Article
Biochemistry & Molecular Biology
Kuan-Ming Chiu, Yen-Ling Hung, Su-Jane Wang, Yi-Ju Tsai, Nan-Lin Wu, Cher-Wei Liang, Der-Chen Chang, Chi-Feng Hung
Summary: Neferine has anti-allergic and anti-inflammatory effects on mast cells by inhibiting degranulation and cytokine expression, decreasing intracellular calcium levels, and reducing the phosphorylation of the MAPK/NF-kappa B pathway. In vivo studies demonstrate that neferine improves dermatitis appearance, mast cell infiltration, and restores barrier protein expression. Neferine also reduces scratching behavior induced by compound 48/80, suggesting its potential as a natural product for skin allergy and inflammation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Medicine, Research & Experimental
Susanna Choi, Myung-A Jung, Youn-Hwan Hwang, Bo-Jeong Pyun, Joo Young Lee, Dong Ho Jung, Kon-Young Ji, Taesoo Kim
Summary: The study demonstrated that Asarum heterotropoides (AH) has anti-allergic effects in treating allergic rhinitis (AR) in mice by reducing allergic symptoms, decreasing levels of allergic mediators, and suppressing tissue thickening. AH showed capacity to modulate AR through regulating various immune cells and epithelial cells.
BIOMEDICINE & PHARMACOTHERAPY
(2021)
Review
Food Science & Technology
Mehtap Civelek, Sabrina Bilotta, Axel Lorentz
Summary: This review summarizes the anti-inflammatory effects of resveratrol on mast cell-mediated allergic reactions. The studies suggest that resveratrol can inhibit mast cell degranulation and the release of proinflammatory mediators, and has positive impacts on allergic rhinitis patients. However, strategies to improve resveratrol's bioavailability need to be developed.
MOLECULAR NUTRITION & FOOD RESEARCH
(2022)
Article
Immunology
Charles Ezeamuzie, Muddanna S. Rao, Ahmed Z. El-Hashim, Elizabeth Philip, Oludotun A. Phillips
Summary: This study reports a new dual inhibitor, PH-251, which can simultaneously inhibit 5-lipoxygenase and mast cell degranulation, with demonstrated in vivo activity in animal models. This compound may offer potential advantages for the treatment of asthma and other allergic and inflammatory diseases.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2022)
Article
Chemistry, Medicinal
Rui Liu, Yonghui Zhang, Yuejin Wang, Yihan Huang, Jiapan Gao, Xi Tian, Tianyou Ma, Tao Zhang
Summary: Herb-derived dictamnine has pharmacological effects on IgE-induced MC activation and OVA-induced murine AR model, reducing local allergic reactions and systemic anaphylaxis. Dictamnine inhibits MC activation via the LYN kinase-mediated molecular signaling pathway, making it a promising treatment for AR.
PHYTOTHERAPY RESEARCH
(2023)
Review
Pharmacology & Pharmacy
Kong Yen Liew, Nurain Irdayani Kamise, Hui Ming Ong, Poi Yi Aw Yong, Fahmida Islam, Ji Wei Tan, Chau Ling Tham
Summary: Allergic diseases are a global health burden, and the current available medications have side effects, poor perceived effectiveness, and high cost. Propolis, a natural herbal medicine with antioxidant, antimicrobial, and anticancer properties, has the potential to be a prophylactic or therapeutic option for allergic diseases. Preclinical studies have shown that propolis extracts have therapeutic effects on allergic inflammation, asthma, allergic rhinitis, atopic dermatitis, and food allergy by inhibiting mast cell and basophil activation. Clinically, propolis consumption as a supplement or adjunct therapy is safe and attenuates pathological conditions in asthma. Flavonoids and cinnamic acid derivatives in propolis contribute to its anti-allergic activities, but their presence varies in different propolis samples. Future studies should focus on the relationship between propolis's anti-allergic activity and its chemical contents.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Immunology
