Article
Agriculture, Multidisciplinary
Mengdi Chen, Daodong Pan, Tianqiong Zhou, Xinchang Gao, Yali Dang
Summary: The novel umami peptide IPIPATKT exhibited excellent dual DPP-IV and ACE inhibitory activities, displaying significant physiological effects in cellular and in vivo models.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2021)
Article
Food Science & Technology
Papungkorn Sangsawad, Sasikan Katemala, Danou Pao, Saranya Suwanangul, Rachasit Jeencham, Manote Sutheerawattananonda
Summary: This study aimed to produce bioactive peptides from sericin using enzymatic hydrolysis methods, with neutrase producing peptides with the strongest DPP-IV and ACE inhibitory activities. The peptides remained stable even after simulated in vitro gastrointestinal digestion and ultrafiltration, showing promise as dietary ingredients for alleviating metabolic syndromes.
Article
Biochemical Research Methods
Shweta Thakur, Jyoti Chhimwal, Robin Joshi, Manglesh Kumari, Yogendra Padwad, Rajiv Kumar
Summary: A novel bioactive peptide BP1 from Picrorhiza kurroa Royle ex Benth. was found to have antioxidant potential and inhibitory activities against ACE and DPP-IV, making it a potential candidate for peptide-based therapeutics in treating diabetes, cardiovascular diseases, and other diseases associated with ROS.
JOURNAL OF PROTEOME RESEARCH
(2021)
Article
Nutrition & Dietetics
Yuchen Li, Gilda Aiello, Enrico Mario Alessandro Fassi, Giovanna Boschin, Martina Bartolomei, Carlotta Bollati, Gabriella Roda, Anna Arnoldi, Giovanni Grazioso, Carmen Lammi
Summary: This study focused on the extraction and hydrolysis of proteins from Chlorella pyrenoidosa (C. pyrenoidosa), showing potential hypotensive and hypoglycemic effects. Peptides derived from this process were found to inhibit ACE and DPP-IV activity effectively, with four peptides predicted to block both enzymes. The stability of these peptides during gastrointestinal digestion was also investigated.
Article
Food Science & Technology
Armin Mirzapour-Kouhdasht, Chul Won Lee, Hyosuk Yun, Jong-Bang Eun
Summary: This study investigated the multifunctionality of bioactive peptides derived from fermented skate skin gelatin hydrolysates, revealing two peptides with ACE inhibitory, DPP-IV inhibitory, and antibacterial activities. The study showed a relationship between hydrolysis time, degree of hydrolysis, and biological activities, with peptides P1 and P2 exhibiting different inhibitory activities against ACE, DPP-IV, and bacterial strains.
FOOD SCIENCE AND BIOTECHNOLOGY
(2021)
Review
Chemistry, Applied
Fernando Rivero-Pino
Summary: New challenges in food production and processing are emerging due to the growing global population and the need for a sustainable food system. Bioactive peptides derived from food proteins have potential preventive and therapeutic applications for various diseases. Extensive research has been conducted on the bioactivity of protein hydrolysates, particularly through in vitro tests, and some studies have examined their efficacy in animal models and human subjects. However, there is limited published literature on the functionality and effects of processing, storage, and gastrointestinal digestion on the bioactivity of these peptides in food matrices. This review aims to summarize the existing literature on protein hydrolysates as functional ingredients, including their processing, storage, and simulated gastrointestinal digestion, and their impact on the bioactivity of these peptides.
Article
Chemistry, Applied
Jialin Li, Xiaofeng Liu, Wen Li, Di Wu, Zhong Zhang, Wanchao Chen, Yan Yang
Summary: Umami peptides with both ACE and DPP-IV inhibitory activities were screened from Stropharia rugosoannulata using prediction tools and molecular docking. These peptides exhibited strong umami and inhibitory activities in evaluations and in vitro experiments. One peptide showed the most significant inhibitory activity. This comprehensive screening strategy provides a rapid approach for identifying high-sensitivity umami peptides with bioactivities.
Review
Veterinary Sciences
Daria Lotito, Eleonora Pacifico, Sara Matuozzo, Nadia Musco, Piera Iommelli, Fabio Zicarelli, Raffaella Tudisco, Federico Infascelli, Pietro Lombardi
Summary: This review compared the composition, characteristics, and management of dairy buffalo calves with those of bovines. The neonatal period is crucial for buffalo calves and is associated with a high mortality rate. Early intake of high-quality colostrum and vaccination play important roles in improving their immune system and reducing mortality rates. The study also highlighted the expanding buffalo breeding industry in Italy and the importance of understanding specific research on buffalo colostrum.
