Article
Plant Sciences
Emmanuel O. Adeyoju, Clement O. Ajayi, Awodayo O. Adepiti, Anthony A. Elujoba
Summary: This study compared the antimalarial activity of methanol and water extracts of MAMA Powder against Plasmodium berghei-infected mice, finding that the water extract exhibited higher efficacy and can be optimized for chloroquine-resistant malaria, aiding in the production of various dosage forms.
JOURNAL OF ETHNOPHARMACOLOGY
(2022)
Article
Plant Sciences
Hae Soo Yun, Sylvatrie-Danne Dinzouna-Boutamba, Sanghyun Lee, Zin Moon, Dongmi Kwak, Dong-Il Chung, Yeonchul Hong, Man Hee Rhee, Youn-Kyoung Goo
Summary: The extract of Petasites japonicus shows potential antimalarial effects by inhibiting the proliferation of Plasmodium parasites and improving hematological parameters. These effects may be attributed to the inhibition of platelet activation related to attenuated glycoprotein VI downstream signaling.
Article
Microbiology
Hae-Soo Yun, Sylvatrie-Danne Dinzouna-Boutamba, Sanghyun Lee, Zin Moon, Dongmi Kwak, Man-Hee Rhee, Dong-Il Chung, Yeonchul Hong, Youn-Kyoung Goo
Summary: The study evaluated the antimalarial activity of Ranunculus japonicus extract against different strains of malaria parasites, showing significant inhibition of both chloroquine-sensitive and resistant strains. In infected mice, the extract demonstrated potent antimalarial activity with improved hepatic, renal, and hematologic parameters, indicating no apparent toxicity.
Article
Biochemistry & Molecular Biology
Ali Mijoba, Esteban Fernandez-Moreira, Nereida Parra-Gimenez, Sandra Espinosa-Tapia, Zuleyma Blanco, Hegira Ramirez, Jaime E. Charris
Summary: A series of benzocycloalkanone derivatives were synthesized as potential antimalarial and antitrypanosomal agents. The compounds were prepared through direct coupling of preformed 4-substituted benzaldehyde and indanone or tetralone substitutes using aldol condensation. Only three compounds showed significant antimalarial activity, while all compounds exhibited marginal activity as trypanocidals. Further investigation is warranted for this new class of Michael acceptor agents.
Article
Multidisciplinary Sciences
Gizachew Kassahun Bizuneh, Getnet Tadege, Betelhem Sirak, Abyot Endale Gurmu, Betelhem Anteneh Adamu, Aschalew Mulatu Tefera, Yeniewa Kerie Anagaw
Summary: This study aimed to determine the in vivo antimalarial activity of the 80% methanol extract and solvent fractions of Cucumis ficifolius roots against Plasmodium berghei infection in mice. The results showed that the root extract of Cucumis ficifolius had a promising suppression of parasitemia and potential antiplasmodial activity.
Article
Integrative & Complementary Medicine
Sakaewan Ounjaijean, Voravuth Somsak
Summary: This study evaluated the antimalarial potential of combination dihydroartemisinin (DHA) and Gymnema inodorum leaf extract (GIE) therapy against Plasmodium berghei in a mouse model. The results showed that the 60/40 ratio of DHA and GIE demonstrated significantly higher antimalarial activity and enhanced the antimalarial effects of DHA.
BMC COMPLEMENTARY MEDICINE AND THERAPIES
(2023)
Article
Pharmacology & Pharmacy
Hegira Ramirez, Jose Dominguez, Esteban Fernandez-Moreira, Juan Rodrigues, Miguel Rodriguez, Jaime E. Charris
Summary: The study successfully synthesized a new series of chalcones and evaluated their antimalarial efficacy. Some of the compounds showed high inhibitory activity and potentially slow down the progression of malaria through inhibition of hemozoin formation. The study also discussed critical aspects of the structure-activity relationship.
Article
Pharmacology & Pharmacy
Jerome Dormoi, Remy Amalvict, Mathieu Gendrot, Bruno Pradines
Summary: The untreated malaria can quickly progress to severe forms, and drug resistance poses a threat to malaria protection efforts worldwide. Therefore, the development of new chemotherapy is necessary. This study contributes new data on the use of methylene blue (MB) in combination with common antimalarial drugs for the treatment of malaria and cerebral malaria. The results show that the combination of MB and AQ is a good candidate for preventing cerebral malaria.
Article
Medicine, Research & Experimental
Atharva R. Bhide, Mansi Suri, Sapna Katnoria, Sukhbir Kaur, Yugandhara B. Jirwankar, Vikas D. Dighe, Anil B. Jindal
Summary: This study evaluated the pharmacokinetics, biodistribution, and antimalarial efficacy of artemether-loaded polymeric nanorods. The results showed that nanorods had higher plasma concentration and lower elimination rate compared to nanospheres. In vitro and in vivo experiments demonstrated that nanorods had better parasitic inhibition and chemosuppression, leading to a higher survival rate in malaria-infected mice compared to free artemether.