Hima Dhakal, Min -Jong Kim, Soyoung Lee, Young-Ae Choi, Namkyung Kim, Taeg Kyu Kwon, Dongwoo Khang, Sang-Hyun Kim
Summary: The study demonstrated that ursolic acid (UA) exerts anti-allergic effects by inhibiting FceRI-mediated mast cell activation. It suppresses mast cell degranulation by reducing intracellular calcium levels and inhibits the expression and release of inflammatory cytokines. Furthermore, UA also inhibits passive cutaneous anaphylaxis and active systemic anaphylaxis reactions in a mouse model in a dose-dependent manner.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2021)
Article
Immunology
Hee-Yun Kim, Hanchul Jung, Hyung-Min Kim, Hyun-Ja Jeong
Summary: Surfactin exhibits significant anti-cancer effects on melanoma skin cancer by enhancing immune response and inducing apoptosis of melanoma cells.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2021)
Article
Chemistry, Medicinal
Jiayu Lu, Xiangjun Wang, Shuai Ge, Yajing Hou, Yuexin Lv, Huaizhen He, Cheng Wang
Summary: This study synthesized two novel derivatives by integrating the active substructures of B10-S and mubritinib and evaluated their anti-allergic inhibitory effects. The results showed that both compounds effectively inhibited the release of beta-hexosaminidase and histamine in cells by targeting MRGPRX2 and reduced intracellular Ca2+ levels. Molecular docking analysis also revealed their binding sites on MRGPRX2. These findings may contribute to the development of synthetic molecules with anti-pseudo-allergic activity in the future.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Immunology
Ji Eon Lee, Min Yeong Choi, Keun Young Min, Min Geun Jo, Young Mi Kim, Hyuk Soon Kim, Wahn Soo Choi
Summary: The study found that nifuratel inhibits antigen-induced mast cell degranulation and secretion of inflammatory cytokines. It does so by inhibiting the phosphorylation of Syk and decreasing the activation of downstream signaling proteins. Nifuratel also significantly suppresses IgE-mediated passive cutaneous anaphylaxis. These findings suggest that nifuratel could be a potential drug candidate for IgE-mediated allergic disorders.
INTERNATIONAL JOURNAL OF IMMUNOPATHOLOGY AND PHARMACOLOGY
(2023)
Article
Plant Sciences
Haruka Asai, Koichi Kato, Moe Suzuki, Misato Takahashi, Erika Miyata, Moeka Aoi, Reika Kumazawa, Fumihiro Nagashima, Hiromasa Kurosaki, Yutaka Aoyagi, Nobuyuki Fukuishi
Summary: The bibenzyl derivatives perD and Ac-perD from the liverwort Radula perrottetii have inhibitory effects on antigen-induced activation of mast cells (MCs), making them potential lead compounds for the development of novel anti-allergic and anti-inflammatory drugs.
Article
Immunology
Tongqian Wu, Lan Ma, Xiaoqian Jin, Jingjing He, Ke Chen, Dingshan Zhang, Rui Yuan, Jun Yang, Qin Zhong, Haiyan Zhou, Zou Xiang, Yu Fang
Summary: The study demonstrated that S100A4 plays a critical role in regulating mast cell activation and allergic responses. S100A4(-/-) mice showed reduced symptoms in allergic models, indicating that S100A4 is required for mast cell activation and may be involved in the regulation of allergic diseases through this mechanism.