VETERINARY SCIENCES
(2023)
Article
Agriculture, Dairy & Animal Science
Arshida Ashraf, Priti Mudgil, Abdulrasheed Palakkott, Rabah Iratni, Chee-Yuen Gan, Sajid Maqsood, Mohammed Akli Ayoub
Summary: The molecular basis of the anti-diabetic properties of camel milk is still unknown, but recent studies suggest that camel whey proteins and their hydrolysates have an impact on in vivo activities. The results show inhibition of DPP-IV by these compounds and their positive effects on the activation of human insulin receptor and glucose uptake.
JOURNAL OF DAIRY SCIENCE
(2021)
Article
Agriculture, Multidisciplinary
Lingyan Dai, Lingxin Kong, Xiao Cai, Peng Jiang, Nian Liu, Dongjie Zhang, Zhijiang Li
Summary: This study developed potential dipeptidyl peptidase IV (DPP-IV) inhibitory oligopeptides from sorghum kafirin using in silico and in vitro methods. The inhibitory activities of these peptides were confirmed through molecular docking and in vitro experiments, and their potential in the treatment of diabetes was highlighted.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Martin Alain Mune Mune, Yoshikatsu Miyabe, Takeshi Shimizu, Wataru Matsui, Yuya Kumagai, Hideki Kishimura
Summary: In this study, we investigated the bioactive peptides produced from the red alga Gracilariopsis chorda through thermolysin hydrolysis of a water-soluble protein (WSP). The results showed that the WSP hydrolysate exhibited strong ACE inhibitory activity, indicating the potential of G. chorda as a source of ACE-inhibitory peptides. Two novel peptides (IDHY and LVVER) with promising inhibitory effects were identified, and their interaction with human ACE was evaluated through molecular docking. In silico analysis further revealed that the ACE inhibitory peptides were mainly located in the highly solvent accessible alpha-helix.
Article
Food Science & Technology
Shilpa Vij, Reenu Kashyap, Kapil Singh Narayan
Summary: In this study, bioactive peptides with immunomodulatory and antimicrobial activity were successfully isolated and identified from fermented buffalo colostrum whey. The peptide fraction of <10 kDa exhibited remarkable immunomodulatory activity, while the permeate fraction of <10 kDa showed higher antimicrobial activity against E. coli pathogens.
JOURNAL OF FUNCTIONAL FOODS
(2022)
Article
Food Science & Technology
Yue Zhang, Daodong Pan, Zhengcang Yang, Xinchang Gao, Yali Dang
Summary: Umami peptides derived from Ruditapes philippinarum have demonstrated ACE and DPP-IV inhibitory activities, as well as the ability to lower blood pressure and blood sugar levels. These peptides function by promoting nitric oxide secretion and reducing endothelin-1 production to exert hypoglycemic and hypotensive effects.
LWT-FOOD SCIENCE AND TECHNOLOGY
(2021)
Article
Nutrition & Dietetics
Jianqiang Li, Carlotta Bollati, Gilda Aiello, Martina Bartolomei, Fabrizio Rivardo, Giovanna Boschin, Anna Arnoldi, Carmen Lammi
Summary: The objective of this study was to evaluate the pleiotropic effect of a commercial casein hydrolysate (CH), which was found to contain peptides with potential inhibitory activities on angiotensin converting enzyme (ACE) and dipeptidyl-peptidase IV (DPP-IV) according to the BIOPEP-UWM database. Both in vitro and cell-based assays demonstrated the anti-diabetic and anti-hypertensive effects of CH, indicating its potential as an ingredient in functional food or nutraceuticals.
FRONTIERS IN NUTRITION
(2023)
Article
Food Science & Technology
Rosana Chirinos, Thomas Valente de Oliveira, Fanny Guzman, Ana Aguilar-Galvez, Andres Figueroa-Merma, Romina Pedreschi, David Campos
Summary: The present research aimed to evaluate the antioxidant, antihypertensive and hypoglycemic properties of three peptides synthesised from tarwi. In vitro and in silico studies were conducted, including molecular docking evaluation and ADMET properties assessment. The results showed potential antioxidant capacity and inhibition of ACE and DPP-IV enzymes for the peptides, particularly the YSGWLGL peptide. The predicted ADMET properties suggested their suitability for use as nutraceuticals, functional ingredients or supplements.
