Article
Chemistry, Medicinal
Huynh Nguyen Khanh Tran, Min Jin Kim, Yeon-Ju Lee
Summary: Eighteen scalarane sesterterpenoids, including eight new derivatives, were isolated from the sponge Hyrtios erectus, showing cytotoxicity against HeLa and MCF-7 cell lines. New derivatives with a gamma-hydroxybutenolide moiety capable of reversible stereoinversion showed different stereochemical behaviors.
Article
Plant Sciences
Di Zhang, Yueying Li, Xiaolei Li, Xiao Han, Zhe Wang, Wenze Zhang, Beibei Dou, Zhongyu Lu, Pinglin Li, Guoqiang Li
Summary: Four new alkaloids were isolated from a marine sponge collected near Xisha Island in the South China Sea. Their structures and absolute configurations were determined, and three of them showed hepatoprotective activity in vivo.
JOURNAL OF NATURAL PRODUCTS
(2022)
Article
Chemistry, Medicinal
Heba A. Abou-Taleb, Ahmed M. Sayed, Hesham Refaat, Faisal Alsenani, Eman Alaaeldin, Fatma A. Mokhtar, Usama Ramadan Abdelmohsen, Nourhan Hisham Shady
Summary: The study revealed the potential anti-cancer activity of Hyrtios erectus extract within niosomes and established a metabolic product-target-cancer disease network through computational chemical analysis, investigating the mechanisms of its anti-cancer effects.
Article
Chemistry, Medicinal
Hao-Bing Yu, Bo Hu, Zhe Ning, Ying He, Xiao-Ling Men, Zi-Fei Yin, Bing-Hua Jiao, Xiao-Yu Liu, Hou-Wen Lin
Summary: Eight new scalarane sesterterpenes were isolated from a marine sponge collected from the South China Sea. Their structures were determined through analysis, and these compounds showed antibacterial and cytotoxic activity.
Article
Biochemistry & Molecular Biology
Buyng Su Hwang, Yong Tae Jeong, Sangbum Lee, Eun Ju Jeong, Jung-Rae Rho
Summary: Densazalin, a polycyclic alkaloid isolated from a marine sponge collected in Korea, possesses a unique structure and exhibits cytotoxic activity against two human tumor cell lines.
Article
Chemistry, Applied
Kajal Chakraborty, Prima Francis
Summary: The bioactivity-guided chromatographic purification of the solvent extract of marine sponge Hyrtios erectus led to the discovery of three undescribed cyanthiwigin-type diterpenoids, erectcyanthins A-C, with erectcyanthin B showing promising potential as a pharmaceutical lead due to its comparable inhibition activity against 3-hydroxy-3-methylglutaryl-coenzyme A reductase with atorvastatin, as well as greater antioxidant and anti-inflammatory properties than other analogues. The study also highlighted the linear relationship between the anti-dyslipidemic activity of erectcyanthins and their electronic parameters and balanced hydrophilic-lipophilic properties.
NATURAL PRODUCT RESEARCH
(2022)
Article
Environmental Sciences
Qiong Wu, Natalie Eisenhardt, Stephanie Shaw Holbert, Joseph R. Pawlik, John R. Kucklick, Walter Vetter
Summary: Halogenated natural products (HNPs) with similar properties to anthropogenic persistent organic pollutants (POPs) were identified in the marine sponge Hyrtios proteus from The Bahamas. Further analysis on octopus from the same area showed similar HNPs. The study indicates that Caribbean marine organisms harbor relatively high concentrations of HNPs.
MARINE POLLUTION BULLETIN
(2021)
Article
Biochemistry & Molecular Biology
Xin-Lian Liu, Ya-Fang Ding, Shu-Ping Wang, Li Liu, Jie Wang, Fan Yang
Summary: Three new polyacetylenes, pellynols P (1), Q (2), and R (3) were isolated from the marine sponge Petrosia sp., along with the known compound pellynol H (4). These compounds exhibited potent cytotoxicity against human hepatocellular carcinoma HepG2, human melanoma A375, and human colorectal carcinoma HT29 cell lines with IC50 values ranging from 1.4 to 4.4 μM.
