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1.
J Inorg Biochem ; 259: 112663, 2024 Jul 14.
Article in English | MEDLINE | ID: mdl-39024775

ABSTRACT

Given the recognized major problem of microbial drug resistance for human health, new metal-based drugs have been currently explored for their antimicrobial properties, including gallium-based compounds as potential metallophores that could perturb Fe's interactions with proteins. Herein we have designed and synthesized two bis-kojate ligands (named L4 and L6) and studied their Ga(III) complexes for their physico-chemical and biological properties. In particular a detailed study of their complexation properties in aqueous solution, showed equilibrium models with formation of quite stable dinuclear 2:3 metal:ligand complexes, though with different stability. Solid state complexes were also prepared and characterized and complementary DFT studies indicated that [Ga2(L4)3] complex, with higher stability, seems to adopt a three-ligand bridging conformation, while that for L6 adopt a one ligand bridging conformation. Preliminary investigation of the antibacterial activity of these gallium complexes showed antipseudomonal activity, which appeared higher for the complex with L4, a feature of potential interest for the scientific community.

2.
Dalton Trans ; 47(21): 7245-7255, 2018 May 29.
Article in English | MEDLINE | ID: mdl-29757339

ABSTRACT

Reaction of benzohydroxamic acid (Bha), 2-pyridinehydroxamic acid (2-pyha), 2-amino-phenylhydroxamic acid (2-NH2-pha) and salicylhydroxamic acid (Sha) with SbCl3 in ethanol gave the corresponding novel hydroxamato Sb(iii) complexes, [Sb(Bha-1H)2Cl] 1, [SbCl2(2-pyha-1H)] 2, [Sb(2-NH2-pha-1H)(2-NH3-pha-1H)]Cl23 and [SbCl(Sha-1H)2] 4. In all cases the hydroxamic acids coordinate to the Sb centres in the typical bidentate hydroxamato (O,O') coordination mode, via the carbonyl oxygen and deprotonated hydroxyl group. Reaction of the histone deacetylase inhibitor (HDACi) suberoylanilidehydroxamic acid (SAHA) with Sb(OEt)3 gave the Sb(iii) hydroxamato/hydroximato complex, [Sb(SAHA-1H)(SAHA-2H)] 6. All test complexes significantly inhibited the promastigote proliferation of Leishmania amazonensis and L. chagasi and induced substantial changes in the general morphology of the parasites, including reduction in size and loss of flagellum, when compared to the untreated promastigotes. A dose-response approach using the test complexes showed a decreased in plasma membrane permeability and the mitochondrial dehydrogenase activities of the Leishmania species. [Sb(Bha-1H)2Cl] exhibited the best activity and was superior to the Sb HDACi complex 6. Though 1 exhibited noteworthy anti-leishmanial activity, the selectivity indexes determined suggest that [Sb(2-NH2-pha-1H)(2-NH3-pha-1H)]Cl23 is the test complex that merits further investigation as a potential anti-leishmanial agent.


Subject(s)
Antimony/pharmacology , Antiprotozoal Agents/pharmacology , Hydroxamic Acids/pharmacology , Leishmania/drug effects , Antimony/chemistry , Antiprotozoal Agents/chemical synthesis , Antiprotozoal Agents/chemistry , Cell Survival/drug effects , Crystallography, X-Ray , Hydroxamic Acids/chemistry , Leishmania/cytology , Models, Molecular , Molecular Structure , Parasitic Sensitivity Tests
3.
Chem Commun (Camb) ; 53(82): 11318-11321, 2017 Oct 12.
Article in English | MEDLINE | ID: mdl-28967013

ABSTRACT

Novel Pt(iv) tumour penetrating peptide (TPP) conjugates are reported. They are the first example of metallodrugs to target a membrane bound heat shock protein 70 positive (memHSP70+) phenotype in cancer cells. The conjugates exhibit superior cytotoxicity as compared to oxaliplatin alone in Pt resistant colorectal cancer cells with relatively high memHSP70+ expression. Substitution of TPP in Pt(iv) peptide conjugates with scrambled peptide (ScP) essentially abolishes the observed cytotoxicity.


Subject(s)
Antineoplastic Agents/chemistry , HSP70 Heat-Shock Proteins/metabolism , Organoplatinum Compounds/chemistry , Peptides/chemistry , Platinum/chemistry , Amino Acid Sequence , Antineoplastic Agents/toxicity , Cell Line, Tumor , Cell Survival/drug effects , Colorectal Neoplasms/metabolism , Colorectal Neoplasms/pathology , HCT116 Cells , HT29 Cells , Humans , Oxaliplatin
4.
Anaesth Intensive Care ; 45(5): 556-561, 2017 09.
Article in English | MEDLINE | ID: mdl-28911284