INTERNATIONAL JOURNAL OF FOOD SCIENCE AND TECHNOLOGY
(2023)
Article
Chemistry, Medicinal
Shuang Mei, Su Jiang, Yuting Wang, Han Jing, Peng Yang, Miao-Miao Niu, Jindong Li, Kai Yuan, Yan Zhang
Summary: This study identifies a dual-targeting peptide, AP-1, that effectively inhibits variants of concern (VOCs) of SARS-CoV-2 without impairing host cell viability. The findings suggest that AP-1 could be a promising broad-spectrum agent for treating emerging VOCs of SARS-CoV-2.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Hyeonjun Lee, Ju Yeon Lee, Hyunsoo Jang, Hye Young Cho, Minhee Kang, Sang Hyun Bae, Suin Kim, Eunji Kim, Jaebong Jang, Jin Young Kim, Young Ho Jeon
Summary: By using liquid chromatography-tandem mass spectrometry and nuclear magnetic resonance experiments, we identified new chemical moieties that bind to the target sites of the protein of interest, allowing for reversible binding and protein degradation. This method has the potential to expand the application of PROTAC technology.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Yingying Li, Xiyou Du, Xinru Kong, Yuelin Fang, Zhijing He, Dongzhu Liu, Hang Wu, Jianbo Ji, Xiaoye Yang, Lei Ye, Guangxi Zhai
Summary: This study proposes a novel nanoplatform based on the autophagy cascade to overcome the obstacles in chemo-immunotherapy. The platform combines chemotherapy and starvation therapy to initiate pro-death autophagy and enhance antigen presentation, while also remodeling the immunosuppressive tumor microenvironment. Furthermore, the study discovers a new therapeutic direction for the respiration inhibitor 3-bromopyruvic acid (3BP) in cancer treatment. Overall, this study offers an opportunity to improve antitumor efficacy and boost immune responses.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei, Linlin Wang, Jingwei Tian, Hongbo Wang
Summary: Breast cancer is a common malignant tumor in women, and drug resistance remains a clinical challenge. In this study, a novel compound, G-5b, was developed with potent antagonistic and degradation activities comparable to the current drug fulvestrant. G-5b also showed improved stability and solubility. Mechanistically, G-5b engages the proteasome pathway to degrade ER, inhibiting the ER signaling pathway and inducing apoptosis and cell cycle arrest. In animal models, G-5b exhibited superior pharmacokinetics and pharmacodynamics properties. Overall, G-5b is a promising long-acting SERD worthy of further investigation and optimization.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Karoline B. Waitman, Larissa C. de Almeida, Marina C. Primi, Jorge A. E. G. Carlos, Claudia Ruiz, Thales Kronenberger, Stefan Laufer, Marcia Ines Goettert, Antti Poso, Sandra V. Vassiliades, Vinicius A. M. de Souza, Monica F. Z. J. Toledo, Neuza M. A. Hassimotto, Michael D. Cameron, Thomas D. Bannister, Leticia Costa-Lotufo, Joa o A. Machado-Neto, Mauricio T. Tavares, Roberto Parise-Filho
Summary: A series of hybrid inhibitors combining pharmacophores of known kinase inhibitors and benzohydroxamate HDAC inhibitors were synthesized and evaluated for their anticancer activity and pharmacokinetic properties. Compounds 4d-f exhibited promising cytotoxicity against hematological cells and moderate activity against solid tumor models. Compound 4d showed potent inhibition of multiple kinase targets and had stable interactions with HDAC and members of the JAK family. These compounds showed selective cytotoxicity with minimal effects on non-tumorigenic cells and favorable pharmacokinetic profiles.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Michal Sulik, Diana Fontinha, Dietmar Steverding, Szymon Sobczak, Michal Antoszczak, Miguel Prudencio, Adam Huczynski
Summary: This study describes the synthesis of the first-in-class ivermectin derivatives obtained through derivatization of the C13 position, along with the unexpected rearrangement of the macrolide ring. These derivatives show potential for antiparasitic activity and are important for the development of new antiparasitic agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Jun Liu, Qiu-Xian Chen, Wen-Fu Wu, Dong Wang, Si -Yu Zhao, Jia-Hao Li, Yi-Qun Chang, Shao-Gao Zeng, Jia-Yi Hu, Yu-Jie Li, Jia-Xin Du, Shu-Meng Jiao, Hai-Chuan Xiao, Qiang Zhang, Jun Xu, Jian-Fu Zhao, Hai -Bo Zhou, Yong-Heng Wang, Jian Zou, Ping-Hua Sun
Summary: A new anti-infective drug strategy has been discovered to attenuate virulence and modulate inflammation caused by drug-resistant Pseudomonas aeruginosa infections. Compound 5f inhibits biofilm formation, macrophage migration, and inflammatory response induced by P. aeruginosa, showing potential as a novel candidate against drug-resistant infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Liuzeng Chen, Ke Wang, Lingyun Wang, Wei Wang, Lifan Wang, Jia Li, Xiaohan Liu, Mengya Wang, Banfeng Ruan
Summary: In this study, a series of novel anti-inflammatory compounds were designed and synthesized based on the natural product pterostilbene skeleton. Among them, compound 8 showed the highest activity and exhibited its effects through inhibition of pro-inflammatory cytokines by blocking the NF-KB/MAPK signaling pathway. Compound 8 also demonstrated a good relieving effect on acute colitis in mice and showed good safety in acute toxicity experiments.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)
Article
Chemistry, Medicinal
Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang
Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2024)