Article
Chemistry, Multidisciplinary
Hong-Quan Xu, Huan Xiao, Jin-Hui Bu, Yan-Feng Hong, Yu-Hong Liu, Zi-Yue Tao, Shu-Fan Ding, Yi-Tong Xia, E. Wu, Zhen Yan, Wei Zhang, Gong-Xing Chen, Feng Zhu, Lin Tao
Summary: The study introduces a comprehensive database for endophytic microorganism natural products (EMNPD), which aims to meet the increasing demand for data mining and sharing in this field. This database provides a wealth of natural product data and links to other databases, facilitating drug discovery and exploration of bioactive substances.
JOURNAL OF CHEMINFORMATICS
(2023)
Review
Chemistry, Medicinal
Junjie Li, Rui Zhao, Peiran Miao, Fengfeng Xu, Jiahao Chen, Xiaoying Jiang, Zi Hui, Liwei Wang, Renren Bai
Summary: This review provides a comprehensive overview of the diverse anti-inflammatory activities of flavonoids and elucidates the underlying pathways in mediating inflammation. It includes a systematic classification and detailed statistical analysis of flavonoids, related anti-inflammatory targets, and in vitro and in vivo test models. The review aims to provide practical information and potential leads for researchers engaged in natural products and anti-inflammatory drug discovery.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Pharmacology & Pharmacy
Jia Fu, Wei Qin, Lu-Qi Cao, Zhe-Sheng Chen, Hui-Ling Cao
Summary: This review summarizes the applications and immobilization methods of receptor chromatography, which is widely used for high-throughput separation and accurate drug screening. The review focuses on screening active compounds in natural products, as well as the design and application of receptor chromatography in drug-receptor interactions.
DRUG DISCOVERY TODAY
(2023)
Review
Biochemistry & Molecular Biology
Li-Juan Deng, Wei-Qing Deng, Shu-Ran Fan, Min-Feng Chen, Ming Qi, Wen-Yu Lyu, Qi Qi, Amit K. Tiwari, Jia-Xu Chen, Dong-Mei Zhang, Zhe-Sheng Chen
Summary: Abnormal N6-methyladenosine (m6A) modification is closely related to cancer development, and finding targeted anticancer drugs is important. Traditional herbs and computer-synthesized compounds are reasonable sources for these drugs. Artificial intelligence has advantages in discovering m6A-targeting anticancer drugs.
Review
Nutrition & Dietetics
Ahyeon Kim, Jiwon Ha, Jeongeun Kim, Yongmin Cho, Jimyung Ahn, Chunhoo Cheon, Sung-Hoon Kim, Seong-Gyu Ko, Bonglee Kim
Summary: Natural products have potential effects in treating pancreatic cancer, particularly through inducing cell apoptosis. Plant extracts are the main focus in the research, while some natural products exhibit multifunctional properties.
Article
Biodiversity Conservation
Steve Carver, Ian Convery, Sally Hawkins, Rene Beyers, Adam Eagle, Zoltan Kun, Erwin Van Maanen, Yue Cao, Mark Fisher, Stephen R. Edwards, Cara Nelson, George D. Gann, Steve Shurter, Karina Aguilar, Angela Andrade, William J. Ripple, John Davis, Anthony Sinclair, Marc Bekoff, Reed Noss, Dave Foreman, Hanna Pettersson, Meredith Root-Bernstein, Jens-Christian Svenning, Peter Taylor, Sophie Wynne-Jones, Alan Watson Featherstone, Camilla Flojgaard, Mark Stanley-Price, Laetitia M. Navarro, Toby Aykroyd, Alison Parfitt, Michael Soule
Summary: Recent interest in the concept of rewilding has sparked confusion among experts, but a unified definition and guiding principles have been established through research and workshops to clarify the concept and improve its effectiveness. Understanding the context of rewilding projects and careful site-specific interpretations are crucial for success in achieving rewilding goals.
CONSERVATION BIOLOGY
(2021)
Review
Biochemistry & Molecular Biology
Yuin Chang, Keng Yoon Yeong
Summary: Since the discovery of the regulatory roles of sirtuins in various pathological processes, there has been a growing interest in researching sirtuins, particularly in the development of modulators. Natural modulators have therapeutic potential in treating various diseases, and this review provides insights into their molecular mechanisms, therapeutic benefits, as well as the challenges and future prospects in drug discovery.
