Article
Chemistry, Medicinal
Thomas Majer, Keshab Bhattarai, Jan Straetener, Justus Pohlmann, Patrick Cahill, Markus O. Zimmermann, Marc P. Huebner, Marcel Kaiser, Johan Svenson, Michael Schindler, Heike Broetz-Oesterhelt, Frank M. Boeckler, Harald Gross
Summary: Two new ircinianin-type sesterterpenoids, ircinianin lactone B and ircinianin lactone C, were isolated from the marine sponge Ircinia wistarii. The structures were determined using spectroscopic data and computational chemistry. In addition, ircinianin showed moderate antiprotozoal activity.
Article
Biochemistry & Molecular Biology
Clemens Hinteregger, Johanna Dolensky, Werner Seebacher, Robert Saf, Pascal Maeser, Marcel Kaiser, Robert Weis
Summary: 2,4-Diaminopyrimidines and (dialkylamino)azabicyclo-nonanes have activity against protozoan parasites. A series of fused hybrids were synthesized and tested in vitro against malaria tropica and sleeping sickness pathogens. The activities and selectivities of compounds strongly depended on the substitution pattern of both ring systems as well as the position of the nitrogen atom in the bicycles.
Article
Chemistry, Multidisciplinary
Enas Reda Abdelaleem, Mamdouh Nabil Samy, Taha F. S. Ali, Muhamad Mustafa, Mahmoud A. A. Ibrahim, Gerhard Bringmann, Safwat A. Ahmed, Usama Ramadan Abdelmohsen, Samar Yehia Desoukey
Summary: This study investigated the activity of the marine sponge Spongia irregularis and its fractions against HCV. The ethyl acetate fraction showed the highest anti-HCV activity and several compounds were identified. Molecular docking calculations and molecular dynamics simulations demonstrated the strong binding affinity and stability of compound 14 with HCV targets.
Article
Chemistry, Medicinal
Chi-Jen Tai, Atallah F. Ahmed, Chih-Hua Chao, Chia-Hung Yen, Tsong-Long Hwang, Fang-Rong Chang, Yusheng M. Huang, Jyh-Horng Sheu
Summary: A variety of compounds, including polyoxygenated and halogenated labdane, polyoxygenated steroid, rare lactone B ring, and an unsaturated fatty acid, were isolated from the Red Sea sponge. Several novel compounds and previously known compounds were identified, and their cytotoxicity and antibacterial/anti-inflammatory activities were evaluated.
Review
Biochemistry & Molecular Biology
Antonio Moreno-Herrera, Sandra Cortez-Maya, Virgilio Bocanegra-Garcia, Bimal Krishna Banik, Gildardo Rivera
Summary: Parasitic infections caused by various protozoa affect millions of people worldwide annually, with limited pharmacological treatments. Developing new and more effective drugs could be crucial in improving therapy outcomes for parasitic diseases.
CURRENT MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Chi-Jen Tai, Chih-Hua Chao, Atallah F. Ahmed, Chia-Hung Yen, Tsong-Long Hwang, Fang-Rong Chang, Yusheng M. Huang, Jyh-Horng Sheu
Summary: Chemical investigation of the Red Sea sponge Spongia sp. resulted in the discovery of four new compounds, secodinorspongins A-D (1-4), as well as a known compound sponginolide (5). The structures of these compounds and their absolute configurations were elucidated using spectroscopic methods and a comparison of calculated and experimental CD spectra. A possible biosynthetic pathway for compounds 1-4 was proposed. The cytotoxic, antibacterial, and anti-inflammatory activities of compounds 1-5 were also evaluated, with compound 1 showing inhibitory activity against Staphylococcus aureus growth, and compounds 4 and 5 suppressing superoxide-anion generation and elastase release in human neutrophils.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
A-Young Shin, Hyi-Seung Lee, Jihoon Lee
Summary: This study analyzed the methanol extract of a marine sponge Spongia sp. collected from the Philippines, and identified 12 unreported alkaloids. The structure of these alkaloids was determined through NMR and HRMS data interpretation, and their antimicrobial activity against bacteria was evaluated.
Article
Plant Sciences
Barbara Verena Dias Galvao, Carlos Fernando Araujo-Lima, Monica Cristine Pereira dos Santos, Mariana Pulmar Seljan, Eduardo Kennedy Carrao-Dantas, Claudia Alessandra Fortes Aiub, Luiz Claudio Cameron, Mariana Simoes Larraz Ferreira, Edira Castello Branco de Andrade Goncalves, Israel Felzenszwalb
Summary: The study identified 14 phenolic compounds in Plinia cauliflora leaf extract, showing certain anti-Trypanosoma cruzi activity but also cytotoxic effects on liver cell lines.
