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1.
J Obstet Gynaecol India ; 74(1): 38-44, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-38434120

RESUMO

Objective: The objective of the study was to determine the quality of life in women after peripartum hysterectomy using a Hindi version of the SF-36 questionnaire. Background: There are long-term effects on quality of life in women after peripartum hysterectomy. The effects on physical, mental, and social functioning have a prolonged recovery. No studies have been done in Indian women after peripartum hysterectomy to evaluate quality of life. Methods: Patients who underwent peripartum hysterectomy from January 2017 to May 2021 were contacted to participate in the study. To determine the quality of life post-surgery, a Hindi version of the 36-item Short-Form Health Survey (SF-36) was used for a face-to-face personal interview-based assessment. The participants were divided into two groups based on the duration between surgery and the interview. The aggregate scores for the eight components of SF-36 were calculated, and responses were analyzed. Results: Out of the 138 post-hysterectomy women, 118 were enrolled in the study. Women who could not be contacted [14 (10.14%)] and those who died post-procedure [6 (4.35%)] were excluded. Out of the total, 43 assessed participants were within 2 years of surgery, and 75 were after 2 years of surgery. The group that was assessed after 2 years of surgery had a significantly lower quality of life in six, out of the eight aspects of SF-36 domains. Conclusion: Women after peripartum hysterectomy undergo a prolonged recovery phase with effects on physical, mental, and social functioning. A multi-disciplinary long-term follow-up including physiotherapy and psychotherapy is required and that should be guided by a dedicated clinical team.

2.
Cureus ; 16(1): e52961, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38406148

RESUMO

Background and aim The regional anesthesia technique is commonly used for upper extremity surgery as an alternative to general anesthesia. The study aimed to compare the efficacy of infraclavicular brachial plexus block (BPB) and a combination of infraclavicular brachial plexus block with suprascapular nerve block for postoperative analgesia in patients undergoing shoulder surgeries. Method A total of 62 patients of both sexes with the American Society of Anaesthesiologists (ASA) physical status I/II/III, aged between 18 and 65 years, and undergoing shoulder surgery, were included in this prospective, single-blinded, randomized controlled trial. Patients were equally allocated into two groups: 31 in group A and 31 in group B. After pre-anesthetic evaluation, the purpose and protocol of the study were explained to patients, and informed consent was obtained. Thirty-one patients in group A were given infraclavicular brachial plexus block using 30 ml 0.375% bupivacaine while 31 patients in group B were given a combination of infraclavicular brachial plexus block using 30 ml 0.375% bupivacaine and suprascapular nerve block using 5 ml 0.375% bupivacaine. Blocks were given using ultrasound guidance and a peripheral nerve stimulator; the suprascapular block was given in the sitting position while the infraclavicular block was provided in the supine position. General anesthesia was administered in the operation theatre in the supine position after the administration of blocks. The pain was assessed using the visual analog scale (VAS) and the satisfaction score was assessed by the numeric rating scale (NRS). The Mann-Whitney U test was applied for comparison of pain between the two groups. The chi-square test was utilized for comparing the categorical variables. Result The postoperative pain was significantly lower (p<0.001) in group B as compared to group A at all the periods of observation, i.e., 0h (2.77±0.72 vs. 5.42±0.77), 6h (3.89±0.70 vs. 5.94±0.73), 12h (5.66±0.93 vs. 6.58±0.88), and 24h (6.16±0.80 vs. 6.74±0.90). These findings illustrate that group B patients who received a combination of infraclavicular brachial plexus block and suprascapular nerve block for shoulder surgeries had better pain relief than group A patients who received only the infraclavicular approach. The mean NRS score of patient satisfaction in group B (7.26±0.58) was significantly higher (p<0.001) in comparison to group A (6.16±0.64). Diaphragmatic palsy was observed in only one case in group A and none in group B. No other complication was observed in any of the patients during the study period. Conclusion The combination of infraclavicular brachial plexus block and suprascapular nerve block displays a positive postoperative analgesic profile with less usage of rescue analgesic doses and better patient satisfaction after shoulder surgery.