CURRENT MEDICINAL CHEMISTRY
(2021)
Review
Chemistry, Analytical
Lin-Sen Qing, Tian-Tian Wang, Han-Yue Luo, Jia-Lan Du, Run-Yue Wang, Pei Luo
Summary: Natural products are still the main source of drug candidates in new drug discovery. Microfluidic technology offers a rapid and efficient research system for natural products through miniaturizing the analytical process onto a single chip. This review comprehensively summarizes the design and applications of microfluidic devices in analyzing, evaluating, and studying natural products, as well as discussing limitations and future research directions.
TRAC-TRENDS IN ANALYTICAL CHEMISTRY
(2023)
Review
Biochemistry & Molecular Biology
Zhihong Xu, Barrett Eichler, Eytan A. A. Klausner, Jetty Duffy-Matzner, Weifan Zheng
Summary: Natural products and their derivatives have shown to be effective drug candidates against various diseases. This paper reviews potent anticancer, anti-HIV, antibacterial, and antimalarial drugs or lead compounds discovered mainly from 2016 to 2022, as well as computer-assisted techniques used in designing new structures based on available natural products.
Review
Biochemistry & Molecular Biology
K. L. T. Dilrukshi Jayawardene, Enzo A. Palombo, Peter R. Boag
Summary: Parasitic nematodes infect a wide range of organisms and have significant impact on human health and agriculture. The main method of controlling these parasites is through anthelmintic drugs, but there is limited selection in the market and resistance is a major issue. Therefore, the development of new anthelmintics is crucial for sustainable parasitic control.
Review
Chemistry, Medicinal
Bhawna Chopra, Ashwani Kumar Dhingra
Summary: Natural products have been used in folklore for centuries for treating various ailments, with plant-derived products recognized as a source of therapeutic agents and structural diversity. After small modifications, natural molecules can offer better pharmacological potential as new molecular entities.
PHYTOTHERAPY RESEARCH
(2021)
Review
Biotechnology & Applied Microbiology
Atanas G. Atanasov, Sergey B. Zotchev, Verena M. Dirsch, Claudiu T. Supuran
Summary: Natural products and their analogues have historically played a significant role in pharmacotherapy, however, they also present challenges. Recent technological and scientific developments are addressing these challenges and revitalizing interest in natural products as drug leads, particularly for combating antimicrobial resistance.
NATURE REVIEWS DRUG DISCOVERY
(2021)
Article
Biochemistry & Molecular Biology
Mahmoud A. A. Ibrahim, Khlood A. A. Abdeljawaad, Alaa H. M. Abdelrahman, Mohamed-Elamir F. Hegazy
Summary: The study utilized in-silico drug discovery approaches to identify nine potent natural-like products as potential inhibitors of SARS-CoV-2 main protease. Among these, four derivatives showed high binding affinities and stability in MD simulations, indicating their potential as drug candidates for COVID-19.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2021)
Article
Cell Biology
Seyun Kim, Seol-Wa Lim, Jiyeon Choi
Summary: Natural products (NPs) have played a significant role in drug discovery and treatment due to their chemical diversity and favorable properties. Recent scientific and technological advances, such as metabolomics tools, chemoproteomics approaches, and artificial intelligence-based computation platforms, have provided new opportunities for exploring and utilizing NPs. However, there are still challenges in NP-driven drug discovery that require the development of novel strategies to overcome.
ANIMAL CELLS AND SYSTEMS
(2022)
Article
Chemistry, Medicinal
Jian-Chuan Liu, Jian Yang, Shu-Xin Lei, Ming-Fan Wang, Yan-Ni Ma, Rui Yang
Summary: In this study, a series of new biphenyl compounds based on natural biphenyl phytoalexins were designed, synthesized, and evaluated for their antifungal activities against four invasive fungi. Promising compounds with remarkable antifungal activity were discovered through modifying the two benzene rings of a well-known biphenyl phytoantitoxin. Notably, compounds 23a, 23e, and 23h exhibited potent activities and a broad antifungal spectrum, with low minimum inhibitory concentrations (MICs) and comparable potency to the positive control amphotericin B against Cryptococcus neoformans. Preliminary mechanism studies suggested that compound 23h exerts its rapid fungicidal activity by disrupting the fungal cell membrane. Moreover, compound 23h displayed significant inhibition against virulence factors of Cryptococcus neoformans, low toxicity to normal human cells, and favorable pharmacokinetic and drug-like properties. These results highlight the bright and promising strategy of developing new antifungal candidates derived from natural phytoalexins.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Cell Biology
Daming Zuo, Yu Chen, Jian-piao Cai, Hao-Yang Yuan, Jun-Qi Wu, Yue Yin, Jing-Wen Xie, Jing-Min Lin, Jia Luo, Yang Feng, Long-Jiao Ge, Jia Zhou, Ronald J. Quinn, San-Jun Zhao, Xing Tong, Dong-Yan Jin, Shuofeng Yuan, Shao-Xing Dai, Min Xu
Summary: The twenty-first century has witnessed more than ten major epidemics or pandemics, including the devastating COVID-19. There is an urgent need for novel antiviral drugs with broad-spectrum coverage. This study reports a new broad-spectrum antiviral compound called PAC5. Oral administration of PAC5 was found to eliminate HBV cccDNA and reduce antigen load in mouse models of HBV infection. Additionally, PAC5 significantly decreased viral loads and attenuated lung inflammation in a hamster model of SARS-CoV-2 omicron (BA.1) infection. The mechanism behind these effects involves activation of hnRNPA2B1 and the TBK1-IRF3 pathway, leading to the production of antiviral type I IFNs. These findings suggest that PAC5 could be a promising option for dealing with emerging infectious diseases.