FRONTIERS IN IMMUNOLOGY
(2021)
Review
Biochemistry & Molecular Biology
Tamara T. Haque, Pamela A. Frischmeyer-Guerrerio
Summary: This article discusses cytokines that regulate mast cell-mediated allergic immune responses. Understanding the mechanisms of these cytokines is important for the development of effective treatment methods.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Immunology
Hee-Yun Kim, Ho-Geun Kang, Hyung-Min Kim, Hyun-Ja Jeong
Summary: This study explored the potential roles of TMP-SMX in melanoma skin cancer, using an immunodeficient mouse model. The results showed that TMP-SMX significantly improved the survival rate, reduced tumor weight and growth, and decreased the levels of vascular endothelial growth factor. Additionally, TMP-SMX inhibited melanoma skin cancer growth by triggering an allergic reaction and promoting immunity. Therefore, TMP-SMX may be considered as an immune booster in cancer chemotherapy.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2023)
Article
Immunology
Yong-Shi Yang, Meng-Da Cao, An Wang, Qing-Mei Liu, Dan-Xuan Zhu, Ying Zou, Ling-Ling Ma, Min Luo, Yang Shao, Dian-Dou Xu, Ji-Fu Wei, Jin-Lyu Sun
Summary: The study found that nano-SiO2 particles can synergistically activate IgE-sensitized mast cells by enhancing the MAPK signaling pathway and exacerbate allergic inflammation.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Biodiversity Conservation
Mohammad Omar Faruque, Gang Feng, Md Nurul Amin Khan, James W. Barlow, Umme Ruman Ankhi, Sheng Hu, M. Kamaruzzaman, Shaikh Bokhtear Uddin, Xuebo Hu
JOURNAL OF ETHNOBIOLOGY AND ETHNOMEDICINE
(2019)
Article
Plant Sciences
Md. Adnan, Md. Nazim Uddin Chy, A. T. M. Mostafa Kam, James W. Barlow, Mohammad Omar Faruque, Xinzhou Yang, Shaikh Bokhtear Uddin
JOURNAL OF ETHNOPHARMACOLOGY
(2019)
Article
Chemistry, Multidisciplinary
Alan J. Hibbitts, Joanne M. Ramsey, James Barlow, Ronan MacLoughlin, Sally-Ann Cryan
Article
Biochemistry & Molecular Biology
Lisa Foley, Jennifer Toney, James W. Barlow, Maura O'Connor, Deirdre Fitzgerald-Hughes, Zebunnissa Ramtoola
Summary: The study evaluated the physical, chemical, and microbiological stability of an extemporaneous oral liquid suspension of losartan potassium, concluding that the suspensions are stable over 28 days when stored at 4 degrees C and room temperature. The initial losartan content was lower than expected but did not significantly change over time. This reduction was related to the acidic pH of the suspension vehicle.
Article
Biochemistry & Molecular Biology
Sean Coll, Mohammad Alhazmi, Patricia de Aguiar Amaral, Sandra Bourgeade-Delmas, Anne-Cecile Le Lamer, James W. Barlow
Summary: In this study, a variety of novel thiochromanones based on natural products with anti-leishmanial activity were designed and synthesized using 2,2,6-trimethoxythiochromanone as a key intermediate. Among the synthesized compounds, phenylalkenyl and haloalkyl amides 11a and 11e were found to be the most potent against Leishmania with IC50 values of 10.5 and 7.2 μM, respectively.
Article
Education & Educational Research
Aisling Kerr, Judith Strawbridge, Caroline Kelleher, James Barlow, Clare Sullivan, Teresa Pawlikowska
Summary: Effective communication between pharmacists and patients is crucial for improving health outcomes. Simulated patients (SPs) play a valuable role in helping pharmacy students develop and adapt their communication skills through role-play exercises. This study showed that SP role-play can enhance students' awareness of communication styles, promote more structured communication, and increase comfort levels, despite a slight decrease in communication scores during mock OSCE sessions.
BMC MEDICAL EDUCATION
(2021)
Article
Public, Environmental & Occupational Health
Judith Strawbridge, John C. Hayden, Tracy Robson, Michelle Flood, Shane Cullinan, Matthew Lynch, Anne Teresa Morgan, Fiona O'Brien, Roisin Reynolds, Steven W. Kerrigan, Gianpiero Cavalleri, Brian P. Kirby, Orna Tighe, Anthony Maher, James W. Barlow
Summary: The COVID-19 pandemic has had a significant impact on pharmacy education worldwide, leading to the need for rapid adaptation and implementation of safety measures. This article describes the challenges faced and measures taken by institutions during the pandemic.
RESEARCH IN SOCIAL & ADMINISTRATIVE PHARMACY
(2022)
Review
Biochemistry & Molecular Biology
Samuel E. Collyer, Gary D. Stack, John J. Walsh
Summary: Actively targeted drug conjugates have been developed to improve the specificity of tubulin binding agents by covalently conjugating them with agents that target cancer cells. These conjugates increase the uptake of the drug by cancer cells while minimizing uptake by normal cells, leading to improved efficacy and tolerability. Antibody targeted strategies have been the most successful in this regard.
