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Halimane Derivatives from Plectranthus ornatus Codd. as Novel Anti-cancer Agents
The objective of this work was to improve the activity of the halimane lead molecule. Further physiochemical characterisation was performed on Hal. To the best of our knowledge, this work constitutes the first published data of the absolute configurations by SCXRD and thermal stability of Hal. Using Hal, reactions with different amines were carried out to afford novel semi-synthetic derivatives and their structural elucidation was completed. The cytotoxicity of the derivatives was assessed against three leukaemia cancer cell lines (CCRF-CEM, K562 and HL-60). The antioxidant activity was investigated using H2O2-induced HGF-...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - April 7, 2024 Category: Drugs & Pharmacology Authors: Gabrielle Bangay Florencia Z Brauning Tomasz Kowalczyk Anna Merecz-Sadowska Ewelina Synowiec Tomasz Śliwiński Nuno Candeias Monica S Estev ão Carlos A M Afonso V ânia André Przemys ław Sitarek Patr ícia Rijo Source Type: research

Role of the microbiota-gut-heart axis between bile acids and cardiovascular disease
Biomed Pharmacother. 2024 Apr 6;174:116567. doi: 10.1016/j.biopha.2024.116567. Online ahead of print.ABSTRACTBile acid (BA) receptors (e.g., farnesoid X-activated receptor, muscarinic receptor) are expressed in cardiomyocytes, endothelial cells, and vascular smooth muscle cells, indicating the relevance of BAs to cardiovascular disease (CVD). Hydrophobic BAs are cardiotoxic, while hydrophilic BAs are cardioprotective. For example, fetal cardiac insufficiency in maternal intrahepatic cholestasis during pregnancy, and the degree of fetal cardiac abnormality, is closely related to the level of hydrophobic BAs in maternal bloo...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - April 7, 2024 Category: Drugs & Pharmacology Authors: Ziyi Zhang Tingting Lv Xiang Wang Menglu Wu Ruolin Zhang Xiaopeng Yang Yongping Fu Zheng Liu Source Type: research

Regulation of myogenic cell proliferation and differentiation during mammalian skeletal myogenesis
Biomed Pharmacother. 2024 Apr 6;174:116563. doi: 10.1016/j.biopha.2024.116563. Online ahead of print.ABSTRACTMammalian skeletal myogenesis is a complex process that allows precise control of myogenic cells' proliferation, differentiation, and fusion to form multinucleated, contractile, and functional muscle fibers. Typically, myogenic progenitors continue growth and division until acquiring a differentiated state, which then permanently leaves the cell cycle and enters terminal differentiation. These processes have been intensively studied using the skeletal muscle developing models in vitro and in vivo, uncovering a compl...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - April 7, 2024 Category: Drugs & Pharmacology Authors: Jiyao Wu Binglin Yue Source Type: research

Myricanol improves metabolic profiles in dexamethasone induced lipid and protein metabolism disorders in mice
This study for the first time applied widely targeted metabolomics to investigate the beneficial effects of MY on glucose, lipids, and protein metabolism in DEX-induced metabolic abnormality in mice. The results showed that MY significantly reversed DEX-induced soleus and gastrocnemius muscle weight loss, muscle fiber damage, and muscle strength loss. MY alleviated DEX-induced metabolic disorders by increasing SIRT1 and glucose transporter type 4 (GLUT4) expressions. Additionally, myricanol prevented muscle cell apoptosis and atrophy by inhibiting caspase 3 cleavages and muscle ring-finger protein-1 (MuRF1) expression. Met...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - April 7, 2024 Category: Drugs & Pharmacology Authors: Tiandan Li Xiaochao Hu Lingyang Fan Yong Yang Kai He Source Type: research

