Article
Biochemistry & Molecular Biology
Henoc del Rosario, Ester Saavedra, Ignacio Brouard, Daniel Gonzalez-Santana, Celina Garcia, Elena Spinola-Lasso, Carlos Tabraue, Jose Quintana, Francisco Estevez
Summary: Synthetic flavonoids with new substitution patterns show potential as anticancer drugs. In this study, twelve chalcones were synthesized and their antiproliferative effects on human tumour cells were evaluated. The most cytotoxic chalcones contained a furoyl substituent linked by an ester or an amide through the 2'-hydroxy or the 2'-amino group of the chalcone skeleton. The synthetic chalcone 2'-furoyloxy-4-methoxychalcone (FMC) displayed higher potency than the antineoplastic agent etoposide and had less toxicity on normal blood cells. The mechanism of action involved cell cycle arrest, induction of apoptosis, and inhibition of tubulin polymerization, and depended on the generation of reactive oxygen species.
BIOORGANIC CHEMISTRY
(2022)
Article
Food Science & Technology
Yunyi Chen, Jiaojiao Liang, Xiao Liang, Jiebiao Chen, Yue Wang, Jinping Cao, Chongde Sun, Jiaming Ye, Qingjun Chen
Summary: Limonin, an important bioactive substance in citrus fruits, shows potential in cancer prevention and treatment. Through in vitro studies on HL-60 cells, it was found that limonin can inhibit cell proliferation and induce apoptosis positively correlated with dosage. Furthermore, Western blot results demonstrate that limonin activates the endogenous apoptosis pathway mediated by mitochondria by regulating apoptotic proteins, thus inhibiting cell proliferation and promoting apoptosis. Additionally, limonin down-regulates the expression of NQO1, suggesting a potential indirect mechanism of its anticancer activity through the regulation of antioxidant enzymes.
FOOD SCIENCE & NUTRITION
(2021)
Article
Biochemistry & Molecular Biology
Magdalena Kluska, Michal Juszczak, Jerzy Zuchowski, Anna Stochmal, Katarzyna Wozniak
Summary: Kaempferol and its glycoside derivatives can modulate the antitumor activity of etoposide in human promyelocytic leukemia cells. Kaempferol increases cell sensitivity to etoposide and reduces free radical levels, while some derivatives decrease apoptosis and increase free radicals compared to kaempferol.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Inorganic & Nuclear
Carley Giffert L. Nongpiur, Charlestine Soh, Danny F. Diengdoh, Akalesh Kumar Verma, Renu Gogoi, Venkanna Banothu, Werner Kaminsky, Mohan Rao Kollipara
Summary: A series of half-sandwich complexes containing 3-acetyl chromen-2one-4(N)-substituted thiosemicarbazone derivatives of ruthenium, iridium, and rhodium were synthesized and evaluated for their antibacterial and anticancer activities. The complexes were characterized using various spectral techniques and X-ray crystallography. The results showed that complex 5 exhibited the highest cytotoxicity in Dalton's lymphoma cells, followed by complex 4, 1, and 2.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Carley Giffert L. Nongpiur, Akalesh Kumar Verma, Rohit Kumar Singh, Mayur Mohan Ghate, Krishna Mohan Poluri, Werner Kaminsky, Mohan Rao Kollipara
Summary: A series of new complexes of ruthenium(II), rhodium(III), and iridium(III) with pyrazoline-based ligands were synthesized and characterized. These compounds exhibited good antibacterial activity against Gram-positive bacteria and moderate antioxidant activity. They also showed moderate affinity for binding to Salmon Milt DNA and demonstrated higher cytotoxicity in Dalton's lymphoma cell lines.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2023)
Article
Nutrition & Dietetics
Mohamad Sitheek Abdul Rahman, Sivakumari Kanakarajan, Rajesh Selvaraj, Ashok Kamalanathan, Sabiha Fatima, Manal Abudawood, Nikhat J. Siddiqi, Humidah Alanazi, Bechan Sharma, Maria de Lourdes Pereira
Summary: The methanolic extract of Durio zibethinus fruits exhibits anticancer effects on HL-60 cells by inducing DNA damage and apoptosis. It causes cell cycle arrest and induction of apoptosis in the HL-60 cell line through an intrinsic mechanism. The study confirms the anticancer effects of the methanolic extract of Durian on HL-60 cells.
