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1.
Semin Diagn Pathol ; 2024 Sep 16.
Artículo en Inglés | MEDLINE | ID: mdl-39307612

RESUMEN

Sclerosing Odontogrenic Carcinoma (SOC) is a recent addition to the category of odontogenic tumours, which was first described by Koutlas et al. in 2008. It was described as primary intraosseous carcinoma with bland cytology, sclerotic stroma with presence of local infiltration showing aggressive behaviour. Following its discovery and the presentation of first case, only a handful of cases have been reported till date, which may be due to underreporting of the cases or inclusion of the case to other diagnosis since the features of this tumour overlaps with many other lesions of the oral cavity. Due to this factor, the pathogenesis of this category of tumours still remains enigmatic. The clinical features as a result of this factor are also not reported of the consistent type and overlaps with the already existing clinical features of other lesions. This lesion has only appeared till date twice in WHO classification of Odontogenic Cysts and Tumours. Thereby, the literature on this category is still in paucity. Therefore, the present review takes into account all of the features, diagnostic criteria and the markers discovered for this lesion and would provide an insight into whether this lesion is justified as a malignant lesion or should not be considered as a separate category of odontogenic tumour.

2.
Semin Diagn Pathol ; 2024 Sep 13.
Artículo en Inglés | MEDLINE | ID: mdl-39304422

RESUMEN

The calcifying odontogenic cyst (COC) is an uncommon developmental odontogenic cyst, the oral counterpart of Malherbe's cutaneous calcifying epithelioma (pilomatricoma). This article presents two unique cases of calcifying odontogenic cysts each exhibiting distinctive histopathological features and its literature review. One case with an unexpected finding of cholesterol granuloma (CG), a rare occurrence in non-inflammatory cysts within an unusual location between two maxillary central incisors. One more instance involves the presence of a compound odontome in conjunction with COC. The cases underscore the clinical and histopathological diversity of COC and highlight the importance of radiological and histopathological assessments for accurate diagnosis. The unexpected association of COC with cholesterol granuloma challenges traditional diagnostic expectations. Additionally, the second case suggests that COCs may warrant sub-categorization to better understand their varied presentations and biological behavior. This article contributes to the expanding knowledge of COC, emphasizing the significance of documenting rare cases to enhance comprehension of its nature, pathogenesis, and oral cavity origin.

3.
J Forensic Leg Med ; 107: 102755, 2024 Sep 14.
Artículo en Inglés | MEDLINE | ID: mdl-39293286

RESUMEN

BACKGROUND: Forensic odontology involves the identification of individuals through dental records, making it a crucial tool in legal investigations. Non-metric dental traits (NMDT), which are variations in dental morphology play a key role as these traits are inherited characteristics that can help establish biological relationships or ancestry. Thus, we aim to assess the frequency and variability of NMDT in the human dentition of four ethnically mixed populations in Uttar Pradesh. This study can aid in the future by maintaining records of ethnic groups and their variability, which can be crucial for disaster victim management and forensic odontology. METHODS: The study was conducted on a total of 100 patients coming to the OPD of Oral Medicine and Oral Pathology and Microbiology of King George's Medical University from January 2022 to July 2023. Impressions of both arches were made for participants using irreversible hydrocolloid (alginate), and casts were examined under a stereomicroscope to assess 15 different morphological characteristics. RESULTS: NMDTs such as winging, shoveling, double-shoveling interruption groove, canine mesial ridge, hypocone, metacone, carabelli's trait, peg-shaped incisors, peg-shaped molar, premolar lingual cusp variation, deflecting wrinkle, protostylid, metaconulid, entoconulid was evaluated. The NMDTS were evaluated in four different ethnics Nordics, Mediterranean, Oriental Mediterranean, and Protoaustraloid amongst which various traits showed a statistically significant variation among the population of Uttar Pradesh. CONCLUSION: The sample studied presented confirmed supernumerary traits like metacone, protostylid, carabellis trait, metaconulid, premolar lingual cusp variation, and deflecting wrinkle were seen highest in Nordic, Mediterranean, Oriental Mediterranean, and Protoaustraloid ethnicity have a significant association with the Uttar Pradesh population.