JOURNAL OF ETHNOPHARMACOLOGY
(2021)
Article
Chemistry, Organic
Wei-Zhuo Tang, Yuan Tian, Shu-Wen Dai, Ao Zhang, Cui-Xian Zhang, Fan Yang, Hui-Min Zhao, Hou-Wen Lin
Summary: Three new merosesquiterpenoids were isolated from a marine sponge and characterized using NMR spectroscopy and HRESIMS. One of the compounds exhibited moderate antifungal activity against three human pathogens.
TETRAHEDRON LETTERS
(2022)
Review
Biochemistry & Molecular Biology
Eyra Ortiz-Perez, Lenci K. Vazquez-Jimenez, Alma D. Paz-Gonzalez, Timoteo Delgado-Maldonado, Alonzo Gonzalez-Gonzalez, Carlos Gaona-Lopez, Antonio Moreno-Herrera, Karina Vazquez, Gildardo Rivera
Summary: Despite the existence of drugs for the treatment of parasitic diseases, they remain a public health issue with varying efficacy and potential serious adverse effects. Over the past two decades, there has been interest in the enzyme carbonic anhydrase (CA) due to its essential role in the life cycle of various parasites. Advances in discovering compounds with potent inhibitory activity suggest that CA is a promising candidate for the development of new antiprotozoal agents.
CURRENT MEDICINAL CHEMISTRY
(2023)
Article
Plant Sciences
Pedro G. Vasquez-Ocmin, Alice Gadea, Sandrine Cojean, Guillaume Marti, Sebastien Pomel, Anne-Cecile Van Baelen, Liliana Ruiz-Vasquez, Wilfredo Ruiz Mesia, Bruno Figadere, Lastenia Ruiz Mesia, Alexandre Maciuk
Summary: In the rural communities of the Alto Amazonas Province in Peru, the use of medicinal Piper species is common practice against parasitic infections. This ethnopharmacological study validated the traditional use of Piper species in Amazonian traditional medicine and identified several species with antiprotozoal activity, suggesting potential for further research. The metabolomic approach proved to be a useful method to identify active compounds in the medicinal plants.
JOURNAL OF ETHNOPHARMACOLOGY
(2021)
Article
Agricultural Engineering
Maryam Akaberi, Zahra Tayarani Najaran, Narjes Azizi, Seyed Ahmad Emami
Summary: Tropical diseases like leishmaniosis pose a major health concern in developing countries, with pathogens developing multiresistance to classic antibiotics, driving the urgent need for new antibiotics. The study focuses on the beneficial effects of Helichrysum spp., comparing their anti-protozoal activities and phytochemical components to tackle infectious diseases in an ongoing project.
INDUSTRIAL CROPS AND PRODUCTS
(2021)
Article
Plant Sciences
Yu-Feng Zhang, Dai-Chun Li, Xiao-Jian Liao, Shi-Hai Xu, Bing-Xin Zhao
Summary: Two new alkaloids, named spongimides A (1) and B (2), along with five known compounds (3-7), were isolated from the marine sponge Spongia sp. The structures of 1 and 2 were determined by spectroscopic methods and X-ray diffraction analysis. Compounds 1, 3, and 4 were the first examples of 2,4-imidazolidinediones isolated from this genus. Furthermore, the cytotoxic and antibacterial activities of compounds 1 and 2 were evaluated.
JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Johanna Dolensky, Clemens Hinteregger, Andreas Leitner, Werner Seebacher, Robert Saf, Ferdinand Belaj, Pascal Maser, Marcel Kaiser, Robert Weis
Summary: N-(Aminoalkyl)azabicyclo[3.2.2]nonanes with terminal tetrazole or sulfonamido partial structure were synthesized. The structures of these compounds were confirmed by various analyses. In vitro experiments showed that the sulfonamide and tetrazole derivatives exhibited significant activities against Plasmodium falciparum and Trypanosoma brucei rhodesiense.