Article
Chemistry, Medicinal
Rui Wang, Yang Li, Haibo Hu, Leentje Persoons, Dirk Daelemans, Steven De Jonghe, Walter Luyten, Besir Krasniqi, Wim Dehaen
Summary: This study synthesized a series of functionalized triterpenoids and evaluated their anticancer and antibacterial activities. Compound 5f showed the strongest anticancer activity, exhibiting significant cytotoxicity against HL-60 cells, inducing mitochondrial dysfunction and apoptosis.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Lucienne Gatt, David G. Saliba, Pierre Schembri-Wismayer, Marion Zammit-Mangion
Summary: The study showed that exposure to tyrosol at a concentration of 9.23 ppm induced monocytic-like differentiation in HL-60 acute myeloid leukaemia cells, resulting in increased cellular oxidative activity and enhanced surface expression of CD11b and CD14. RNA-seq analysis confirmed upregulation of monocyte genes and loss of neutrophil genes, indicating a shift towards monocytic differentiation. Cell cycle analysis revealed an accumulation of cells in the Sub G(0)/G(1) phase following tyrosol exposure, along with an increase in apoptotic and necrotic markers, suggesting differentiation followed by cell death. This selective cytotoxic effect could have therapeutic potential against leukaemia.
APPLIED SCIENCES-BASEL
(2021)
Article
Biochemistry & Molecular Biology
Junmin Zhang, Qianhe Xu, Di Ma
Summary: This study found that beta-Lapachone can selectively kill human promyelocytic leukemia HL-60 cells by inhibiting TrxR and increasing oxidative stress. Overexpression of TrxR reduced the effectiveness of beta-Lapachone, while knockdown of the enzyme increased its cytotoxicity. This discovery contributes to the understanding of the mechanism of action of beta-Lapachone and supports its potential as an anticancer drug candidate.
FREE RADICAL BIOLOGY AND MEDICINE
(2022)
Article
Pharmacology & Pharmacy
Hulinyue Peng, Longtai You, Chunjing Yang, Kaixin Wang, Manting Liu, Dongge Yin, Yuchen Xu, Xiaoxv Dong, Xingbin Yin, Jian Ni
Summary: The study showed that ginsenoside Rb1 effectively alleviates cytotoxicity induced by triptolide (TP) in HL-7702 cells through inhibition of apoptosis and cell cycle arrest mechanisms. Additionally, ginsenoside Rb1 reduces oxidative stress levels by enhancing the activity of the antioxidant pathway.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Chemistry, Inorganic & Nuclear
P. K. Anuja, Nilmadhab Roy, Utpal Das, Seshu Varddhan, Suban K. Sahoo, Priyankar Paira
Summary: A class of half-sandwich [Ru(eta(6)-p-cymene)(N<^>O 8-hydroxyquinoline)(PTA)] complexes were introduced for brain cancer therapy, and their anticancer activities and toxic effects were evaluated through cellular, molecular, and in vivo experiments.
DALTON TRANSACTIONS
(2022)
Article
Environmental Sciences
Yin-Chen Hsiao, Fu-Shin Chueh, Yi-Shih Ma, Jin-Cherng Lien, Te-Chun Hsia, Wen-Wen Huang, Yu-Cheng Chou, Po-Yuan Chen, Jing-Gung Chung, Hung-Yi Chen, Kuo-Ching Liu
Summary: The combination treatment of GEN and Asp shows a greater anti-leukemia activity on human leukemia HL-60 cells compared to GEN or Asp treatment alone. Suggestions that this combination may enhance the efficacy of Asp in inducing apoptosis in HL-60 cells.
ENVIRONMENTAL TOXICOLOGY
(2021)
Article
Oncology
Satyam Kumar Agrawal, Madhunika Agrawal, Parduman Raj Sharma, Khursheed Ahmad, Abdul Sami Shawl, Saroj Arora, Ajit Kumar Saxena
Summary: The alcoholic extract of Anagallis arvensis demonstrated significant apoptosis induction in HL-60 cells, including chromatin condensation, nuclear fragmentation, and alterations in cell cycle. Additionally, treated cells showed decreased levels of anti-apoptotic protein Bcl-2, increased ROS production, and changes in mitochondrial membrane potential. Moreover, the activation of downstream apoptotic pathway proteins and DNA ladder formation were observed, suggesting the potential of AAE as an effective anticancer agent against leukemia cells.