4.
Head Neck Pathol ; 18(1): 83, 2024 Sep 16.
Artículo en Inglés | MEDLINE | ID: mdl-39283410

RESUMEN

INTRODUCTION: Giant cell-rich lesions are a diverse group of lesions that usually occur in bone and contain varying numbers of reactive osteoclastic-type multinucleate giant cells. These lesions present a challenge in pathologic diagnosis, often requiring a combination of clinical, radiographic, and histopathological assessments. The present retrospective observational study aims to provide a concise diagnostic criterion by combining all these parameters, which will aid in effective diagnosis and targeted treatment planning in the future. MATERIAL AND METHOD: Previously diagnosed cases of these lesions were taken from the archives and categorized as Central Giant Cell Granuloma (CGCG), CGCG with secondary Aneurysmal Bone Cyst (ABC), primary ABC, and Brown's Tumour. Their demographic characteristics along with clinical, radiological, and histological data were retrieved and compiled into the table. The data was then analyzed and classified into aggressive and non-aggressive CGCG according to the criteria set in the study. RESULT: 10 reported cases were of isolated CGCG, 5 were CGCG with secondary ABC, 5 of Brown's tumor and 3 were that of conventional ABC. Out of these, the lesions showing extensive size along with an increased number of giant cells were categorized under aggressive CGCG, whereas those with less aggressive characteristics were categorized under non-aggressive CGCG. The aggressive category comprised 5 cases of isolated CGCG, 2 cases of CGCG with secondary ABC, 3 cases of primary ABC, and 5 of brown tumor, whilst the rest of the cases were categorized under non-aggressive CGCG. CONCLUSION: Since all these share overlapping features, thereby this type of concise categorization is the dire need so that the lesions can have a precise diagnosis with treatment and follow-up intervals for aggressive lesions.


Asunto(s)
Granuloma de Células Gigantes , Enfermedades Maxilomandibulares , Humanos , Granuloma de Células Gigantes/patología , Estudios Retrospectivos , Femenino , Masculino , Enfermedades Maxilomandibulares/patología , Adolescente , Niño , Adulto , Adulto Joven , Quistes Óseos Aneurismáticos/patología
5.
J Pharm Bioallied Sci ; 16(Suppl 3): S2467-S2469, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-39346245

RESUMEN

Background: It is frequently observed that dental students require so many consents to manage medically compromised patients, especially cardiovascular patients with periodontitis requiring dental treatment. Aims and Objectives: The present study aimed to assess the dental students' knowledge, attitudes, and practices regarding the management of cardiovascular disease (CVD) patients with periodontitis requiring dental treatment. Material and Methods: The cross-sectional study was conducted among 611 dental undergraduate and postgraduate students (branches of Periodontology, Oral and Maxillofacial Surgery, Oral Medicine and Radiology, Endodontics, Prosthodontics, and Public Health and Dentistry) of central Gujrat. Self-administered structured questionnaires with 23 questions were distributed in pen-and-paper physical format. Statistical analysis for descriptive statistics like frequency, percentage, mean, standard deviation, confidence interval, one-way analysis of variance, post hoc test for multiple comparisons, Fisher's exact test, and Pearson's correlation has been done by MS Excel and STATA/IC-13. Results: As per the post hoc test, both groups of students have significantly different knowledge (-4.20210*, P = 0.028) and their practices (0.68632, P = 0.968) but no significant difference between their attitudes (-6.22828, P = 0.089). According to the Pearson correlation test, a weak positive/no relationship between knowledge, attitudes, and practice is reported in both study groups. There is a weak positive relation between knowledge and attitudes (0.270) and between knowledge and practices (0.121), and a similar relationship between their attitudes and practices (0.172) was observed in both groups. Conclusion: Correct knowledge, attitudes, and practices regarding dental management of CVD patients with periodontitis can reduce medical consent to improve the treatment quality of dental students.