Article
Parasitology
Aline Avila Brustolin, Aquila Carolina Fernandes Herculano Ramos-Milare, Tatiane Franca Perles de Mello, Sandra Mara Alessi Aristides, Maria Valdrinez Campana Lonardoni, Thais Gomes Verzignassi Silveira
Summary: Cinnamaldehyde has anti-Leishmania activity against L. amazonensis, with low toxicity to human cells but moderate toxicity to macrophages. Further research into the use of cinnamaldehyde for treating cutaneous leishmaniasis is recommended.
EXPERIMENTAL PARASITOLOGY
(2022)
Article
Chemistry, Applied
Yan Wang, Muhammad Aamer, Meral Aslay, Bilge Sener, Farooq-Ahmad Khan, Atia-tul Wahab, Atta-ur Rahman, Muhammad Iqbal Choudhary
Summary: A new steroidal alkaloid michainine and nine known compounds were isolated from Fritillaria michailovskyi for the first time, including ribonucleosides, steroids, and fatty acids. Michainine showed positive inhibitory activity on butyrylcholinesterase and non-cytotoxicity against 3T3 cell line.
NATURAL PRODUCT RESEARCH
(2022)
Article
Chemistry, Multidisciplinary
Che-Sheng Hsu, Carlos R. Goncalves, Veronica Tona, Amandine Pons, Marcel Kaiser, Nuno Maulide
Summary: The article presents a method of synthesizing amine compounds using highly electron-deficient iminium ions and highlights its broad applicability through a specific case study.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Article
Chemistry, Medicinal
Sabina Beilstein, Radhia El Phil, Suzanne Sherihan Sahraoui, Leonardo Scapozza, Marcel Kaiser, Pascal Maser
Summary: This article discusses the experimental methods and strategies for selecting drug-resistant parasites, using African trypanosomes as an example. Researchers need to consider factors such as the environmental conditions, life stages, and pressure for selecting drug resistance, while taking into account the laboratory settings.
Article
Biochemistry & Molecular Biology
Ozlem Sevik Kilicaslan, Sylvian Cretton, Luis Quiros-Guerrero, Merveilles A. Bella, Marcel Kaiser, Pascal Maeser, Joseph T. Ndongo, Muriel Cuendet
Summary: This study isolated and identified 16 compounds from P. bicarpellata extracts, including two previously unreported compounds. The absolute configurations of these compounds were determined through analysis of experimental and calculated data. The extracts and compounds were evaluated for their antiprotozoal activity, with tubotaiwine displaying the most significant antiplasmodial activity.
Article
Chemistry, Organic
Blaise Kimbadi Lombe, Lea Winand, Jan Diettrich, Melanie Tobermann, Wolf Hiller, Marcel Kaiser, Markus Nett
Summary: In this study, we report the discovery of massinidine, an aguanidine alkaloid with antiplasmodial activity, from bacteria of the genus Massilia. The biosynthetic genes of massinidine were identified and validated through heterologous expression. Bioinformatic analysis reveals the widespread potential for massinidine biosynthesis in various proteobacteria.
Article
Microbiology
Melissa L. Sykes, Emily K. Kennedy, Kevin D. Read, Marcel Kaiser, Vicky M. Avery
Summary: Chagas disease and Human African Trypanosomiasis (HAT) are parasitic diseases that pose a serious threat to human health. The existing treatment methods are not highly effective, thus there is a need for new therapeutic drugs. Through in vitro assays, compounds with selective activity against these parasites have been identified and evaluated for further research and development.
Article
Plant Sciences
J. Mcebisi Mabuza, Marcel Kaiser, M. Johanna Bapela
Summary: This study evaluated the antiplasmodial and cytotoxic activity of Pappea capensis extracts and fractions, and identified the major compounds responsible for the observed antiplasmodial activity. The results validated the traditional use of P. capensis for malaria treatment and demonstrated the potential for discovering novel antiplasmodial constituents.
JOURNAL OF ETHNOPHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Johanna Dolensky, Clemens Hinteregger, Andreas Leitner, Werner Seebacher, Robert Saf, Ferdinand Belaj, Pascal Maser, Marcel Kaiser, Robert Weis
Summary: N-(Aminoalkyl)azabicyclo[3.2.2]nonanes with terminal tetrazole or sulfonamido partial structure were synthesized. The structures of these compounds were confirmed by various analyses. In vitro experiments showed that the sulfonamide and tetrazole derivatives exhibited significant activities against Plasmodium falciparum and Trypanosoma brucei rhodesiense.