3.
Sultan Qaboos Univ Med J ; 23(2): 220-226, 2023 May.
Artigo em Inglês | MEDLINE | ID: mdl-37377822

RESUMO

Objectives: Post-operative pain after a modified radical mastectomy ranges from moderate to severe. Pectoralis (PECS) block has been found to be more effective than erector spinae block in reducing pain and the consumption of rescue analgesia in the post-operative period. This study aimed to compare the effect of erector spinae block and PECS block on the quality of recovery after modified radical mastectomy using the quality of recovery (QoR-40) score. Methods: This randomised controlled study was conducted at King George's Medical University, Lucknow, India, from 9th October 2020 to 9th October 2021. After general anaesthesia, patients were given blocks according to computer-generated randomisation: Group I: PEC I and PEC II (PECS) blocks; Group II: erector spinae plane (ESP) block; and Group III: control group (no intervention). The QoR-40 score was observed on the morning of the surgery and after 24 hours. Time to rescue analgesia and the total consumption of rescue analgesia in the first 24 hours were also observed. Results: A total of 90 patients were included (30 in each group). In the post-operative period after 24 hours, global QoR-40 scores were 183.64 ± 6.36, 179.68 ± 6.38 and 171.37 ± 6.88 in the PECS, ESP and control groups (P <0.0001). But there was no statistically significant difference between the QoR scores of PECS and ESP group patients (P = 0.0551). The total requirement of rescue analgesic was significantly lower in the PECS group (137.28 ± 31.46 mg) than in the ESP (189.46 ± 42.98 mg) and control (229.57 ± 46.80 mg) groups (P <0.0001). Time to first rescue analgesia was significantly higher in the PECS group (6.53 ± 2.78 hours) than in the ESP (4.05 ± 2.91 hours) and control (2.15 ± 1.51 hours) groups (P <0.0001). Conclusion: Both ESP and PECS blocks were effective in improving the QoR score and in reducing the consumption of rescue analgesia after modified radical mastectomy.


Assuntos
Analgesia , Neoplasias da Mama , Bloqueio Nervoso , Humanos , Feminino , Mastectomia Radical Modificada , Anestésicos Locais , Neoplasias da Mama/cirurgia , Analgésicos Opioides , Mastectomia , Dor Pós-Operatória/tratamento farmacológico , Dor Pós-Operatória/prevenção & controle
4.
Bioorg Chem ; 133: 106380, 2023 04.
Artigo em Inglês | MEDLINE | ID: mdl-36731295

RESUMO

The present study reports a series of 3-aryl-3H-benzopyran-based amide derivatives as osteogenic agents concomitant with anticancer activity. Six target compounds viz 22e, 22f, 23i, and 24b-d showed good osteogenic activity at 1 pM and 100 pM concentrations. One of the potential molecules, 24b, effectively induced ALP activity and mRNA expression of osteogenic marker genes at 1 pM and bone mineralization at 100 pM concentrations. These molecules also presented significant growth inhibition of osteosarcoma (MG63) and estrogen-dependent and -independent (MCF-7 and MDA-MB-231) breast cancer cells. The most active compound, 24b, inhibited the growth of all the cancer cells within the IC50 10.45-12.66 µM. The mechanistic studies about 24b showed that 24b induced apoptosis via activation of the Caspase-3 enzyme and inhibited cancer cell migration. In silico molecular docking performed for 24b revealed its interaction with estrogen receptor-ß (ER-ß) preferentially.