NUTRITION AND CANCER-AN INTERNATIONAL JOURNAL
(2021)
Article
Biochemistry & Molecular Biology
Monaj Kumar Sarkar, Amrita Kar, Adithyan Jayaraman, Karthi Shanmugam, Vellingiri Vadivel, Santanu Kar Mahapatra
Summary: Myricitrin induces apoptosis in HL-60 leukemia cells by reducing mitochondrial membrane potential, increasing DNA fragmentation, inhibiting cell survival proteins, and inducing pro-apoptotic proteins.
MOLECULAR BIOLOGY REPORTS
(2021)
Article
Genetics & Heredity
Masoumeh Fardi, Ali Mohammadi, Behzad Baradaran, Sahar Safaee
Summary: The study suggests that ZEB2 suppression through apoptosis induction could be an effective therapeutic method for myeloid leukemia, as it induces apoptosis, modulates gene expression, and reduces cell proliferation and viability.
CURRENT GENE THERAPY
(2021)
Article
Plant Sciences
Silvia de Maria Souza, Luciano Santos de Souza, Valdenizia Rodrigues Silva, Milena Botelho Pereira Soares, Daniel Pereira Bezerra, Roberto Wagner da Silva Gois, Horlando Carlota da Silva, Gilvandete Maria Pinheiro Santiago, Gardenia Carmen Gadelha Militao
Summary: In this study, the antiproliferative effects of two natural compounds, pacharin and bauhiniastatin-1, isolated from Bauhinia acuruana on breast cancer cells were investigated. The results showed that both compounds exhibited cytotoxicity against various tumor cell lines, including human breast adenocarcinoma, while having no toxicity on normal cells. The mechanism of action was found to be related to the inhibition of myeloid cell leukemia-1 protein, leading to apoptosis of breast adenocarcinoma cells.
Article
Agricultural Engineering
Diego Pereira de Souza, Jose Francisco de Carvalho Goncalves, Josiane Celerino de Carvalho, Karyne Kathlen Guedes da Silva, Andreia Varmes Fernandes, Gleisson de Oliveira Nascimento, Marcio Viana Ramos, Hector Henrique Ferreira Koolen, Daniel Pereira Bezerra, Alberdan Silva Santos
Summary: The essential oil from the leaves of Guatteria citriodora Ducke has potential applications in various industries due to its chemical composition and antimicrobial activity. It contains citronellal and citronellol as the main compounds and exhibits antimicrobial effects against bacteria and fungi. The mechanism of action may involve damage to the cytoplasmic membrane.
INDUSTRIAL CROPS AND PRODUCTS
(2022)
Article
Biochemistry & Molecular Biology
Sheila S. Fontes, Mateus L. Nogueira, Rosane B. Dias, Clarissa A. Gurgel Rocha, Milena B. P. Soares, Marcos A. Vannier-Santos, Daniel P. Bezerra
Summary: This study investigated the combination of curcumin and disulfiram in the treatment of melanoma and found synergistic anti-tumor effects. The combination promoted apoptosis and DNA fragmentation in melanoma cells and increased oxidative stress. In animal experiments, the combination therapy inhibited tumor growth.
Article
Chemistry, Medicinal
Gleyton Sousa, Maria C. F. de Almeida, Lucas L. Locio, Vanda L. dos Santos, Daniel P. Bezerra, Valdenizia R. Silva, Sinara M. de Almeida, Alice Simon, Thiago da S. Honorio, Lucio M. Cabral, Rosane N. Castro, Ricardo O. de Moura, Arthur E. Kummerle
Summary: In this study, twenty new acridine-thiosemicarbazone derivatives were synthesized and showed strong antiproliferative activities, with DL-08 exhibiting the highest potency. Certain active derivatives were studied for their interactions with DNA and inhibition of topoisomerase II alpha by in silico and in vitro methods. Non-clinical toxicity tests on mice at a dose of 2000 mg/kg showed no serious signs of toxicity for selected compounds.
