Synthesis, Antimalarial, Antileishmanial, and Cytotoxicity Activities and Preliminary In Silico ADMET Studies of 2-(7-Chloroquinolin-4-ylamino)ethyl Benzoate Derivatives.

A series of heterocyclic chloroquine hybrids, containing a chain of two carbon atoms at position four of the quinolinic chain and acting as a link between quinoline and several benzoyl groups, is synthesized and screened in vitro as an inhibitor of β-hematin formation and in vivo for its antimalarial activity against chloroquine-sensitive strains of ANKA in this study. The compounds significantly reduced haeme crystallization, with IC values < 10 µM. The values were comparable to chloroquine's, with an IC of 1.

One-Pot Synthesis of CdTe/ZnS Quantum Dots and their Physico-Chemical Characterization.

A known property of quantum dots (QDs) is their characteristic luminescence, which would make it possible to detect different types of cancers after being functionalized with some type of biological molecule. For this reason, in the present investigation a methodological analysis of the physicochemical characteristics of the CdTe/ZnS core/shell QDs was carried out, using techniques such as Optical Absorbance Spectroscopy (UV-Vis), Molecular Fluorescence, Fourier Transform Infrared Spectroscopy (FT-IR), Dynamic Light Scattering (DLS), X-Ray Diffraction (XRD), Transmission Electron Microscopy (TEM) and Zeta Potential that allowed to verify the photoluminescent effectiveness of these semiconductor nanocrystals as an alternative to conventional techniques currently used for the detection of specific cancers smaller than 1 cm. The study consisted of theoretically determining the bandgap energy, the size of the nanocrystals and the molar absorptivity from the wavelength value for the maximum intensity of the excitonic peak.

Efficacy and Safety of Gabapentin on Postoperative Pain Management After Bariatric Surgery: A Systematic Review and Meta-Analysis.

Purpose: Examine the efficacy and safety of perioperative gabapentin in bariatric surgical patients.

Design: Systematic Review and Meta-analysis.

Methods: An exhaustive search was conducted using PubMed, Cochrane Library, MEDLINE, CINAHL, Google Scholar, and other gray literature.

Novel 7-Chloro-(4-thioalkylquinoline) Derivatives: Synthesis and Antiproliferative Activity through Inducing Apoptosis and DNA/RNA Damage.

A series of 78 synthetic 7-chloro-(4-thioalkylquinoline) derivatives were investigated for cytotoxic activity against eight human cancer as well as 4 non-tumor cell lines. The results showed, with some exceptions, that sulfanyl - and sulfinyl - derivatives exhibited lower cytotoxicity for cancer cell lines than those of well-described sulfonyl N-oxide derivatives -. As for compound , the most pronounced selectivity (compared against BJ and MRC-5 cells) was observed for human cancer cells from HCT116 (human colorectal cancer with wild-type p53) and HCT116p53-/- (human colorectal cancer with deleted p53), as well as leukemia cell lines (CCRF-CEM, CEM-DNR, K562, and K562-TAX), lung (A549), and osteosarcoma cells (U2OS).

Synthesis, Leishmanicidal, Trypanocidal, Antiproliferative Assay and Apoptotic Induction of (2-Phenoxypyridin-3-yl)naphthalene-1(2)-one Derivatives.

The coexistence of leishmaniasis, Chagas disease, and neoplasia in endemic areas has been extensively documented. The use of common drugs in the treatment of these pathologies invites us to search for new molecules with these characteristics. In this research, we report 16 synthetic chalcone derivatives that were investigated for leishmanicidal and trypanocidal activities as well as for antiproliferative potential on eight human cancers and two nontumor cell lines.

Molecular Mechanisms of Chloroquine and Hydroxychloroquine Used in Cancer Therapy.

Tumour relapse, chemotherapy resistance, and metastasis continue to be unsolved issues in cancer therapy. A recent approach has been to scrutinise drugs used in the clinic for other illnesses and modify their structure to increase selectivity to cancer cells. Chloroquine (CQ) and hydroxychloroquine (HCQ), known antimalarials, have successfully treated autoimmune and neoplastic diseases.

Caracasine, An -kaurane Diterpene with Proapoptotic and Pro-differentiator Activity in Human Leukaemia Cell Lines.

Background: Kaurane-type diterpenoids, obtained from various natural sources, have shown many biological activities, including anti-inflammatory and antitumor effects. Caracasine, an -kaurane diterpenoid isolated from the flowers of , was shown to induce apoptosis in leukaemia cell lines.

