Article
Polymer Science
Katia Rubini, Elisa Boanini, Silvia Parmeggiani, Adriana Bigi
Summary: In this study, curcumin was used as a functionalizing agent to develop antioxidant materials with modulated physico-chemical properties in gelatin films. The functionalized films exhibited remarkable antioxidant properties and sustained curcumin release, suggesting potential applications in various fields. The properties of the materials varied based on the curcumin content and presence of crosslinking agent, demonstrating the versatility of gelatin in different applications.
Article
Materials Science, Multidisciplinary
S. Shakeel Nawaz, K. B. Manjunatha, S. Ranganatha, S. Supriya, Prabhat Ranjan, Tanmoy Chakraborty, Dileep Ramakrishna
Summary: In this study, two nickel complexes (NiClCur and NiAcCur) were synthesized and their structural characteristics were analyzed using various spectroscopic techniques. The complexation between nickel and the ligand was revealed by H-1 NMR study. Theoretical analysis of the complexes was conducted using Conceptual-Density-Functional-Theory. Nonlinear optics and transmission measurements were performed on the complexes, and their optical limiting behavior was calculated. This work provides new insights into the field of NLO by implementing curcumin-based metal complexes.
Article
Plant Sciences
Mohamed Jawed Ahsan, Kavita Choudhary, Amena Ali, Abuzer Ali, Faizul Azam, Atiah H. Almalki, Eman Y. Santali, Md. Afroz Bakht, Abu Tahir, Salahuddin
Summary: Curcumin analogues have shown promising anticancer activity, with compounds 3b and 3c exhibiting the most potential. These compounds demonstrated significant growth inhibitions against multiple cancer cell lines and displayed good selectivity and binding affinity. These analogues may offer beneficial therapeutic intervention for cancer treatment and prevention.
Article
Chemistry, Medicinal
Run Xu, Yongxiang Song, Jun Li, Jianhua Ju, Qinglian Li
Summary: Desotamides A4 and A6, with l-Ile at position II and d-Lys or d-Arg at position VI, exhibit enhanced antibacterial activities against a range of Gram-positive pathogens, including drug-resistant strains like MRSA. Their broad spectrum and increased potency make them promising candidates for further antibiotic development.
Review
Chemistry, Medicinal
Seyedeh Roya Alizadeh, Mohammad Ali Ebrahimzadeh
Summary: Quercetin, a valuable natural flavonoid, exhibits various biological activities, but its low solubility and poor bioavailability limit its applications. Researchers have designed and synthesized new quercetin derivatives to improve its biological activities. This review focused on categorizing and studying the biological activities, structure-activity relationship, and action mechanism of O-glycoside quercetin derivatives.
PHYTOTHERAPY RESEARCH
(2022)
Article
Food Science & Technology
Fakfan Luangapai, Methavee Peanparkdee, Satoshi Iwamoto
Summary: The study successfully incorporated a curcumin nanoemulsion (CurNE) into chitosan (CH)-based films to improve their mechanical properties and reduce water vapor permeability. Evaluation of thermal and electrical properties revealed structural alterations. The antioxidant activity of CH-NE was significantly higher than CH.
INTERNATIONAL JOURNAL OF FOOD SCIENCE AND TECHNOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Gaia Rocchitta, Carla Rozzo, Marina Pisano, Davide Fabbri, Maria Antonietta Dettori, Paolo Ruzza, Claudia Honisch, Roberto Dallocchio, Alessandro Dessi, Rossana Migheli, PierAndrea Serra, Giovanna Delogu
Summary: This study synthesized three curcumin-inspired compounds and analyzed their activities. The results showed that these compounds have inhibitory effects on melanin synthesis and have high antioxidant activity.
Article
Biochemistry & Molecular Biology
Dalia Urbonaviciene, Ramune Bobinaite, Pranas Viskelis, Ceslovas Bobinas, Aistis Petruskevicius, Linards Klavins, Jonas Viskelis
Summary: The aim of this study was to characterize the variation in biologically active compounds, antioxidant activity and physico-chemical properties in bilberries from different sites in Northern Europe. The study found variations in the biologically active compounds and antioxidant activity of bilberries, suggesting the influence of genotype.