Article
Chemistry, Multidisciplinary
Ana L. S. Moura, Pedro H. Machado, Rodrigo S. Correa
Summary: This study presents the synthesis and characterization of two new picrate salts: 2,2'-bis(pyridinium)ketone picrate (DPK-PA) and 4,4'-bis(tert-butyl)-2-pyridine-2-pyridinium picrate (BBBPY-PA). Both crystal structures contain an ion-pair, a picrate anion, and a bipyridine derivative. The crystal packing of DPK-PA and BBBPY-PA is stabilized by strong N-H...O hydrogen bonding interactions, as revealed by Hirshfeld surface analysis and fingerprint plots. The compounds were further analyzed by UV-Vis and infrared spectroscopy, supporting the formation of new materials. However, no fluorescence was observed in both compounds, indicating their limited potential as chemical sensors.
STRUCTURAL CHEMISTRY
(2023)
Review
Biochemistry & Molecular Biology
Diego de Carvalho Carneiro, Lila Teixeira de Araujo, Girlaine Cafe Santos, Patricia Kauanna Fonseca Damasceno, Jaqueline Leite Vieira, Ricardo Ribeiro dos Santos, Josiane Dantas Viana Barbosa, Milena Botelho Pereira Soares
Summary: Osteoarthritis is a joint disease characterized by cartilage deterioration. Intra-articular injections of mesenchymal stem cells have shown promising results in animal models and humans. However, further clinical trials are needed to support the efficacy and safety of this approach in the regeneration of articular cartilage.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Plant Sciences
Paulo Michel Pinheiro Ferreira, Livia Queiroz de Sousa, Rayran Walter Ramos de Sousa, Domingos de Jesus Rodrigues, Evaldo dos Santos Moncao Filho, Mariana Helena Chaves, Gerardo Magela Vieira Junior, Marcia dos Santos Rizzo, Livia Alves Filgueiras, Anderson Nogueira Mendes, Daisy Jereissati Barbosa Lima, Claudia Pessoa, Joao Marcelo de Castro e Sousa, Ana Carolina Borges da Cruz Rodrigues, Milena Botelho Pereira Soares, Daniel Pereira Bezerra
Summary: This study evaluates the acute and subacute toxic effects of marinobufagin and its anticancer action. It found that marinobufagin has mild and reversible alterations in key metabolic organs without direct gastrointestinal effects, but can cause acute ataxia, convulsions and death at higher exposure.
JOURNAL OF ETHNOPHARMACOLOGY
(2023)
Article
Chemistry, Physical
Benedicto A. V. Lima, Jaldyr de J. G. Varela Jr, Javier Ellena, Alzir A. Batista, Alberico B. F. da Silva, Rodrigo S. Correa
Summary: Reactions of cis-[RuCl2(P-P)(bipy)] precursors with the SpymMe2 ligand yielded complexes of the [Ru(SpymMe2)(P-P)(bipy)]PF6 type. The structures of the complexes were characterized and analyzed using various techniques, including spectroscopy, electrochemical analysis, elemental analysis, and single-crystal X-ray diffraction. Theoretical studies were also conducted using the DFT/B3LYP method, which helped to explain the stability and properties of the complexes compared to the precursors. The results showed the importance of coordination and ligand positioning in determining the stability and properties of the complexes.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Inorganic & Nuclear
F. M. Niquini, P. H. Machado, J. M. Montilla-Suarez, A. L. S. Moura, R. S. Correa
Summary: Here, a new picrate salt contains a protonated Schiff base (SB) is introduced. The compound exhibits a higher melting point (246-250 degrees C) compared to the base free salt (99-101 degrees C), indicating the formation of a salt. The presence of both a protonated SB and the picrate anion is confirmed by UV-Vis and infrared experiments. The single-crystal X-ray diffraction analysis reveals the formation of an ion pair in the new compound, and the intermolecular interactions and crystal self-assembly are explored in detail. The salt exhibits strong N-H...O hydrogen bonds and pi-pi stacking interactions, which are different from the weak interactions in the neutral SB. Additionally, the fluorescence properties and coordination capability with metals of the SB are investigated, but no significant results are observed.