CURRENT MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Camille Scotti, James W. Barlow
Summary: This article reviews novel nitrile-containing molecules isolated from natural sources between 1998 and 2021, and discusses their biological activity. These molecules, gathered from various origins in the plant, animal, and microbial worlds, exhibit diverse biological activities and hold great potential for medicinal applications.
NATURAL PRODUCT COMMUNICATIONS
(2022)
Article
Chemistry, Applied
Franciely Vanessa Costa, Alice Gadea, Altamir Rocha Antunes, Solenn Ferron, alvaro Jose Back, James W. Barlow, Vanilde Citadini-Zanette, Francoise Lohezic-Le Devehat, Patricia de Aguiar Amaral
Summary: This study evaluated the influence of environmental factors on the chemical profile of C. pinnatifida, a plant used in Brazilian folk medicine. Results showed that samples collected from different altitudes had different metabolic profiles.
NATURAL PRODUCT RESEARCH
(2022)
Review
Food Science & Technology
Quanxiang Yan, Tao Zhang, Christine O'Connor, James W. W. Barlow, John Walsh, Gaia Scalabrino, Feng Xu, Helen Sheridan
Summary: Vitamin K1 and Vitamin K2 are two important micronutrients in the Vitamin K family, found in green leafy plants and algae (Vitamin K1) and animal and fermented foods (Vitamin K2) respectively. This review explores the various biological functions of Vitamin K2, including promotion of osteogenesis, prevention of calcification, relief of menopausal symptoms, enhancement of mitochondrial energy release, hepato- and neuro-protective effects, and potential use in the treatment of coronavirus disease. The mechanisms of action associated with these effects are also discussed. Overall, Vitamin K, especially Vitamin K2, plays a crucial role in maintaining human health by affecting major body systems and regulating numerous physiological and pathological processes. However, further research is needed to fully understand its therapeutic potential in preventing and treating various diseases.
FOOD SCIENCE & NUTRITION
(2023)
Review
Plant Sciences
Mark J. J. Lyons, Carsten Ehrhardt, John J. J. Walsh
Summary: Fungal metabolites, such as orellanine found in mushrooms, have potential as novel anticancer drugs. This review focuses on orellanine's historical significance, structural features, toxicomechanics, chromatographic analysis, synthesis, and chemotherapeutic potential. The toxicity mechanisms of orellanine in kidney tissue are still disputed, and its chromatographic analysis and biological evaluation face challenges. Despite these obstacles, orellanine has shown promising data in preclinical studies for metastatic clear cell renal cell carcinoma, leading to phase I/II trials in humans.
JOURNAL OF NATURAL PRODUCTS
(2023)
Article
Chemistry, Medicinal
Patricia Rossa Milanez, Falaise Matos Ramos da Silva, Rahisa Scussel, Maria Eduarda de Melo, Andre Bittencourt Martins, Ricardo Andrez Machado-de-Avila, James William Barlow, Paulo Emilio Feuser, Flavia Karine Rigo, Patricia de Aguiar Amaral
Summary: This study focused on the extraction and purification of cannabinoid compounds from forensic samples of Cannabis sativa L., Cannabaceae, and demonstrated promising effects of various cannabinoid extracts in a murine melanoma cancer cell line.
REVISTA BRASILEIRA DE FARMACOGNOSIA-BRAZILIAN JOURNAL OF PHARMACOGNOSY
(2021)
Article
Biochemistry & Molecular Biology
Sajib Rudra, Afroza Tahamina, Nazim Uddin Emon, Md Adnan, Mohammad Shakil, Md Helal Uddin Chowdhury, James W. Barlow, Mona S. Alwahibi, Mohamed Soliman Elshikh, Mohammad Omar Faruque, Shaikh Bokhtear Uddin
Article
Multidisciplinary Sciences
Helena Castro, Tania Cruz, Patricia de Aguiar Amaral, Paula da Silva Cardoso, Ahmed Alsaffar, Patrick Farrell, Ana M. Tomas, James W. Barlow
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)