Mastoparan M promotes functional recovery in stroke mice by activating autophagy and inhibiting ferroptosis
Biomed Pharmacother. 2024 Apr 6;174:116560. doi: 10.1016/j.biopha.2024.116560. Online ahead of print.ABSTRACTNeuronal ferroptosis and autophagy are crucial in the pathogenesis of cerebral ischemia-reperfusion injury (CIRI). Mastoparan M (Mast-M), extracted from the crude venom of Vespa magnifica (Smith), comprises 14 amino acid residues. Previous studies suggested that Mast-M reduces neuronal damage following global CIRI, but its protective mechanisms remain unclear. The present study examined the effect of Mast-M on middle cerebral artery occlusion/reperfusion (MCAO/R) induced neurological deficits using Grip, Rotarod, Lo...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - April 7, 2024 Category: Drugs & Pharmacology Authors: Qian Wang Chaojie Liu Mingran Chen Jie Zhao Dexiao Wang Pengfei Gao Chenggui Zhang Hairong Zhao Source Type: research

Sacubitril/Valsartan inhibits M1 type macrophages polarization in acute myocarditis by targeting C-type natriuretic peptide
In conclusion, Sac/Val exerts a protective effect in myocarditis by increasing CNP concentration and inhibiting M1 macrophages polarization.PMID:38581923 | DOI:10.1016/j.biopha.2024.116535 (Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie)
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - April 6, 2024 Category: Drugs & Pharmacology Authors: Changhu Liu Qi Long Han Yang Hongmin Yang Yaohan Tang Bingjun Liu Zihua Zhou Jing Yuan Source Type: research

Hepatoprotective and cardioprotective effects of empagliflozin in spontaneously hypertensive rats fed a high-fat diet
Biomed Pharmacother. 2024 Apr 5;174:116520. doi: 10.1016/j.biopha.2024.116520. Online ahead of print.ABSTRACTA combination of liver and heart dysfunction worsens the prognosis of human survival. The aim of this study was to investigate whether empagliflozin (a sodium-glucose transporter-2 inhibitor) has beneficial effects not only on cardiac and renal function but also on hepatic function. Adult (6-month-old) male spontaneously hypertensive rats (SHR) were fed a high-fat diet (60% fat) for four months to induce hepatic steatosis and mild heart failure. For the last two months, the rats were treated with empagliflozin (empa...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - April 6, 2024 Category: Drugs & Pharmacology Authors: Silvie Hojn á Hana Mal ínská Martina H üttl Zde ňka Vaňourková Irena Markov á Denisa Mikl ánková Jaroslav Hrdli čka Franti šek Papoušek Jan Neck ář Petr Kujal Michal Behuliak Hana Rauchov á Michaela Kadlecov á David Sedmera Krist ýna Nef Source Type: research

RNA expression changes driven by altered epigenetics status related to NASH etiology
In conclusion, the chromatin landscape is altered in NASH patients compared to patients without this liver condition. This alteration might cause mRNA changes explaining, at least partially, the etiology and pathophysiology of the disease.PMID:38579398 | DOI:10.1016/j.biopha.2024.116508 (Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie)
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - April 5, 2024 Category: Drugs & Pharmacology Authors: Daniel Castellano-Castillo Bruno Ramos-Molina Mar ía Dolores Frutos Isabel Arranz-Salas Armando Reyes-Engel Mar ía Isabel Queipo-Ortuño Fernando Cardona Source Type: research

Therapeutic potential of LINS01 histamine H < sub > 3 < /sub > receptor antagonists as antineoplastic agents for triple negative breast cancer
Biomed Pharmacother. 2024 Apr 4;174:116527. doi: 10.1016/j.biopha.2024.116527. Online ahead of print.ABSTRACTThe aims of this work were to evaluate the expression of histamine H3 receptor (H3R) in triple negative breast cancer (TNBC) samples and to investigate the antitumoral efficacy and safety of the LINS01 series of H3R antagonists, through in silico, in vitro, and in vivo approaches. Antitumor activity of LINS01009, LINS01010, LINS01022, LINS01023 was assayed in vitro in 4T1 and MDA-MB-231 TNBC cells (0.01-100 μM), and in vivo in 4T1 tumors orthotopically established in BALB/c mice (1 or 20 mg/kg). Additionally, H3R e...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - April 5, 2024 Category: Drugs & Pharmacology Authors: Ignacio A Ospital M ónica A Táquez Delgado Melisa B Nicoud Michelle F Corr êa Gustavo A Borges Fernandes Isabela W Andrade Paolo Lauretta Roc ío Martínez Vivot Mar ía Betina Comba Mar ía Marta Zanardi Daniela Speisky Juan L Uriburu Jo ão P S Ferna Source Type: research