6.
Science ; 385(6708): 574, 2024 Aug 02.
Artículo en Inglés | MEDLINE | ID: mdl-39088636
7.
Indian J Otolaryngol Head Neck Surg ; 76(4): 3519-3523, 2024 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-39130237

RESUMEN

The term "idiopathic lymphoplasmacellular mucositis" (ILPM) refers to a set of conditions marked by extensive lymphocyte and plasma cell infiltrates in the submucosa which can involve the oral cavity, upper respiratory tract and the genital epithelium. There is no recognized cause of ILPM, and the diagnosis is mostly done on an exclusion basis. Herein, we report a 32-year-old man presented with an erosive ulcerated lesion on the hard palate and review the literature regarding the possible differential diagnosis including squamous cell carcinoma. We also reviewed the previously reported cases of ILPM with palatal involvement to summarise clinical presentation, treatment, and outcome of the entity to date.

8.
Indian J Otolaryngol Head Neck Surg ; 76(4): 3537-3542, 2024 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-39130296

RESUMEN

Giant cell tumor (GCT) is a benign, locally aggressive neoplasm with a high recurrence rate with common occurrence in the long bone and the cases in the maxillofacial region bone are very rare. Due to the paucity of the cases, there is not enough information available regarding the behavior of the tumor. Also, the differentiation of this aggressive lesion with the commonly occurring reactive giant cell lesions is crucial and needs more research. This study is pertaining to the review of literature of the cases of GCT in the oral cavity with their clinicopathological, radiographic, and biochemical analyses. Although there are no available studies regarding the immunohistochemical characteristics of this lesion, this study is the first step in this direction to differentiate this tumor better and identify the possible pathogenesis.

9.
ACS Med Chem Lett ; 15(8): 1340-1350, 2024 Aug 08.
Artículo en Inglés | MEDLINE | ID: mdl-39140062

RESUMEN

A convergent strategy for the first total synthesis of the lipopeptide bacilotetrin C has been developed. The key features of this synthesis include Crimmins acetate aldol, Steglich esterification, and macrolactamization. Twenty-nine variants of the natural product were prepared following a systematic structure-activity relationship study, where some of the designed analogues showed promising cytotoxic effects against multiple human carcinoma cell lines. The most potent analogue exhibited a ∼37-fold enhancement in cytotoxicity compared to bacilotetrin C in a triple-negative breast cancer (MDA-MB-231) cell line at submicromolar doses. The study further revealed that some of the analogues induced autophagy in cancer cells to the point of their demise at doses much lower than those of known autophagy-inducing peptides. The results demonstrated that the chemical synthesis of bacilotetrin C with suitable improvisation plays an important role in the development of novel anticancer chemotherapeutics, which would allow future rational design of novel autophagy inducers on this template.

10.
ACS Med Chem Lett ; 15(8): 1250-1259, 2024 Aug 08.
Artículo en Inglés | MEDLINE | ID: mdl-39140063

RESUMEN

Herein, we have demonstrated that the siRNA activity could be enhanced by incorporating the guide strand in the RISC complex through thermodynamic asymmetry caused by m3U-based destabilizing modifications. A nuclease stability study revealed that 2'-OMe-m3U and 2'-OEt-m3U modifications slightly improved the half-lives of siRNA strands in human serum. In the in vitro gene silencing assay, 2'-OMe-m3U modification at the 3'-overhang and cleavage site of the passenger strand in anti-renilla and anti-Bcl-2 siRNA duplexes were well-tolerated and exhibited improved gene silencing activity. However, gene silencing activity was attenuated when these modifications were incorporated at position 3 in the seed region of the antisense strand. The molecular modeling studies using these modifications at the seed region with the MID domain of hAGO2 explained that the 2'-alkoxy group makes steric interactions with the amino acid residues of the hAGO2 protein.