ABSTRACT

Nicotine replacement therapy is widely used in critically ill smokers and its effect on delirium, mortality and duration of intensive care unit (ICU) admission is unknown. The aims of this review were to determine whether the management of nicotine withdrawal with nicotine replacement therapy reduces delirium, mortality or length of stay in critically ill smokers in ICU. The primary outcome was incidence of author-defined ICU delirium. Secondary outcomes were ICU or hospital mortality, ICU-free days at day 28, and ICU or hospital length of stay. We conducted a systematic review and meta-analysis of the data sources MEDLINE, EMBASE, CINAHL, and the Cochrane Database of Systematic Reviews for randomised controlled trials and observational studies. Clinical trials, observational studies and systematic reviews comparing nicotine replacement therapy with placebo or no treatment were included. Case reports, case series, non-systematic reviews and studies that involved children were excluded. Eight studies were eligible (n=2,636) for inclusion in the data synthesis. In a meta-analysis of observational studies, nicotine replacement therapy was associated with increased delirium (three studies; n=908; I2=0%; finite element method: odds ratio 4.03 [95% confidence interval 2.64, 6.15]; P <0.001). There was no difference in ICU mortality (three studies; n=1,309; P=0.10, I2=44%; finite element method: odds ratio 0.58; 95% confidence intervals 0.31-1.10) and hospital mortality or 28-day ICU-free days. In the absence of high-quality data, nicotine replacement therapy cannot currently be recommended for routine use to prevent delirium or to reduce hospital or ICU mortality in critically ill smokers.


Subject(s)
Delirium/prevention & control , Smoking Prevention , Tobacco Use Cessation Devices , Critical Illness/mortality , Hospital Mortality , Humans , Intensive Care Units , Nicotine/administration & dosage , Nicotine/adverse effects , Randomized Controlled Trials as Topic , Substance Withdrawal Syndrome/drug therapy , Tobacco Use Cessation Devices/adverse effects , Tobacco Use Disorder/drug therapy
5.
Dalton Trans ; 45(27): 11008-14, 2016 Jul 05.
Article in English | MEDLINE | ID: mdl-27314129

ABSTRACT

Reaction of Bi(NO3)3 with benzohydroxamic acid (Bha) and salicylhydroxamic acid (Sha) gives the novel Bi(iii) complexes [Bi2(Bha-1H)2(µ-Bha-1H)2(η(2)-NO3)2] () and [Bi6(CH3OH)2(η(1)-NO3)2(η(2)-NO3)(OH2)2(Sha-1H)12](NO3)2 (). X-ray crystal structure of reveals two hydroxamato coordination modes; bidentate bridging (O, O') and bidentate non-bridging (O, O') and of reveals one coordination mode; bidentate bridging (O, O'). , specifically designed to and demonstrated to inhibit the activity of urease, exhibits excellent antibacterial activity against three strains of Helicobacter pylori with MIC ≥ 16 µg mL(-1).


Subject(s)
Anti-Bacterial Agents/pharmacology , Bismuth/chemistry , Coordination Complexes/pharmacology , Enzyme Inhibitors/pharmacology , Helicobacter pylori/drug effects , Urease/antagonists & inhibitors , Anti-Bacterial Agents/chemistry , Coordination Complexes/chemistry , Crystallography, X-Ray , Enzyme Inhibitors/chemistry , Helicobacter pylori/enzymology , Molecular Structure
6.
Obes Rev ; 15 Suppl 4: 93-106, 2014 Oct.
Article in English | MEDLINE | ID: mdl-25196408

ABSTRACT

When compared with men of other racial or ethnic groups, African American men are more likely to experience adverse health conditions. The systematic review objectives were to (i) determine the current evidence base concerning African American men's response to lifestyle behavioural interventions designed to promote weight loss, increase physical activity, and/or improve healthy eating and (ii) determine the next steps for research in these areas. The PubMed, Web of Science, Psych Info and Cochrane databases were searched to identify papers published before January 1, 2013 that reported change in weight, physical activity and/or dietary patterns in African American men aged 18 and older, as a result of behavioural change strategies. The titles and abstracts of 1,403 papers were screened; after removing duplicates, 141 papers were read to determine their eligibility. Seventeen publications from 14 studies reported outcomes for African American men. Eight large multi-centre trials and six community-based studies were identified. African American men were an exclusive sample in only four studies. Five studies showed statistically significant improvements. Although the available evidence appears to show that these interventions produce positive results, the relative and the long-term effectiveness of weight loss, dietary and/or physical activity interventions for this population are unknown.


Subject(s)
Behavior Therapy , Black or African American , Diet, Reducing , Exercise , Obesity/prevention & control , Weight Loss , Black or African American/statistics & numerical data , Behavior Therapy/methods , Diet, Reducing/psychology , Exercise/psychology , Health Behavior , Humans , Male , Motor Activity , Obesity/psychology , United States/epidemiology
7.
Public Health ; 125(7): 417-23, 2011 Jul.
Article in English | MEDLINE | ID: mdl-21724208

ABSTRACT

Although gender, racial and ethnic differences in health in the USA are well documented, it is less clear how race and gender intersect to produce large and consistently poor health outcomes for men of colour, particularly Black American men. This paper will illustrate how race and gender intersect at multiple levels to shape men's health and health behaviours, and function as fundamental social determinants of health. The paper will conclude by discussing the need to attend to the role of male gender in pathways and processes underlying racial health disparities, and the challenges of developing health promotion interventions for Black American men.


Subject(s)
Black or African American , Health Behavior , Health Status Disparities , Health Status , Life Style/ethnology , Adult , Cultural Characteristics , Exercise , Feeding Behavior/ethnology , Humans , Male , Obesity/ethnology , Social Conditions , United States
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