JOURNAL OF STRUCTURAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Rafaela G. A. Costa, Suellen L. R. Silva, Ingrid R. S. B. Dias, Maiara de S. Oliveira, Ana Carolina B. da C. Rodrigues, Rosane B. Dias, Daniel P. Bezerra
Summary: Acute myeloid leukemia (AML) is a heterogeneous disease group with various mutations triggering malignant proliferation. AML relapse is mainly caused by leukemic stem cells (LSCs) with self-renewal capacity and resistance to traditional therapies. LSCs have low oxidative stress levels due to low mitochondrial activity and high ROS-removing pathway activity. Targeting oxidative stress could be a potential strategy to eliminate AML LSCs.
Article
Biochemistry & Molecular Biology
Gregory F. Grawe, Katia M. Oliveira, Celisnolia M. Leite, Tamires D. de Oliveira, Analu R. Costa, Carlos A. F. Moraes, Joao Honorato, Marcia R. Cominetti, Eduardo E. Castellano, Rodrigo S. Correa, Sergio P. Machado, Alzir A. Batista
Summary: This study reports on three new ruthenium(II) complexes and their cytotoxicity against lung and breast cancer cell lines. The results show that these complexes have potential as anticancer agents, with better selectivity than cisplatin. The complexes also exhibit interactions with DNA and human serum albumin, indicating their promising therapeutic effects.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Julia H. V. Rodrigues, Alexandre B. de Carvalho, Valdenizia R. Silva, Luciano de S. Santos, Milena B. P. Soares, Daniel P. Bezerra, Katia M. Oliveira, Rodrigo S. Corre
Summary: We report on the synthesis and characterization of four new heteroleptic Cu(II) complexes with different ligands. These complexes show moderate interaction with DNA and BSA, and exhibit cytotoxicity against human cancer cells. Among them, complexes 2 and 4 show higher cytotoxicity, suggesting the importance of the phen ligand in enhancing the biological effect of the compounds.
Review
Biochemistry & Molecular Biology
Damiao P. de Sousa, Renan Oliveira S. Damasceno, Riccardo Amorati, Hatem A. Elshabrawy, Ricardo D. de Castro, Daniel P. Bezerra, Vitoria Regina V. Nunes, Rebeca C. Gomes, Tamires C. Lima
Summary: In this review, the authors provide an overview of the mechanisms of pharmacological action of essential oils and their components in various biological systems. They discuss the antioxidant, anti-inflammatory, antitumor, antimicrobial activities, as well as the mechanisms of action against various types of viruses. The data indicate that the chemical diversity in the composition of essential oils allows them to interfere with biological processes at different levels, making them a promising source for the development of new drugs.
Article
Chemistry, Inorganic & Nuclear
Marilia I. F. Barbosa, Rodrigo S. Correa, Adriana P. M. Guedes, Alex M. Graca, Francyelli M. Andrade, Celisnolia M. Leite, Elisangela P. Silveira-Lacerda, Javier Ellena, Henrique V. Reis, Antonio C. Doriguetto, Alzir A. Batista
Summary: Herein, we report on the synthesis and characterization of ruthenium compounds with different amino acids as ligands. The complexes were characterized using various techniques and the structures of two compounds were determined using X-ray diffraction. In vitro evaluation showed that these compounds exhibited cytotoxic activities against triple-negative breast cancer cells and inhibited their migration. Therefore, these compounds may be promising drug candidates for the treatment of triple-negative breast cancer.
Review
Pharmacology & Pharmacy
Paulo Michel Pinheiro Ferreira, Rayran Walter Ramos de Sousa, Dalton Dittz, Joao Marcelo de Castro e Sousa, Francisco Leonardo Torres-Leal, Daniel Pereira Bezerra
Summary: We critically analyzed clinical trials of chloroquine and hydroxychloroquine with or without macrolides during the first wave of COVID-19 and discussed their limitations. The studies showed that these drugs did not show clinical advantages and were not effective in reducing mortality or improving symptoms in COVID-19 patients. The evidence was based mainly on retrospective trials with low quality, making it unreliable for decision-making.
BRAZILIAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2023)