11.
Semin Diagn Pathol ; 2024 Aug 23.
Artículo en Inglés | MEDLINE | ID: mdl-39217025

RESUMEN

BACKGROUND: The Calcifying Odontogenic Cysts (COC) displays a wide range of clinical and histopathological variations as well as diverse biological behaviors. This diversity has led to confusion and disagreement regarding the terminology and classification of this lesion. The previous classification attempts to categorize COC into two concepts. The first concept, termed "monistic," suggests that all COCs are neoplastic despite the majority being cystic in structure and seemingly non-neoplastic. The second concept, known as "dualistic," posits that COC comprises two distinct entities: a cyst and a neoplasm. This research discusses various previous classifications of COC found in the literature and proposes a new, straightforward universal classification based solely on histopathology, aiming to facilitate understanding for surgeons. MATERIAL AND METHODS: Fifteen cases of COC have been collected with clinicopathological parameters including detailed information regarding patient demographics, symptoms, anatomical site, radiological characteristics, duration of evolution, recurrence, and types of histopathology according to the proposed classification. RESULT: A total of fifteen cases of COC were analyzed. According to the histological analysis of the proposed classification Type 1: 5 (33.3), Type II: 4 (26.6), Type III: 3(20), and Type IV:3(20) and recurrence in 3 (20 %) of cases. CONCLUSION: It simplifies the complexities arising from variations in the cystic linings of type IV of COC, which can be overlooked and have caused recurrence in the current research. Therefore, the key requirement for arriving at a validated and practical conclusion lies in the accurate histological classification of calcifying odontogenic cysts and their impact on treatment.

12.
Stud Health Technol Inform ; 316: 719-723, 2024 Aug 22.
Artículo en Inglés | MEDLINE | ID: mdl-39176896

RESUMEN

Automatic deidentification of Electronic Health Records (EHR) is a crucial step in secondary usage for biomedical research. This study introduces evaluation of an intricate hybrid deidentification strategy to enhance patient privacy in secondary usage of EHR. Specifically, this study focuses on assessing automatic deidentification using OpenDeID pipeline across diverse corpora for safeguarding sensitive information within EHR datasets by incorporating diverse corpora. Three distinct corpora were utilized: the OpenDeID v2 corpus containing pathology reports from Australian hospitals, the 2014 i2b2/UTHealth deidentification corpus with clinical narratives from the USA, and the 2016 CEGS N-GRID identification corpus comprising psychiatric notes. The OpenDeID pipeline employs a hybrid approach based on deep learning and contextual rules. Pre-processing steps involved harmonizing and addressing encoding and format issues. Precision, Recall, F-measure metrics were used to assess the performance. The evaluation metrics demonstrated the superior performance of the Discharge Summary BioBERT model. Trained on three corpora with a total of 4,038 reports, the best performing model exhibited robust deidentification capabilities when applied to EHR. It achieved impressive micro-averaged F1-scores of 0.9248 and 0.9692 for strict and relaxed settings, respectively. These results offer valuable insights into the model's efficacy and its potential role in safeguarding patient privacy in secondary usage of EHR.


Asunto(s)
Registros Electrónicos de Salud , Humanos , Confidencialidad , Anonimización de la Información , Aprendizaje Profundo , Estados Unidos , Australia , Procesamiento de Lenguaje Natural
13.
Free Radic Biol Med ; 223: 144-159, 2024 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-39084577