MOLECULAR PHARMACEUTICS
(2023)
Article
Biochemistry & Molecular Biology
Fernanda Valerio Lopes, Pedro Henrique Fazza Stroppa, Juliane Aparecida Marinho, Roberta Reis Soares, Lara de Azevedo Alves, Priscila Vanessa Zabala Capriles Goliatt, Clarice Abramo, Adilson David da Silva
Summary: This study evaluated the antimalarial activity of triazole derivatives, with compound 5 showing promising potential for further development in antimalarial chemotherapy. In vitro and in vivo studies showed that compound 5 had significant parasitemia suppression and minimal cytotoxicity, making it a leading candidate for future research in antimalarial drug development.
CHEMICO-BIOLOGICAL INTERACTIONS
(2021)
Article
Plant Sciences
Stephenie C. Alaribe, Akolade R. Oladipupo, Goodness C. Uche, Maryan U. Onumba, Duncan Ota, Olufunsho Awodele, Wellington A. Oyibo
Summary: The study evaluated the antimalarial activity of a polyherbal mixture and its constituent plants, showing significant antiplasmodial effects in various assays. While the herbal mixtures demonstrated parasite suppression and prophylaxis comparable to positive controls, they had lower parasite clearance rates. The combination of herbal plants may produce synergistic or additive effects against malaria, suggesting their use as traditional remedies warrant further investigation for clinical usefulness.
JOURNAL OF ETHNOPHARMACOLOGY
(2021)
Article
Microbiology
Fidelia Ijeoma Uche, Xiaozhen Guo, Jude Okokon, Imran Ullah, Paul Horrocks, Joshua Boateng, Chenggang Huang, Wen-Wu Li
Summary: This study investigates the in vitro and in vivo antiplasmodial activities of BBIQ alkaloids and their analogues, showing promising results with significant anti-parasitic effects at low concentrations. Cycleanine and its semisynthetic analogues demonstrate improved potency and selectivity, with potential as leads for further drug development.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Article
Infectious Diseases
Loeki Enggar Fitri, Agustina Tri Endharti, Hafshah Yasmina Abidah, Alif Raudhah Husnul Khotimah, Heni Endrawati
Summary: The study aimed to investigate the effectiveness and cytotoxicity of fractions 14 and 36K of Streptomyces hygroscopicus subsp. Hygroscopicus metabolite extract as antimalarial compounds against Plasmodium berghei in vitro. The results showed that both fractions have antimalarial activity, with fraction 14 having higher potency.
INFECTION AND DRUG RESISTANCE
(2023)
Article
Infectious Diseases
John Oludele Olanlokun, Mercy Toluwase Ekundayo, Oluwakemi Ebenezer, Neil Anthony Koorbanally, Olufunso Olabode Olorunsogo
Summary: The African Mistletoe plant has anti-malarial properties, with its hexane fraction showing excellent efficacy against both susceptible and resistant strains of malaria parasites. It reduces parasite load, improves hematological parameters, increases heme, and decreases hemozoin content in infected mice. Friedelan-3-one, a major component, may be responsible for this activity.
INFECTION AND DRUG RESISTANCE
(2021)
Article
Biology
Oluwole Solomon Oladeji, Abimbola Peter Oluyori, Adewumi Oluwasogo Dada
Summary: Morinda lucida, a plant traditionally used to treat malaria in Nigeria, has shown antiplasmodial properties in this study. The leaves and bark of Morinda lucida could be potential sources for developing effective antimalarial drugs.
SAUDI JOURNAL OF BIOLOGICAL SCIENCES
(2022)
Article
Chemistry, Medicinal
David S. P. Cardoso, Annamaria Kincses, Marta Nove, Gabriella Spengler, Silva Mulhovo, Joao Aires-de-Sousa, Daniel J. V. A. dos Santos, Maria-Jose U. Ferreira
Summary: This study aimed to enhance multidrug resistance (MDR) reversing activity in cancer by deriving new compounds from major epimeric alkaloids isolated from Tabernaemontana elegans. The derivatives showed increased activity, with those containing N-phenethyl moieties exhibiting the strongest P-glycoprotein inhibitory effects. Synergistic interactions with the antineoplastic drug doxorubicin were observed, highlighting the potential of these compounds as MDR reversers. Lipophilicity and bulkiness features were associated with inhibitory activity based on the explored QSAR models.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Organic
Ricardo J. Ferreira, Gabriella Spengler, Andreas Orthaber, Daniel J. V. A. dos Santos, Maria-Jose U. Ferreira
Summary: Pedrolide is a diterpenoid with a unique carbon skeleton, pedrolane, which can reverse multidrug resistance mediated by P-glycoprotein.
Article
Energy & Fuels
Rayanne O. Araujo, Flaviana C. P. Ribeiro, Vanuza O. Santos, Victoria M. R. Lima, Jamily L. Santos, Jose E. S. Vilaca, Jamal S. Chaar, Newton P. S. Falcao, Adrian M. Pohlit, Luiz K. C. de Souza
Summary: Global economic and social development has led to an increased demand for energy, requiring technological advancements in the development of new safe, renewable, and sustainable energy sources. Biomass has become important due to its abundance and renewable nature. This study focuses on the availability and characteristics of unexplored Amazonian biomass sources for potential energy production, aiming to provide important information for renewable energy policies in the Amazon region.