Targeted delivery of NO donor and ROS scavenger for synergistic treatment of rheumatoid arthritis
Biomed Pharmacother. 2024 Apr 4;174:116540. doi: 10.1016/j.biopha.2024.116540. Online ahead of print.ABSTRACTRheumatoid arthritis (RA) is characterized by high level of reactive oxygen species (ROS) and proinflammatory cytokines, which facilitate the activation of the inflammatory signaling such as NF-κB pathway and exacerbate the development of inflammation. Herein, we designed a nanodrug by encapsulating the NO donor S-nitrosoglutathione (GSNO) into an emulsion and coating the surface with a polydopamine (PDA) layer to yield GSNO@PDA, which simultaneously scavenged the extra ROS and suppressed NF-κB signaling for poten...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - April 5, 2024 Category: Drugs & Pharmacology Authors: Rongrong Luo Jingjing Su Wenying Zhang Wenguang Huang Qianqian Zhou Pengchao Sun Yongxing Zhao Source Type: research

A novel HDAC8 inhibitor H7E exerts retinoprotective effects against glaucomatous injury via ameliorating aberrant M üller glia activation and oxidative stress
In this study, we investigated the protective effects and cellular mechanisms of H7E, a novel small molecule inhibits HDAC8, using in vitro and in vivo glaucoma-like models. Importantly, H7E mitigated extracellular MMP-9 activity and MCP-1 levels in glutamate- or S100B-stimulated reactive Müller glia. In addition, H7E inhibited the upregulation of inflammation- and proliferation-related signaling pathways, particularly the ERK and JNK MAPK pathways. Under conditions of oxidative damage, H7E prevents retinal cell death and reduces extracellular glutamate released from stressed Müller glia. In a mouse model of NMDA-induced...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - April 5, 2024 Category: Drugs & Pharmacology Authors: Liang-Huan Wu Yu-Wen Cheng Fan-Li Lin Kai-Cheng Hsu Mong-Heng Wang Jing-Lun Yen Tsung-Jen Wang Tony Eight Lin Yi-Chien Liu Wei-Jan Huang George Hsiao Source Type: research

A novel potent class I HDAC inhibitor reverses the STAT4/p66Shc apoptotic defect in B cells from chronic lymphocytic leukemia patients
Biomed Pharmacother. 2024 Apr 4;174:116537. doi: 10.1016/j.biopha.2024.116537. Online ahead of print.ABSTRACTChronic Lymphocytic Leukemia (CLL) patients have a defective expression of the proapoptotic protein p66Shc and of its transcriptional factor STAT4, which evoke molecular abnormalities, impairing apoptosis and worsening disease prognosis and severity. p66Shc expression is epigenetically controlled and transcriptionally modulated by STAT4; epigenetic modifiers are deregulated in CLL cells and specific histone deacetylases (HDACs) like HDAC1, are overexpressed. Reactivation of STAT4/p66Shc expression may represent an a...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - April 5, 2024 Category: Drugs & Pharmacology Authors: Sara Rossi Vanessa Tatangelo Maria Dichiara Stefania Butini Sandra Gemma Simone Brogi Silvia Pasquini Martina Cappello Fabrizio Vincenzi Katia Varani Ludovica Lopresti Margherita Malchiodi Chiara Carrara Alessandro Gozzetti Monica Bocchia Giuseppe Marotta Source Type: research