Article
Chemistry, Organic
Kah Yean Lum, Jonathan M. White, Daniel J. G. Johnson, Vicky M. Avery, Rohan A. Davis
Summary: Nine new fluorinated analogues were synthesised using late-stage functionalisation on the Open Source Malaria (OSM) triazolopyrazine scaffold. The structures of all analogues were characterised and their inhibitory activity against Plasmodium falciparum and cytotoxicity against a human embryonic kidney cell line were tested. Some compounds showed moderate antimalarial activity, while none displayed cytotoxicity at high concentrations. Substitution of CF3 and CF2H moieties at the C-8 position significantly reduced antimalarial activity, while incorporation of a CF2Me group completely abolished the effect.
BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Plant Sciences
Chen Zhang, Kah Yean Lum, Aya C. Taki, Robin B. Gasser, Joseph J. Byrne, Luis J. Montaner, Ian Tietjen, Vicky M. Avery, Rohan A. Davis
Summary: The study focused on the purification and synthesis of a bioactive compound derived from Eremophila microtheca. A library of carbamate-based compounds was generated using the synthesized compound as a scaffold, and their activities against parasites, malaria, and HIV were evaluated. The results showed promising antiparasitic, antimalarial, and antiviral activities of certain compounds.
JOURNAL OF NATURAL PRODUCTS
(2023)
Article
Chemistry, Medicinal
Folake A. Egbewande, Brett D. Schwartz, Sandra Duffy, Vicky M. Avery, Rohan A. Davis
Summary: The incorporation of bromine, iodine or fluorine into the tricyclic core structure of thiaplakortone A (1), a potent antimalarial marine natural product, was achieved. Although yields were low, a small library of thiaplakortone A analogues (3-11) was synthesised using a Boc-protected thiaplakortone A (2) as a scaffold for late-stage functionalisation. The antimalarial activity of the new analogues was evaluated, with the mono-brominated analogue (compound 5) showing the best activity against both drug-sensitive and drug-resistant strains of Plasmodium falciparum.
Article
Oncology
Alanah Varricchio, Sidra Khan, Zoe K. Price, Rohan A. Davis, Sunita A. Ramesh, Andrea J. Yool
Summary: Glioblastoma is a highly lethal brain tumor with invasive spreading capabilities. This study found that blocking glutamate receptors and aquaporin-1 channels can limit the motility of tumor cells without causing harm to normal brain cells. Using combination therapy can focus the effects on cancer cells while minimizing off-target effects.
Article
Chemistry, Medicinal
Yushu Gu, Miaomiao Liu, Bart L. Staker, Garry W. Buchko, Ronald J. Quinn
Summary: SARS-CoV-2 is the pathogen responsible for COVID-19 and the global pandemic. Repurposing clinically approved drugs, gallic acid was identified as a compound that tightly binds to nsp7, a component essential for viral replication. The identification of the gallic acid-binding site may enable the development of a SARS-CoV-2 therapeutic through virtual docking and other strategies.
ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE
(2023)
Article
Biotechnology & Applied Microbiology
Rohan A. Davis, Gunnar Cervin, Karren D. Beattie, Topul Rali, Marilyne Fauchon, Claire Hellio, Lovisa Bodin Akerlund, Henrik Pavia, Johan Svenson
Summary: This study investigates the antifouling potential of polyphenolic resveratrol multimers isolated from two Anisoptera species found in the Papua New Guinean rainforest. The compounds showed inhibitory effects on marine microfoulers and barnacle cyprids, with (-)-hopeaphenol demonstrating strong inhibitory effects against both microalgal and bacterial adhesion. Resveratrol displayed lower antifouling activity and higher toxicity against MCR-5 fibroblasts. This study highlights the potential of natural products as a valuable source for the discovery of novel antifouling agents with low toxicity.