BIOENERGY RESEARCH
(2022)
Editorial Material
Biochemistry & Molecular Biology
Maria-Jose U. Ferreira
Article
Plant Sciences
Catia Ramalhete, Bruno M. F. Goncalves, Filipa Barbosa, Noelia Duarte, Maria-Jose U. Ferreira
Summary: Momordica balsamina, also known as balsam apple or African pumpkin, is a highly nutritious vegetable commonly used as food in sub-Saharan Africa. It has been traditionally used in medicine to treat diseases like malaria and diabetes. The main active compounds in this plant are cucurbitane-type triterpenoids called cucurbitacins, which have shown various biological activities, including anti-cancer, antibacterial, anti-malarial, and antidiabetic properties.
PHYTOCHEMISTRY REVIEWS
(2022)
Article
Fisheries
Marieta Nascimento de Queiroz, Zelina Estevam dos Santos Torres, Adrian Martin Pohlit, Eduardo Akifumi Ono, Elizabeth Gusmao Affonso
Summary: Piper aduncum, a native plant of the Amazon, has important medicinal properties and can be a sustainable source for pharmaceutical industry. This study found that the ethanol extract of this plant is effective in controlling monogeneans in Colossoma macropomum without compromising fish health and survival.
Article
Chemistry, Medicinal
Raquel Durao, Catia Ramalhete, Ana Margarida Madureira, Eduarda Mendes, Noelia Duarte
Summary: Human African trypanosomiasis and American trypanosomiasis are neglected tropical diseases caused by protozoan parasites. They have spread worldwide due to human migration, military interventions, and climate changes. Finding new drugs from higher plants is a valuable approach to treat these diseases.
Review
Clinical Neurology
R. P. Romero-Galisteo, M. Gonzalez-Sanchez, L. Costa, R. Brandao, C. Ramalhete, C. Leao, L. Jacobsohn
Summary: This study identified and described outcome measures for objective and subjective assessment in persons with Rett syndrome, finding a relationship between most instruments and activity limitations. The findings offer promising information for clinicians and researchers, but there are methodological limitations to be considered.
EUROPEAN JOURNAL OF PAEDIATRIC NEUROLOGY
(2022)
Article
Anthropology
Gina Frausin, Ana Carla dos Santos Bruno, Ari de Freitas Hidalgo, Lin Chau Ming, William Milliken, Adrian Martin Pohlit
Summary: This paper examines the impact of biomedical healthcare on the ethnomedicinal knowledge of forest peoples in the Brazilian Amazonia region, and finds that they have varied beliefs and treatments for malaria.
JOURNAL OF ETHNOBIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Shirley A. R. Sancha, Adriana Gomes, Joana B. Loureiro, Lucilia Saraiva, Maria Jose U. Ferreira
Summary: In this study, phytochemical analysis of Pancratium maritimum revealed the presence of various Amaryllidaceae alkaloids, which exhibited significant growth inhibitory effects against breast cancer cell lines, including triple-negative breast cancer. Among the isolated compounds, the homolycorine-type alkaloid 7 showed promising anti-proliferative activity through induction of apoptosis, modulation of mitochondrial reactive oxygen species, and G2/M cell cycle arrest. Furthermore, compound 7 exhibited synergistic effects when combined with conventional chemotherapeutic drugs.
Article
Biochemistry & Molecular Biology
Cristina Duarte Silva, Catia Ramalhete, Gabriella Spengler, Silva Mulhovo, Joseph Molnar, Maria-Jose U. Ferreira
Summary: Compounds extracted from Momordica balsamina have shown potential as multidrug resistance (MDR) reversers and have synergistic effects with doxorubicin.
Article
Biochemistry & Molecular Biology
Shirley A. R. Sancha, Nikoletta Szemeredi, Gabriella Spengler, Maria-Jose U. Ferreira
Summary: In order to overcome multidrug resistance in cancer chemotherapy, lycorine, a major Amaryllidaceae alkaloid isolated from Pancratium maritimum, was derivatized to obtain 31 new compounds. These compounds showed significant activity in the study of anticancer drug resistance.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Catia A. Bonito, Ricardo J. Ferreira, Maria-Jose U. Ferreira, Jean-Pierre Gillet, M. Natalia D. S. Cordeiro, Daniel J. V. A. dos Santos
Summary: In this study, the impact of four P-gp mutations on drug-binding and efflux-related signal-transmission mechanism was evaluated. The repacking of the transmembrane helices induced by mutations and ligands indicates P-gp's sensitivity to perturbations in the transmembrane region. Changes in drug-binding were observed as a consequence of transmembrane helices repacking, but were not always correlated with alterations in ligand binding mode and affinity. The changes in drug efflux are mostly related to changes in drug specificity rather than effects on signal-transmission mechanism.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Editorial Material
Biochemistry & Molecular Biology
Maria-Jose U. Ferreira
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
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)