Objective: The present study aimed to ascertain the compound's mechanism of cell death induction using two leukaemia cell lines, Jurkat E6.

Synthesis and in silico ADME/Tox profiling studies of heterocyclic hybrids based on chloroquine scaffolds with potential antimalarial activity.

A series of heterocyclic chloroquine hybrids containing either a β-phenethylamine fragment or a 2-aminoindane moiety were synthesized and screened in vitro as inhibitors of β-hematin formation and in vivo for their antimalarial activity against chloroquine-sensitive strains of Plasmodium berghei ANKA. Although these new compounds were not found to be more active than chloroquine in vivo, all new compounds significantly reduced heme crystallization with IC values < 1 μM. Compounds 12 and 13 were able to inhibit heme crystallization with IC values of 0.

In vitro evaluation and in vivo efficacy of nitroimidazole-sulfanyl ethyl derivatives against Leishmania (V.) braziliensis and Leishmania (L.) mexicana.

The aim of this study was to synthesize several small molecules of the type 5-nitroimidazole-sulfanyl and evaluate biological properties against the main Leishmania species that cause cutaneous leishmaniasis in Venezuela. Final compounds 4-7 were generated through simple nucleophilic substitution of 1-(2-chloroethyl)-2-methyl-5-nitroimidazole 3 with 2-mercaptoethanol, 1-methyl-2-mercaptoethanol, and 2-thyolacetic acid derivative. Compound 8 was synthesized via a coupling reaction between 7 and (S)-Methyl 2-amino-4-methylpentanoate hydrochloride.

Synthesis and antimalarial and anticancer evaluation of 7-chlorquinoline-4-thiazoleacetic derivatives containing aryl hydrazide moieties.

Twelve 7-chloroquinoline derivatives were designed and synthesized using the principle of molecular hybridization through the coupling of 2-[2-(7-chloroquinolin-4-ylthio)-4-methylthiazol-5-yl]acetic acid 1 with various benzoyl hydrazines 2a-l. The synthetic compounds were tested as antimalarials. Some of them showed an efficient in vitro activity as inhibitors of β-hematin formation and an in vivo activity in a murine model, resulting in compounds 8 and 9 as the most active ones with IC values of 0.

Postacute Management of Older Adults Suffering an Osteoporotic Hip Fracture: A Consensus Statement From the International Geriatric Fracture Society.

Background: The majority of patients require postacute care (PAC) after a hip fracture. Despite its importance, there is no established consensus regarding the standards of care provided to hip fracture patients in PAC facilities.

Methodology: A writing group was created by professionals from the International Geriatric Fracture Society (IGFS) with representation from other organizations.

The Role of Chloroquine and Hydroxychloroquine in Immune Regulation and Diseases.

Chloroquine (CQ) and hydroxychloroquine (HCQ) are derivatives of the heterocyclic aromatic compound quinoline. These economical compounds have been used as antimalarial agents for many years. Currently, they are used as monotherapy or in conjunction with other therapies for the treatment of autoimmune diseases such as systemic lupus erythematosus (SLE), rheumatoid arthritis (RA), Sjögren's syndrome (SS) and antiphospholipid antibody syndrome (APS).

Is it necessary to tie the medial row in rotator cuff repair double-row constructs when using suture tape?

Purpose: To evaluate the selected biomechanical differences of a double-row -osseous equivalent rotator cuff repair with a knotless versus knot-tying medial row using suture tape in regard to repair displacement, stiffness, and ultimate load to failure.

Methods: In 16 fresh-frozen human shoulders (8 matched pairs), double-row rotator cuff repairs were performed with medial-row mattress knots (MK) on one side, the other without (NK). Two DVRT (Differential Variable Reluctance Transducer) sensors were attached between the humerus and 3 mm above the repair site and were used to measure the displacement across the repair during cycling.

Effects of Flavonoids and Its Derivatives on Immune Cell Responses.

Background: Various pieces of evidence have shown that people who consume foods rich in polyphenolic and flavonoids compounds have a lower incidence of inflammatory, autoimmune diseases and cancer.

Objective: The study aimed to review the most potent compounds that affect the immune response and diseases associated with it.

Methods: Publications in PubMed and EmBase, from 1974-2018, and patents form Free patents online, Scifinder, Espacenet and Mendeley in which flavonoids, their semi-synthetic and synthetic derivatives are involved in immunosuppressive or immunostimulatory responses in vitro and in vivo.

Caracasine acid, an ent-3,4-seco-kaurene, promotes apoptosis and cell differentiation through NFkB signal pathway inhibition in leukemia cells.