Article
Biochemistry & Molecular Biology
Simon H. Apte, Penny L. Groves, Maxine E. Tan, Viviana P. Lutzky, Tharushi de Silva, Joshua N. Monteith, Stephanie T. Yerkovich, Brendan J. O'Sullivan, Rohan A. Davis, Daniel C. Chambers
Summary: Idiopathic pulmonary fibrosis is a common and deadly lung disease with unknown cause. Recent advances in genomic research have identified potential therapeutic compounds for lung fibrosis, including a compound isolated from an Australian rainforest plant with antifibrotic properties.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Tam M. T. Tran, Russell S. Addison, Rohan A. Davis, Bernd H. A. Rehm
Summary: The sponge-derived natural products ianthelliformisamines A-C can work synergistically with ciprofloxacin to reduce the minimum inhibitory concentration (MIC) of Pseudomonas aeruginosa biofilms. Ianthelliformisamine C exhibits bactericidal effects on both free-living and biofilm populations of various strains, including the clinically relevant mucoid variant.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Multidisciplinary
Ka Ho Chow, Ronald J. Quinn, Ian D. Jenkins, Elizabeth H. Krenske
Summary: Oxazolidinones are commonly used as chiral auxiliaries in asymmetric synthesis. The selectivity of removing chiral auxiliaries using different nucleophiles, such as LiOOH, LiOBn, LiSBn, and LiOH, is found to be dependent on the decomposition barrier of the formed intermediates. Mechanistic studies are conducted using DFT calculations to understand the origin of selectivity.
AUSTRALIAN JOURNAL OF CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Yushu Gu, Miaomiao Liu, Bart L. Staker, Garry W. Buchko, Ronald J. Quinn
Summary: SARS-CoV-2 is the cause of COVID-19 and the global pandemic. Repurposing approved drugs can accelerate clinical treatments. Gallic acid was found to bind to the viral protein nsp7, offering potential for SARS-CoV-2 therapeutic development.
ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE
(2023)
Review
Biochemistry & Molecular Biology
Anthony R. Carroll, Brent R. Copp, Rohan A. Davis, Robert A. Keyzers, Michele R. Prinsep
Summary: This review covers the literature on marine natural products (MNPs) published in 2020, with 757 citations referring to compounds isolated from a variety of marine organisms. The emphasis is on new compounds, their biological activities, source organisms, and country of origin. The review also includes relevant reviews, biosynthetic studies, and syntheses that led to structural revisions, as well as a meta analysis of bioactivity data on new MNPs reported in the past five years.
NATURAL PRODUCT REPORTS
(2023)
Article
Chemistry, Multidisciplinary
Robert J. Young, Sabine L. Flitsch, Michael Grigalunas, Paul D. Leeson, Ronald J. Quinn, Nicholas J. Turner, Herbert Waldmann
Summary: This article reviews the case for focusing on Nature in drug discovery, specifically biomimetic molecules and natural products. It discusses the declining natural product-likeness of licensed drugs and the logic of seeking new bioactive agents with enhanced natural mimicry. The article also explores the potential for computational guidance in designing tailored molecules and emphasizes the advantages of organic/biological structures.
Review
Biochemistry & Molecular Biology
Miaomiao Liu, Alexander P. Martyn, Ronald J. Quinn
Summary: Natural products have the ability to recognize protein surfaces and have advantages in drug delivery. PROTACs, a novel protein degradation approach, have potential applications in the field of natural products. This review summarizes the chemical synthesis and challenges of natural product-based PROTACs, as well as methods for detecting their mechanism of action.
NATURAL PRODUCT REPORTS
(2022)
Review
Biochemistry & Molecular Biology
Anthony R. Carroll, Brent R. Copp, Rohan A. Davis, Robert A. Keyzers, Michele R. Prinsep
Summary: This review summarizes the literature on marine natural products (MNPs) published in 2020, covering a wide range of compounds isolated from various marine organisms. The focus is on new compounds discovered in 2020, including their biological activities, source organisms, and country of origin. The review also includes a meta analysis of bioactivity data for new MNPs reported in the past five years.
NATURAL PRODUCT REPORTS
(2022)