CHEMISTRY & BIODIVERSITY
(2022)
Article
Biochemistry & Molecular Biology
Junya Mukomura, Hiroki Nonaka, Hiromasa Sato, Maho Kishimoto, Masayoshi Arai, Naoyuki Kotoku
Summary: This study synthesized and evaluated simplified analogs of marine sponge-derived alkaloid to discover novel anti-mycobacterial substances. The ring truncation effectively reduced cytotoxicity, and the N-(2-arylethyl)quinolin-3-amine skeleton was identified as a promising scaffold for anti-mycobacterial lead compounds.
Article
Chemistry, Organic
Philipp Moosmann, Tohru Taniguchi, Kazuo Furihata, Hiroaki Utsumi, Yuji Ise, Yasuhiro Morii, Nobuhiro Yamawaki, Tomohiro Takatani, Osamu Arakawa, Shigeru Okada, Shigeki Matsunaga
Summary: Myrindole A, a bis-indole alkaloid isolated from a deep-sea sponge, had a complex structure that was ultimately determined through a combination of experiments and spectral comparison. It showed antimicrobial activity against both Gram-positive and Gram-negative bacteria.
Article
Chemistry, Multidisciplinary
Nguyet A. Nguyen, Zhenjian Lin, Ipsita Mohanty, Neha Garg, Eric W. Schmidt, Vinayak Agarwal
Summary: Marine sponges are a rich source of bioactive compounds produced by bacteria symbiotically associated with the sponge host. A gene cluster encoding a cryptic ribosomally synthesized and post-translationally modified peptide (RiPP) is conserved in sponge microbiomes across different oceans, indicating a unique conservation pattern compared to non-symbiotic bacteria. Enzymes responsible for halogenation and cyclodehydration reactions in RiPPs have been discovered in sponge microbiomes, showing diverse interactions with substrate peptides.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2021)
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, Medicinal
Shamsunnahar Khushi, Angela A. Salim, Ahmed H. Elbanna, Laizuman Nahar, Robert J. Capon
Summary: Thorectandra choanoides (CMB-01889) was identified as a potential source of new chemistry from marine sponge extracts in southern Australia, leading to the discovery of a new alkaloid. Detailed spectroscopic analysis and biosynthetic origins shed light on pharmaceutical potential, with insights into the specificity of IDO substrates and the reactive transformation of Michael acceptors.
Review
Biochemistry & Molecular Biology
Vinita Manimaran Nadar, Selvambigai Manivannan, Rajasekar Chinnaiyan, Muthusamy Govarthanan, Kumar Ponnuchamy
Summary: In recent years, researchers have been interested in biological macromolecules due to their various biological uses. Marine sponges, as multicellular heterotrophic organisms, produce secondary metabolites for defense against predators, biofouling, and microbial diseases. Extracted from marine sponges, over 5,000 marine natural compounds, including aaptamine, have been studied extensively and show promise for various biological purposes, such as cancer treatment and protease inhibition.
CHEMICAL BIOLOGY & DRUG DESIGN
(2022)
Article
Chemistry, Medicinal
Oleg A. Tryapkin, Alexey V. Kantemirov, Sergey A. Dyshlovoy, Vladimir S. Prassolov, Pavel V. Spirin, Gunhild von Amsberg, Maria A. Sidorova, Maxim E. Zhidkov
Summary: Fascaplysin is a marine alkaloid that has diverse and potent biological activity, making it a promising lead drug candidate. It has the potential to be an effective anticancer agent due to its ability to inhibit CDK4 and induce intrinsic apoptosis in cancer cells. However, its high toxicity caused by DNA intercalation and the limited methods for synthesis of derivatives hinder the studies on structural optimization.
Article
Plant Sciences
Yu-Ting Li, Xiao Feng, Yunjiang Feng, Yuanyuan Cheng, Li-Wen Tian
Summary: Four new furostanol saponins and a new pregane-type saponin, along with six known steroidal saponins, were isolated from the rhizomes of Smilax china. Compound 1 showed strong inhibitory activity against proinflammatory mediators.