Caracasine acid (CA) is an ent-3,4-seco-kaurene isolated from the plant Croton micans. Decreased cancer cell lines viability was reported upon CA treatment. The present study aimed to investigate the mechanism of CA induced cytotoxicity using two human cell lines, Jurkat E6.

What Is the Optimal Number of Samples for Culture in Patients Undergoing Surgery for Foot and Ankle Infections?

Recommendation: The optimal number of samples for culture in patients undergoing surgery for foot and ankle infections is unknown. We recommend that multiple tissue samples be taken.

Level Of Evidence: Consensus.

Sorafenib-induced Facial Acneiform Eruption.

Sorafenib is a multikinase inhibitor that is used to treat hepatocellular carcinoma by inhibiting tumor cell growth and angiogenesis. Cutaneous adverse events of sorafenib are commonly reported, with alopecia and hand-foot skin reactions most frequently encountered. Acneiform eruptions represent rare adverse events that have only been reported at high doses of sorafenib.

Hypomyopathic Dermatomyositis Presenting with Idiopathic CD4 T-lymphocytopenia and Delayed Anti-MDA5 Positivity.

A 47-year-old Haitian male with no known past medical history was admitted to the hospital for gradually progressive dyspnea, nonproductive cough, and weight loss. He also endorsed a one-year history of joint pains. He was febrile and tachycardic and in mild respiratory distress.

A Rare Case of Low-grade Appendiceal Mucinous Neoplasm: A Case Report.

Low-grade appendiceal mucinous neoplasm (LAMN) is a rare malignancy with symptoms varying depending on the clinical manifestations. The most worrisome complication of this particular neoplasm is seeding of mucin into the adjacent peritoneum leading to pseudomyxoma peritonei (PMP). There is a lack of standardized treatment approach; however, an appendectomy-only approach is currently being used for the resection of non-metastatic disease.

Optimization of antimalarial, and anticancer activities of (E)-methyl 2-(7-chloroquinolin-4-ylthio)-3-(4-hydroxyphenyl) acrylate.

Chemically modified versions of bioactive substances, are particularly useful in overcoming barriers associated with drug formulation, drug delivery and poor pharmacokinetic properties. In this study, a series of fourteen (E)-methyl 2-(7-chloroquinolin-4-ylthio)-3-(4-hydroxyphenyl) acrylate (2-15) were prepared by using a one step synthesis from 1 previously described by us as potential antimalarial and antitumor agent. Molecules were evaluated as inhibitors of β-hematin formation, where most of them showed a significant inhibition value (% > 70).

Role of Hypothalamic-Pituitary-Adrenal axis and corticotropin-releasing factor stress system on cue-induced relapse to alcohol seeking.

A large body of evidence has shown that the Corticotropin Releasing Factor (CRF) system, which plays a key role in stress modulation, is deeply involved in relapse to alcohol seeking induced by exposure to stressful events such as foot shock or yohimbine injections. Exposure to environmental cues is also known to be a trigger for alcohol relapse, nevertheless, the relationship between the relapse evoked by the cue-induced model and the CRF stress systems remains unclear. The purpose of this study was to evaluate, in male Wistar rats, the involvement of the CRF system and Hypothalamic-Pituitary-Adrenal (HPA) axis in relapse induced by environmental cues.

[Prophylaxis in hemophilia: situation analysis and call-to-action in Latin America. A report from the GLAITH group].

Prophylactic treatment in the management of hemophilia has been a crucial factor in improving the prognosis and quality of life for people with hemophilia (PCH). However, it is not globally implemented. In Latin America it is difficult to assess the status of PCH and the its management does not conform to ideal standards.

The transverse force experienced by the radial head during axial loading of the forearm: A cadaveric study.

Background: When designing a radial head replacement, the magnitude and direction of forces applied across the proximal radio-ulnar joint (PRUJ) and the radiocapitellar joint must be included. These designs often focus on axial loads transmitted to the radial head by the capitellum; however, the radial head also bears a significant transverse force at the PRUJ. Load transmission by the central band of the interosseous ligament induces a force component in a lateral direction perpendicular to the axis of the limb, which is borne by the articular surfaces of the proximal and distal radio-ulnar joints.

Peptide vaccines for cancer therapy.

For around four decades, vaccines of different kinds have been developed to treat different types of cancer. However, promising results encountered in the early phase contrasted with the results recorded in clinical studies. Recent discoveries in the vaccine field, adjuvants and delivery systems, and antigen presentation have lead to new patented approaches.