RESUMEN

Parkinson's disease is a progressive neurodegenerative disease that affects the motor and non-motor circuits of the brain. Currently, there are no promising therapeutic measures for Parkinson's disease, and most strategies designed to alleviate the Parkinson's disease are palliative. The dearth of therapeutic interventions in Parkinson's disease has driven attention in the search for targets that may augment dopamine secretion, promote differentiation towards dopaminergic neuronal lineage, or aid in neuroprotection from neuronal stress and inflammation, and prevent Parkinson's disease associated motor impairment and behavioural chaos. The study first reports that Rev-erbα plays an important role in regulating the differentiation of undifferentiated neuronal cells towards dopaminergic neurons through abating Sox2 expression in human SH-SY5Y cells. Rev-erbα directly binds to the human Sox2 promoter region and represses their expression to promote differentiation towards dopaminergic neurons. We have reported a novel mechanism of Rev-erbα which effectively abrogates 1-methyl-4-phenylpyridinium induced cytotoxicity, inflammation, and oxidative stress, exerted a beneficial effect on transmembrane potential, and suppressed apoptosis in the neuronal in vitro model of Parkinson's disease. Rev-erbα ligand SR9011 was observed to ease the disease severity in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine induced mouse model of Parkinson's disease. Rev-erbα alleviates the locomotor behavioural impairment, prevents cognitive decline and promotes motor coordination in mice. Administration of Rev-erbα ligand also helps in replenishing the dopaminergic neurons and abrogating the neurotoxin mediated toxicity in an in vitro and in vivo Parkinson's disease model. We conclude that Rev-erbα emerges as a moonlighting nuclear receptor that could be targeted in the treatment and alleviation of Parkinson disease.


Asunto(s)
Neuronas Dopaminérgicas , Neurogénesis , Miembro 1 del Grupo D de la Subfamilia 1 de Receptores Nucleares , Factores de Transcripción SOXB1 , Neuronas Dopaminérgicas/metabolismo , Neuronas Dopaminérgicas/patología , Neuronas Dopaminérgicas/efectos de los fármacos , Animales , Miembro 1 del Grupo D de la Subfamilia 1 de Receptores Nucleares/metabolismo , Miembro 1 del Grupo D de la Subfamilia 1 de Receptores Nucleares/genética , Humanos , Ratones , Neurogénesis/efectos de los fármacos , Factores de Transcripción SOXB1/metabolismo , Factores de Transcripción SOXB1/genética , Enfermedades Neuroinflamatorias/metabolismo , Enfermedades Neuroinflamatorias/patología , Diferenciación Celular , Enfermedad de Parkinson/metabolismo , Enfermedad de Parkinson/patología , Enfermedad de Parkinson/genética , Estrés Oxidativo/efectos de los fármacos , Apoptosis
14.
J Cancer Res Ther ; 20(3): 881-887, 2024 Apr 01.
Artículo en Inglés | MEDLINE | ID: mdl-39023595

RESUMEN

INTRODUCTION: Oral squamous cell carcinoma is a major cause of death throughout the developed world. Human papillomavirus (HPV) type 16 has also been suggested to play a role in etiology of head and neck squamous cell carcinoma (HNSCC). p16 expression is now being used as a surrogate marker of HPV infection in squamous cell carcinoma. Dysfunction in the p53 tumor suppressor gene is implicated in many cancers, including head and neck cancer. Overexpression or mutation of EGFR is found in 80%-100% of the patients with HNSCC, and is associated with poor prognosis and decreased survival. MATERIALS AND METHODS: In this cross-sectional observation study, total of 100 cases of HNSCC were taken. p16, p53, and EGFR expression was determined by immunohistochemical staining and correlated with clinicopathological parameters. p16 expression was also correlated with expression of p53 and EGFR. The obtained results were analyzed and evaluated using Chi-square test, value of P < 0.05 was taken significant. RESULTS: p16, p53, and EGFR were positive in 60%, 44%, and 58% cases, respectively. A statistically significant association was observed between p16 with age, site of the tumor, abnormal sexual habits and lymph node involvement. Significant expression also seen between p53 with age and abnormal sexual habits and immunohistochemical expression of p16 with p53 and EGFR. CONCLUSION: Immunohistochemical expression of p16 can be used as a surrogate marker of HPV. Study of p16, p53, and EGFR expression may provide clinicians with more exact information in order to evaluate tumor aggressiveness and treatment modalities.