Article
Biochemistry & Molecular Biology
Alireza Mousavi, Parham Foroumadi, Zahra Emamgholipour, Pascal Maser, Marcel Kaiser, Alireza Foroumadi
Summary: The nitro-containing compounds discovered in this study showed high activity against Trypanosoma brucei, making them potential candidates for treating sleeping sickness.
Article
Biochemistry & Molecular Biology
Nina Scheiber, Gregor Blaser, Eva-Maria Pferschy-Wenzig, Marcel Kaiser, Pascal Maser, Armin Presser
Summary: In this study, a series of cyclohexadienone and naphthoquinone derivatives were synthesized using different hypervalent iodine(III) reagents and evaluated for their in vitro antiprotozoal activity. It was found that benzyl naphthoquinone 5c was the most active and selective molecule against T. brucei rhodesiense.
Article
Biochemistry & Molecular Biology
Clemens Hinteregger, Johanna Dolensky, Werner Seebacher, Robert Saf, Pascal Maeser, Marcel Kaiser, Robert Weis
Summary: 2,4-Diaminopyrimidines and (dialkylamino)azabicyclo-nonanes have activity against protozoan parasites. A series of fused hybrids were synthesized and tested in vitro against malaria tropica and sleeping sickness pathogens. The activities and selectivities of compounds strongly depended on the substitution pattern of both ring systems as well as the position of the nitrogen atom in the bicycles.
Article
Chemistry, Multidisciplinary
Werner Seebacher, Marcel Kaiser, Pascal Maeser, Robert Saf, Eva-Maria Pferschy-Wenzig, Robert Weis
Summary: Several 1-benzyl and 1,3-dibenzyl derivatives of tetrahydropyridinylidene salts with varying electron withdrawing substituents at the aromatic residues have been synthesized and investigated for their biological activities and cytotoxicity. Characterization of these compounds was carried out using FT-IR, HRMS and NMR spectroscopy.
MONATSHEFTE FUR CHEMIE
(2023)
Article
Chemistry, Medicinal
Theresa Hermann, Robin Wallner, Johanna Dolensky, Werner Seebacher, Eva-Maria Pferschy-Wenzig, Marcel Kaiser, Pascal Maser, Robert Weis
Summary: The compound MMV030666 in MMV's Malaria Box exhibits multi-stage activity against various strains of Plasmodium falciparum without resistance development. By modifying the structure, a series of compounds were prepared and the relationship between the structure and activity was revealed. Furthermore, the pharmacokinetic and physicochemical parameters were improved.
Article
Multidisciplinary Sciences
Srinivasa P. S. Rao, Matthew K. Gould, Jonas Noeske, Manuel Saldivia, Rajiv S. Jumani, Pearly S. Ng, Olivier Rene, Yen-Liang Chen, Marcel Kaiser, Ryan Ritchie, Amanda Fortes Francisco, Nila Johnson, Debjani Patra, Harry Cheung, Colin Deniston, Andreas D. Schenk, Wilian A. Cortopassi, Remo S. Schmidt, Natalie Wiedemar, Bryanna Thomas, Rima Palkar, Nahdiyah A. Ghafar, Vanessa Manoharan, Catherine Luu, Jonathan E. Gable, Kah Fei Wan, Elmarie Myburgh, Jeremy C. Mottram, Whitney Barnes, John Walker, Charles Wartchow, Natasha Aziz, Colin Osborne, Juergen Wagner, Christopher Sarko, John M. Kelly, Ujjini H. Manjunatha, Pascal Maeser, Jan Jiricek, Suresh B. Lakshminarayana, Michael P. Barrett, Thierry T. Diagana
Summary: Millions of people in Latin America and sub-Saharan Africa are at risk of trypanosomatid infections. Researchers have identified a class of cyanotriazoles (CTs) that have potent trypanocidal activity and can potentially be used for the treatment of Chagas disease and human African trypanosomiasis. These CT compounds act by selectively and irreversibly inhibiting trypanosomal topoisomerase II and stabilizing DNA:enzyme cleavage complexes.
Review
Medicine, Research & Experimental
Sonja Bernhard, Marcel Kaiser, Christian Burri, Pascal Maeser
Summary: After a century of impractical and toxic chemotherapy, a new oral cure called Fexinidazole is now available for human African trypanosomiasis. It has been discovered and developed through extensive screening and testing in both cell cultures and animal models, and has shown promising results in clinical trials conducted in the Democratic Republic of the Congo. With its safety and effectiveness confirmed, Fexinidazole has been endorsed by the European Medicines Agency and included in the new treatment guidelines issued by the WHO.