Article
Food Science & Technology
Rongxin Han, Shuai Shao, Hongyin Zhang, Hongyu Qi, Fengqin Xiao, Yingxin Shen, Lin Fan, Haidong Wang, Daqing Zhao, Guangzhe Li, Mingming Yan
Summary: This study demonstrates that WJSPHs exhibit high antioxidant activity and ACE inhibitory activity in vitro, suggesting their potential application as antioxidant peptides for preventing oxidative-related diseases.
JOURNAL OF FOOD SCIENCE
(2022)
Review
Chemistry, Medicinal
Santosh Kumar Verma, Rameshwari Verma, Shekhar Verma, Yogesh Vaishnav, S. P. Tiwari, K. P. Rakesh
Summary: This review summarizes the current innovations of oxadiazole-based derivatives with potential antituberculosis activity, discussing their role as bioisosteric substitutions and interactions with anti-TB targets.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Yisett Gonzalez, Randy Mojica-Flores, Dilan Moreno-Labrador, Marisin Pecchio, K. S. Jagannatha Rao, Maicol Ahumedo-Monterrosa, Patricia L. Fernandez, Oleg V. Larionov, Johant Lakey-Beitia
Summary: Tetrahydrocurcumin, the most abundant curcumin transformation product in biological systems, has higher anti-inflammatory activity and bioavailability compared to curcumin. This article describes the synthesis and evaluation of tetrahydrocurcumin derivatives for their anti-inflammatory activities. Some of the derivatives showed better inhibition than tetrahydrocurcumin.
Article
Food Science & Technology
Kristyna Opustilova, Barbora Lapcikova, Lubomir Lapcik, Shweta Gautam, Tomas Valenta, Peng Li
Summary: Physicochemical analyses were conducted on curcumin standard sample and curcumin multiple emulsions. The study revealed poor stability of the emulsions and showed that the content of curcuminoid substances can be determined using MDSC method. CLSM observation confirmed the presence of suspended curcumin particles in the oil phase.
Article
Chemistry, Multidisciplinary
Haiyang Hu, Zuyue Liao, Mengyao Xu, Shengli Wan, Yuesong Wu, Wenjun Zou, Jianming Wu, Qingze Fan
Summary: Statistical analysis and Box-Behnken design were used to optimize the preparation of PLGA nanoparticles loaded with PTX and CUR. By adjusting the surfactant concentration, polymer concentration, and oil-water ratio, nanoparticles with excellent properties were obtained.
Article
Polymer Science
Aji Prasetyaningrum, Dani P. Utomo, Al Farrel A. Raemas, Tutuk D. Kusworo, Bakti Jos, Mohammad Djaeni
Summary: This study aimed to enhance the properties of CaCl2 crosslinked sodium alginate/κ-carrageenan incorporated with clove essential oil by evaluating the effects on physicochemical, morphological, antioxidant, and antibacterial properties. The addition of κ-carrageenan and CaCl2 improved the surface morphology and mechanical properties of the films, while the incorporation of clove essential oil showed effectiveness in antioxidant and antimicrobial activity.
Article
Chemistry, Multidisciplinary
Kajal Dhawan, Prasad Rasane, Jyoti Singh, Sawinder Kaur, Damanpreet Kaur, Harshal Avinashe, Dipendra Kumar Mahato, Pradeep Kumar, Mahendra Gunjal, Esra Capanoglu, Shafiul Haque
Summary: The aim of this study was to formulate and determine the sensory, proximate, phytochemical, and antioxidant properties of matcha hard candies incorporated with spices such as ginger, cinnamon, and holy basil. Different concentrations of spices/herbs were incorporated into standardized matcha hard candy. The best formulations for matcha ginger hard candy, matcha cinnamon hard candy, and matcha tulsi hard candy were selected based on organoleptic evaluation and showed significant proximate, phytochemical, and antioxidant profiles. This study demonstrates the excellent nutritional and phytochemical potential of spiced matcha hard candy as a nutraceutical food product.
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)