Asunto(s)
Biomarcadores de Tumor , Inhibidor p16 de la Quinasa Dependiente de Ciclina , Receptores ErbB , Neoplasias de Cabeza y Cuello , Carcinoma de Células Escamosas de Cabeza y Cuello , Proteína p53 Supresora de Tumor , Humanos , Receptores ErbB/metabolismo , Receptores ErbB/genética , Proteína p53 Supresora de Tumor/metabolismo , Proteína p53 Supresora de Tumor/genética , Masculino , Femenino , Inhibidor p16 de la Quinasa Dependiente de Ciclina/metabolismo , Inhibidor p16 de la Quinasa Dependiente de Ciclina/genética , Persona de Mediana Edad , Carcinoma de Células Escamosas de Cabeza y Cuello/patología , Carcinoma de Células Escamosas de Cabeza y Cuello/virología , Carcinoma de Células Escamosas de Cabeza y Cuello/metabolismo , Carcinoma de Células Escamosas de Cabeza y Cuello/mortalidad , Carcinoma de Células Escamosas de Cabeza y Cuello/genética , Neoplasias de Cabeza y Cuello/patología , Neoplasias de Cabeza y Cuello/metabolismo , Neoplasias de Cabeza y Cuello/virología , Neoplasias de Cabeza y Cuello/genética , Anciano , Adulto , Biomarcadores de Tumor/metabolismo , Biomarcadores de Tumor/genética , Estudios Transversales , Infecciones por Papillomavirus/complicaciones , Infecciones por Papillomavirus/virología , Infecciones por Papillomavirus/patología , Infecciones por Papillomavirus/metabolismo , Inmunohistoquímica , Carcinoma de Células Escamosas/patología , Carcinoma de Células Escamosas/metabolismo , Carcinoma de Células Escamosas/virología , Carcinoma de Células Escamosas/genética , Pronóstico
15.
Med J Armed Forces India ; 80(4): 404-411, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-39071760

RESUMEN

Adenoid cystic carcinoma (ACC) is an uncommon tumor that usually appears in the major salivary glands of the head and neck region, including the minor glands in the oral cavity, sinonasal tract, and other sites. ACC of the head and neck may have a low-grade histological appearance. This malignant tumor has unusual clinical characteristics such as occasional regional lymph node metastases and a prolonged yet continuously advancing clinical course. Additionally, it is an invasive tumor with perineural invasion, difficult-to-clear margins, metastasis, and localized recurrence. The cribriform and tubular proliferation of basaloid cells, which mostly display a myoepithelial cellular phenotype, are ACC's distinct histologic characteristics. The degree of genetic alterations and aneuploidy observed in tumor genomes are linked to the severity of histologic grade, which correlates with clinical prognosis. The three predominant cell types (PCTs) i.e., conventional ACC (C-ACC), myoepithelial-predominant ACC (M-ACC), and epithelial-predominant ACC (E-ACC)-and their respective applications will be reviewed. The function of extracellular matrix (ECM) components such as laminin, type IV collagen, fibronectin, and tenascin are also emphasized. An attempt has been made to explore the recent molecular diversity, regulatory pathways prevalent in PCT, ECM with its genetic changes, and translational utility with targeted therapies for ACC.

17.
Aust Endod J ; 2024 Jul 01.
Artículo en Inglés | MEDLINE | ID: mdl-38946250

RESUMEN

Transverse root fracture (TRF) is classified as a cervical, middle or apical third root fracture on a periapical radiograph. The International Association of Dental Traumatology (IADT) suggests that cone-beam computed tomography (CBCT) should be considered, when conventional radiographs provide 'insufficient' information for diagnosis and treatment planning. Considering that CBCT can divulge additional information, it would be beneficial to have a clinically pertinent three-dimensional classification for TRF. The proposed alphanumeric classification includes the traumatised tooth number, describes the number of TRF, the facial and lingual location of each fracture line on the anatomic root, and its position relative to the crest of the alveolar bone. Further, diastasis, displacement of the coronal fragment and status of the alveolar bone at the site of TRF are also documented. This comprehensive classification system would provide a standard format for reporting, aid in referral communication and can be applied for future outcome studies on TRF.