Assuntos
Antineoplásicos , Benzopiranos , Benzopiranos/farmacologia , Amidas/farmacologia , Simulação de Acoplamento Molecular , Antineoplásicos/farmacologia , Receptor beta de Estrogênio/metabolismo , Apoptose , Proliferação de Células , Linhagem Celular Tumoral
5.
J Pediatr Surg ; 58(2): 263-265, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36376124

RESUMO

AIMS OF STUDY: Anterior urethral valves (AUVs) are rare congenital anomalies causing lower urinary tract obstruction in children. The present study highlights the clinical approach in identifying the condition and its treatment options. METHOD: Single centre, retrospective study of children. RESULT: Over a 16 year duration, 14 children were diagnosed with AUVs and diverticula with a mean age of 15 months. Clinical features included straining at micturation and a palpable penile swelling. Diagnosis was confirmed with voiding cystourethrogram and cystoscopy. An open surgical procedure was performed in 12 cases and endoscopic intervention done in one. On follow up 13 patients showed restoration of a normal voiding stream and normal renal function. One child died of chronic renal failure due to a delayed presentation, severe back-pressure changes, urinary ascites, and urosepsis. One patient developed a small urethrocutaneous fistula that healed spontaneously. CONCLUSION: AUV, though rare, should be recognizable due to the combination of a poor urinary stream and visible swelling in the ventral aspect of penis. Open surgical excision is the method of choice, and the outcome is excellent. LEVEL OF EVIDENCE: Level IV.


Assuntos
Divertículo , Doenças Uretrais , Criança , Masculino , Humanos , Lactente , Uretra/cirurgia , Uretra/anormalidades , Estudos Retrospectivos , Doenças Uretrais/diagnóstico , Doenças Uretrais/cirurgia , Cistoscopia , Divertículo/diagnóstico por imagem , Divertículo/cirurgia
6.
Indian J Anaesth ; 67(12): 1051-1060, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-38343679

RESUMO

Background and Aims: Cancer pain guidelines remain confined due to implementation barriers, preventing them from attaining a global perspective. The guidelines must be robust in development and inculcate high-quality content to achieve practical utility. Quality indicators related to safe opioid practice empower effective guideline implementation. Methods: The protocol was registered prospectively in PROSPERO (CRD42021244823). Guidelines published over the last decade providing insights into cancer pain management and incorporating safe opioid practice were evaluated. The review's primary outcome was to evaluate the quality of cancer pain guidelines. Appraisal of guidelines for research and evaluation II (AGREE II) instrument was used to assess a guideline's quality. The ADAPTE collaboration-guideline adaptation resource tool kit (ADAPTE) provided insights into its adaptation based on specific questions within the guideline. Results: Fourteen cancer pain guidelines met the eligibility criteria and were included for quality evaluation. Eight guidelines were evaluated with combined AGREE II and ADAPTE process, attaining >66.7% in the rigour of development domain score, summated scaled domain score, and specific ADAPTE tools to evaluate the quality of each guideline. The intra-class correlation coefficient was utilised for resolving inter-rater agreement. 'Safe opioid practice' within a guideline was assessed for quality content implementation. Conclusion: Combined AGREE II and ADAPTE identified four cancer pain guidelines, namely Ministry of Health Malaysia, National Comprehensive Cancer Network, NCEC-National Clinical Guideline, and World Health Organization, which were of the highest quality and incorporated safe opioid practice effectively.

7.
Am J Dermatopathol ; 44(7): 519-522, 2022 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-35385850

RESUMO

ABSTRACT: A case of lupus erythematosus tumidus (LET), a subtype of chronic cutaneous lupus erythematosus, in an 85-year-old woman who presented with discrete indurated erythematous plaques over the face and upper chest is described. A skin biopsy showed features in keeping with a diagnosis of LET. Unusually however, the lymphocytic infiltrate contained frequent macrophages that demonstrated hemophagocytosis. Most of the phagocytosed cells were lymphocytes, but there was also evidence of erythrophagocytosis. The presence of conspicuous hemophagocytosis has only rarely been reported in skin biopsies of patients with autoimmune conditions. These include systemic lupus, neonatal lupus and dermatomyositis, and on 2 occasions in cases of nonspecified cutaneous lupus erythematosus. To the best of our knowledge, hemophagocytosis as a feature of LET has not been previously described in the literature.