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
Marine & Freshwater Biology
Saul Gonzalez-Murcia, Merrick Ekins, Tom C. L. Bridge, Christopher N. Battershill, Geoffrey P. Jones
Summary: Substratum preferences and contact interactions among sessile organisms play a crucial role in shaping the structure of benthic communities on coral reefs. This study investigated the substratum preferences and interactions of sponges in coastal coral reefs, revealing their high association with dead coral, coral rubble, and calcium carbonate rock. The most frequent interactions were observed with algae, corals, and crustose coralline algae, with sponges often overgrowing their spatial competitors. Our findings highlight the importance of substratum preferences and interactions in influencing community dynamics on coral reefs.
Article
Chemistry, Medicinal
Chao Wang, Thanh Nguyen, Xinzhou Yang, George D. Mellick, Yunjiang Feng
Summary: This research investigated the chemical constituents of A. sieboldii var. seoulense extract and found that several active small molecules exhibited moderate perturbation to cellular compartments related to Parkinson's Disease. The results supported the traditional application of Xixin in the treatment of PD.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(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
Zoology
Merrick Ekins, John N. A. Hooper
Summary: This research discovered three new species of carnivorous sponges from the Cladorhizidae family in the Great Barrier Reef, Queensland, Australia: Abyssocladia falkor sp. nov., Abyssocladia jeanvaceleti sp. nov., and Axoniderma wanda sp. nov. These specimens were collected by ROV during the FK200802-Seamounts, Canyons & Reefs of the Coral Sea Cruise on the RV Falkor from the Schmidt Ocean Institute. Additionally, the presence of two complete specimens enabled the redescription of two previously known Australian species of carnivorous sponge (Chondrocladia (Chondrocladia) zygainadentonis Ekins et al., 2020a and Asbestopluma (Asbestopluma) maxisigma Ekins et al., 2020a), which were previously only based on incomplete specimens from the East coast of Australia.
Article
Zoology
Mohammed Abdel Latif Ezz El-Arab, Merrick Ekins
Summary: Ophlitaspongia (?) arbuscula Row, 1911 and Ophlitaspongia (?) horrida Row, 1911 from the Red Sea have been re-described and illustrated using new specimens, showing the variation within the species. Examination of the type and fresh material suggests that both species are unlikely to belong to the genus Ophlitaspongia and are most likely assigned to Clathria (Clathria) Schmidt, 1862 due to the presence of echinating (acantho)styles and a reticulate skeleton.
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
Zoology
Merrick Ekins, Dirk Erpenbeck, Cecile Debitus, Sylvain Petek, Tepoerau Mai, Gert Woerheide, John N. A. Hooper
Summary: This study examines the taxonomy of sponge specimens with unique chemistry collectively known as Fascaplysinopsis reticulata. The results revealed that Fascaplysinopsis reticulata is a species complex comprising the genus Fascaplysinopsis, as well as two new genera: Skolosachlys gen. nov. and Rubrafasciculus gen. nov. Several new species were described within these genera.
Article
Zoology
Merrick Ekins, Soraya Baker, John N. A. Hooper
Summary: Four new species of encrusting Hamacantha (Vomerula) were discovered in the bathyal depths of seamounts in southeast Australia, along with a re-description of a previously known species from New Caledonia. A comparison table of all known species of H. (Vomerula) was provided, bringing the total number of known species in the subgenus to 26. This study also marks the first record of the genus Hamacantha in the Australian Exclusive Economic Zone.
Article
Plant Sciences
Gugulethu P. Khumalo, Thanh Nguyen, Ben-Erik Van Wyk, Yunjiang Feng, Ian E. Cock
Summary: In this study, the immunomodulatory and anti-inflammatory properties of bark from ten important southern African plants were evaluated. It was found that most of these plants exhibited cytokine inhibitory effects, providing new insights into the mechanisms by which they regulate inflammation.
JOURNAL OF ETHNOPHARMACOLOGY
(2024)
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
