were purified from its cell-free cultural broth and identified as (±)-nematophin, cyclo (L-Pro-Gly), and N, N′-dimethyl-cyclo (L-Phe-L-Leu). Nematophin demonstrated a wider antifungal spectrum than the other two compounds. It also exhibited strong inhibitory effects on mycelial growth of Rhizoctonia solani and Phytophthora infestans with EC50 values of 40.00 and 51.25 μg/ml, respectively. Its (S)-configuration structure [(+)-nematophin] was also synthesized and exhibited higher antimicrobial activity than the enantiomeric mixture. The detached leaf assay revealed that nematophin possessed significant preventive and curative efficacy against R. solani on broad bean leaves showing corresponding control efficacies of 93.01 and 94.93% at 1,000 μg/ml, comparable to those of a chemical fungicide (carbendazim) at 500 μg/ml. Additionally, the pot experiments indicated that nematophin could effectively inhibit the disease extension on rice and broad bean plants caused by R. solani. Nematophin also exerted some adverse influences on the sclerotial development of R. solani by dramatically suppressing their formation and maturation at 40.00 μg/ml, as well as their germination at 15.00 μg/ml. Morphological and ultrastructural observations showed that the hyphae of R. solani became twisted, shriveled, and deformed at the growing points after exposure to nematophin at 40.00 μg/ml, and that the subcellular fractions also became abnormal concurrently, especially the mitochondrial structure. These results indicate that nematophin has great potential to be used as a bio-pesticide in agricultural production.
研究领域:
农业科学
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微生物学
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植物病理学
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生物技术
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DOI
PubMed
高影响因子
PEST MANAGEMENT SCIENCE
·
2024
·
IF 3.8
Liangzhen Shu,Ya Lv,Zhongyin Chen,Yixian Huang,Meng Zhang,Zhichao Jin,Tingting Li,Yonggui Robin Chi
BACKGROUND Potato virus Y (PVY) is a prominent representative of plant viruses. It can inflict severe damage upon Solanaceae plants, leading to global dissemination and substantial economic losses. To discover new antiviral agents, a class of planar chiral thiourea molecules through the key step of N -heterocyclic carbene-catalyzed nitrile formation reaction was synthesized with excellent optical purities for antiviral evaluations against plant virus PVY. RESULTS The absolute configurations of the planar chiral compounds exhibited obvious distinctions in the anti-PVY activities. Notability, compound ( S )- 4u exhibited remarkable curative activities against PVY, with a half maximal effective concentration (EC 50 ) of 349.3 μg mL −1 , which was lower than that of the ningnanmycin (NNM) (EC 50 = 400.8 μg mL −1 ). Additionally, The EC 50 value for the protective effects of ( S )- 4u was 146.2 μg mL −1 , which was superior to that of NNM (276.4 μg mL −1 ). Furthermore, the mechanism-of-action of enantiomers of planar chiral compound 4u was investigated through molecular docking, defensive enzyme activity tests and chlorophyll content tests. CONCLUSION Biological mechanism studies have demonstrated that the configuration of planar chiral target compounds plays a crucial role in the molecular interaction with PVY-CP, enhancing the activity of defense enzymes and affecting chlorophyll content. The current study has provided significant insights into the roles played by planar chiralities in plant protection against viruses. This paves the way for the development of novel green pesticides bearing planar chiralities with excellent optical purities. © 2024 Society of Chemical Industry.
研究领域:
植物病理学
·
有机化学
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药学
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生物化学
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农业科学
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DOI
PubMed
高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2024
·
IF 5.7
Yixian Huang,Xiaolin Peng,Jinli Chen,Liangzhen Shu,Meng Zhang,Jiamiao Jin,Zhichao Jin,Yonggui Robin Chi
Potato virus Y (PVY) is an important plant virus that has spread worldwide, causing significant economic losses. To search for novel structures as potent antiviral agents, a series of chiral indole derivatives containing oxazoline moieties were designed and synthesized and their anti-PVY activities were evaluated. Biological activity tests demonstrated that many chiral compounds exhibited promising anti-PVY activities and that their absolute configurations exhibited obvious distinctions in antiviral bioactivities. Notably, compound (S)-4v displayed excellent curative and protective efficacy against PVY, with EC50 values of 328.6 and 256.1 μg/mL, respectively, which were superior to those of commercial virucide ningnanmycin (NNM, 437.4 and 397.4 μg/mL, respectively). The preliminary antiviral mechanism was investigated to determine the difference in antiviral activity between the two enantiomers of 4v chiral compounds. Molecular docking indicated a stronger binding affinity between the coating proteins of PVY (PVY-CP) and (S)-4v (−6.5 kcal/mol) compared to (R)-4v (−6.2 kcal/mol). Additionally, compound (S)-4v can increase the chlorophyll content and defense-related enzyme activities more effectively than its enantiomer. Therefore, this study provides an important basis for the development of chiral indole derivatives containing oxazoline moieties as novel agricultural chemicals.
研究领域:
植物病理学
·
药物化学
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农业科学
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）