Assuntos
Lúpus Eritematoso Cutâneo , Lúpus Eritematoso Discoide , Lúpus Eritematoso Sistêmico , Linfo-Histiocitose Hemofagocítica , Idoso de 80 Anos ou mais , Feminino , Humanos , Recém-Nascido , Lúpus Eritematoso Cutâneo/patologia , Lúpus Eritematoso Discoide/patologia , Linfo-Histiocitose Hemofagocítica/complicações , Pele/patologia
8.
J Obstet Gynaecol India ; 71(4): 424-429, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34566303

RESUMO

BACKGROUND: The cases of intrauterine contraceptive device (IUCD) with missing strings have risen due to increasing popularity of postpartum IUCD in Indian women. This has lead to increase in the burden of referral cases in tertiary care centres. Manual vacuum aspiration (MVA) device is a cheap and non-invasive method, well established for surgical abortion in first trimester of pregnancy. This study was undertaken to assess if MVA device can be used in retrieving IUCD in low resource setting, hence, reducing the need for referral or need of expensive and invasive techniques. METHOD: A prospective interventional study was conducted over a period of 6 months. A total of 50 women who were desirous of IUCD removal with non-visibility of strings at the external cervical os were included in the study. All cases were more than 12 weeks postpartum and had an ultrasound confirmed intrauterine location of IUCD. Women with pregnancy, extrauterine location of IUCD, active pelvic infection and cervical cancer were excluded. RESULTS: The incidence of IUCD with missing strings was 19.4%. Almost a third of the cases (36%) were referred from outside Delhi for IUCD removal to our centre. In 30% cases IUCD could successfully be removed using the MVA device. Majority of the IUCDs were inserted in hospital by a gynaecologist (90%), and most of the insertions were post-placental (62%). CONCLUSION: Retrieval of IUCD with missing strings with MVA device is a novel method and can be an initial approach in low resource setting before referral to a higher centre for management.

9.
Am J Dermatopathol ; 43(11): 822-826, 2021 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-33606379

RESUMO

ABSTRACT: A case of localized argyria in a 36-year-old female jeweler is described who presented with 2 discrete and asymptomatic bluish-black pigmented macules on the pulp of her left middle finger. A skin biopsy from both lesions demonstrated deposition of brown/black pigmented granules along the basement membrane zone of eccrine glands, blood vessels, nerves, and the dermo-epidermal junction fully in keeping with silver deposition. In addition, there was yellow-brown deposition seen within the interstitial dermis mimicking an early form of ochronosis, so called "pseudo-ochronosis." This latter feature is rarely described in cases of argyria. Transmission electron microscopy and energy dispersive x-ray spectroscopy confirmed the presence of electron dense particles up to 150 nm in diameter and the presence of silver, respectively. On further questioning, the patient had a history of localized and chronic exposure to silver, which specifically involved holding and manipulating silver wires and rings over the left middle finger. This case highlights an unusual and rare presentation of localized argyria in a jeweler. In addition, our case showed preferential silver deposition on dermal elastic fibers which has not been previously described in the literature.


Assuntos
Argiria/patologia , Dermatite Ocupacional/patologia , Joias , Adulto , Argiria/diagnóstico , Argiria/etiologia , Feminino , Dedos , Dermatoses da Mão/induzido quimicamente , Dermatoses da Mão/patologia , Humanos , Ocronose/patologia
10.
Molecules ; 25(22)2020 Nov 21.
Artigo em Inglês | MEDLINE | ID: mdl-33233418

RESUMO

Construction of a focused library of polycyclic ether-benzopyrans was undertaken in order to discover new therapeutic compounds that affect Leishmania growth and infectivity. This is especially of interest since there are few drug therapies for leishmaniasis that do not have serious drawbacks such high cost, side effects, and emerging drug resistance. The construction of these polycyclic ether-benzopyrans utilized an acetoxypyranone-alkene [5+2] cycloaddition and the Suzuki-Miyaura cross-coupling. The multi-gram quantity of the requisite aryl bromide was obtained followed by effective Pd-catalyzed coupling with boronic acid derivatives. Compounds were tested in vitro using the parasitic protozoan, Leishmania tarentolae. Effects of concentration, time, and exposure to light were evaluated. In addition, the effects on secreted acid phosphatase activity and nitric oxide production were investigated, since both have been implicated in parasite infectivity. The data presented herein are indicative of disruption of the Leishmania tarentolae and thus provide impetus for the development and testing of a more extensive library.