18.
Indian J Otolaryngol Head Neck Surg ; 76(3): 2257-2272, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38883453

RESUMEN

Owing to high global prevalence, incidence and associated mortality, cancer of head and neck particularly oral cancer remains a cardinal domain for research and trials. Immune-modulatory therapies that employ patients own immune system for therapeutic benefits in oral cancer seems promising. The aim of this review is to gauge the potential of immunotherapy as fourth domain of Oral cancer therapeutics. Articles were searched using suitable search terms in MEDLINE and Google Scholar database to include clinical trials, meta-analyses, and research in humans/animals/cell lines published in peer reviewed journals. A total of 97 articles were included in this review. Literature has several studies and trials where different types of immunotherapies has been attempted but it is crucial to identify precise biomarkers of genome based targeted agents and to find parameters to select patients who might benefit from immunotherapy. Also further research is required to estimate predictive value of tumor mutational burden and mutational signatures so as to aid in personalized prediction of oral cancer therapeutic response.

19.
Chembiochem ; 25(16): e202400162, 2024 Aug 19.
Artículo en Inglés | MEDLINE | ID: mdl-38874536

RESUMEN

Pain management following acute injury or post-operative procedures is highly necessary for proper recovery and quality of life. Opioids and non-steroidal anti-inflammatory drugs (NSAIDS) have been used for this purpose, but opioids cause addiction and withdrawal symptoms whereas NSAIDS have several systemic toxicities. Derivatives of the naturally occurring iboga alkaloids have previously shown promising behavior in anti-addiction of morphine by virtue of their interaction with opioid receptors. On this frontier, four benzofuran analogs of the iboga family have been synthesized and their analgesic effects have been studied in formalin induced acute pain model in male Swiss albino mice at 30 mg/kg of body weight dose administered intraperitoneally. The antioxidant, anti-inflammatory and neuro-modulatory effects of the analogs were analyzed. Reversal of tail flick latency, restricted locomotion and anxiogenic behavior were observed in iboga alcohol, primary amide and secondary amide. Local neuroinflammatory mediators' substance P, calcitonin gene related peptide, cyclooxygenase-2 and p65 were significantly decreased whereas the depletion of brain derived neurotrophic factor and glia derived neurotrophic factor was overturned on iboga analog treatment. Behavioral patterns after oral administration of the best analog were also analyzed. Taken together, these results show that the iboga family of alkaloid has huge potential in pain management.


Asunto(s)
Benzofuranos , Modelos Animales de Enfermedad , Inflamación , Nocicepción , Animales , Ratones , Masculino , Benzofuranos/farmacología , Benzofuranos/química , Benzofuranos/uso terapéutico , Inflamación/tratamiento farmacológico , Inflamación/metabolismo , Nocicepción/efectos de los fármacos , Dolor Agudo/tratamiento farmacológico , Dolor Agudo/metabolismo , Analgésicos/farmacología , Analgésicos/química , Analgésicos/uso terapéutico
20.
Chemphyschem ; : e202400599, 2024 Jun 17.
Artículo en Inglés | MEDLINE | ID: mdl-38884606

RESUMEN

An electrochemical N-acylation of sulfoximine has been achieved via the coupling of α-keto acids and NH-sulfoximines. This process involves the sequential cleavage of C-C bond followed by C(sp2)-N bond formation, with the liberation of H2 and CO2 as the by-products. A library of N-aroylated sulfoximines is produced via the coupling of aroyl and sulfoximidoyl radicals by anodic oxidation under constant current electrolysis (CCE). The compatibility of the present protocol has been demonstrated by coupling of various bio-active compounds, such as NH-sulfoximine derived from (-)-borneol, L-menthol, D-glucose derivative, and some commercial drugs such as flurbiprofen, and ibuprofen. This late-stage functionalization highlights the importance of this sustainable protocol. Besides this, various control experiments and detection of H2 evolution have been performed to support the proposed mechanism.

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