Assuntos
Benzopiranos/síntese química , Benzopiranos/farmacologia , Éter/síntese química , Éter/farmacologia , Leishmania/efeitos dos fármacos , Compostos Policíclicos/síntese química , Compostos Policíclicos/farmacologia , Fosfatase Ácida/metabolismo , Benzopiranos/química , Brometos/química , Catálise , Contagem de Células , Reação de Cicloadição , Ensaios Enzimáticos , Leishmania/enzimologia , Leishmania/crescimento & desenvolvimento , Neuroglia/efeitos dos fármacos , Neuroglia/metabolismo , Paládio/química , Compostos Policíclicos/química
11.
J Cancer Res Ther ; 16(3): 534-538, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32719263

RESUMO

BACKGROUND AND OBJECTIVE: Glossopharyngeal nerve block (GNB) technique has been used as alternative of treatment of cancer and noncancer pain of the oral cavity. The objective of the study is to compare the two approaches (extraoral and intraoral) of GNB in patients of carcinoma of the tongue in terms of efficacy, duration, and complications. MATERIALS AND METHODS: This was a prospective comparative randomized study over a period of 1 year. Fifty patients of either sex of ASA physical status and 2, between 21 and 70 years of age, suffering from carcinoma of the tongue, were selected. The patients were randomly divided into two groups. Group I received 4 mL of 0.5% bupivacaine combined with 40 mg, of triamcinolonacetonide by extraoral approach of GNB, and Group II received the same amount of drug by intraoral approach of GNB. Hemodynamic parameters, degree of pain relief using visual analog scale (VAS), number of attempts, effect on quality of life (QOL), and complication were noted during the performance of GNB. RESULTS: Demographic profile in both groups was comparable. Rate of complication and number of attempts to complete intervention were higher in Group I, which was found to be statistically significant. However, mean VAS scores in Group I were significantly higher as compared to those in Group II during most of the study period starting from the 1st follow-up at 30 min to the 2nd month postintervention (P < 0.05). No statistically significant difference in mean QOL scores of two groups was observed for the entire study period except at 1 week when mean scores in Group I were higher as compared to those in Group II (P = 0.011). CONCLUSION: The intraoral approach of GNB was better with respect to pain control and improvement in QOL whereas the rate of complication and number of attempts was lower in extraoral approach of GNB.


Assuntos
Bupivacaína/administração & dosagem , Dor do Câncer/terapia , Nervo Glossofaríngeo/efeitos dos fármacos , Bloqueio Nervoso/métodos , Manejo da Dor/métodos , Neoplasias da Língua/terapia , Triancinolona Acetonida/administração & dosagem , Adenocarcinoma/patologia , Adenocarcinoma/terapia , Adulto , Idoso , Anestésicos Locais/administração & dosagem , Anti-Inflamatórios/administração & dosagem , Dor do Câncer/etiologia , Dor do Câncer/patologia , Vias de Administração de Medicamentos , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Estudos Prospectivos , Qualidade de Vida , Neoplasias da Língua/patologia , Adulto Jovem
12.
Interdiscip Sci ; 11(3): 337-347, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29128919

RESUMO

Campylobacteriosis is a deadly disease which has developed resistance to most of the available chemotherapeutic agents. Although various studies provide evidence of acquired immunity following exposure to Campylobacter jejuni, no effective vaccine has been developed, still. Hence, there is an urgent need to identify potential vaccine candidates for Campylobacter species. In the proposed study, Campylobacter jejuni subsp. jejuni serotype O:2 (strain NCTC 11168) was taken and computational approach was employed to screen C. jejuni genome for promising vaccine candidates. From 1623 protein-coding sequences, 37 potential antigens were screened for epitope prediction based on surface association, consensus antigenicity predictions, solubility, transmembrane domain, and ortholog analysis. Comprehensive immunogenic analysis of these 37 antigens revealed that antigen Q0PA22 shows the greatest potential for experimental immunogenicity analysis. It has several potential CD4+ and CD8+ T-cell epitopes, as well as high probability of B-cell epitope regions as compared to well-characterized antigen Omp18 (Uniprot ID:Q0PC24). Among the highest scoring predicted epitopes, an optimal set of epitopes with respect to overall immunogenicity in target populations for campylobacteriosis viz. Europe, North America and Southwest Asia was determined. An epitope AMLTYMQWL from antigen no. 6(Q0PA22) binds to the most prevalent allele HLA-A*0201, and this epitope has most immunogenicity for all the target populations. In addition, this epitope exhibited highly significant TCR-pMHC interactions having a joint Z value of 4.87. Homology mapping studies of the predicted epitope show best homology to a well-studied antigenic peptide from influenza virus H5N1. Therefore, the predicted epitope might be a suitable vaccine candidate.


Assuntos
Vacinas Bacterianas/farmacologia , Infecções por Campylobacter/prevenção & controle , Campylobacter jejuni/genética , Genoma Bacteriano , Vacinologia , Animais , Biologia Computacional , Desenho de Fármacos , Epitopos , Epitopos de Linfócito B/imunologia , Epitopos de Linfócito T/imunologia , Humanos , Vírus da Influenza A , Complexo Principal de Histocompatibilidade , Camundongos , Redes Neurais de Computação , Peptídeos/imunologia , Proteoma
13.
South Asian J Cancer ; 5(4): 204-209, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-28032091

RESUMO

CONTEXT: Celiac plexus block (CPB) (is an effective way to reduce cancer-associated pain in upper abdominal malignancies. AIMS: To evaluate the efficacy and safety of different volumes of 70% alcohol in CPB. SETTINGS AND DESIGN: Prospective, randomized, controlled clinical study. SUBJECTS AND METHODS: Thirty patients of carcinoma gall bladder were randomly divided into three groups (n = 10) to receive 20, 30, and 40 ml of 70% alcohol in CPB. STATISTICAL ANALYSIS USED: All the continuous data were assessed analysis of variance followed by post-hoc tests (Tukey's Honestly Significant Difference test). Ordinal data were compared using Kruskal-Wallis H-test followed by Mann-Whitney U-test. Categorical comparisons were performed using Chi-square test. RESULTS: A significant difference in visual analog scale (VAS) score of Group I, Group I and Group III was observed from week 6 onward until the end of the study. At all these time intervals, VAS scores in Group I was higher than both Groups II and III during this time interval. VAS scores in Group III were significantly lower as compared to Group II from week 10 onward until the end of the study. As compared to baseline, at all the follow-up intervals, mean morphine requirement was significantly lower in Group II and Group III. A quality of life (QOL) score of Group III were higher as compared to Group I. Between Group II and Group III, significant difference was observed at week 16 only when Group III had a higher score as compared to Group II. CONCLUSIONS: VAS score, QOL, and reduction in morphine consumption were increased on increasing the volume of alcohol in CPB, 40 ml being most effective.

14.
Bioorg Med Chem Lett ; 26(21): 5322-5327, 2016 11 01.
Artigo em Inglês | MEDLINE | ID: mdl-27671497

RESUMO

Different alkyl amide (15a-l) and alkyl amine (16a-e) derivatives of 7,8-dimethoxy-3-hydroxy-2-(4-methoxyphenyl)benzopyran-4-one were synthesized and evaluated for their anticancer activity against five different cancer cell lines using SRB assay. Compounds 15e, 15i, 15j and 16a-e showed significant anticancer activity within the range of IC50 2.58-34.86µM. The most promising molecule, 16c, was further analyzed for its effect on cell cycle and apoptosis of estrogen receptor positive cancer cells (MCF-7 cells) which showed that 16c triggered apoptosis in MCF-7 cells and arrested cells population at sub-G0 (apoptotic) and G2M phase. In tubulin polymerization assay, 16c interfered with kinetics of tubulin polymerization.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Benzopiranos/síntese química , Benzopiranos/farmacologia , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Humanos , Concentração Inibidora 50 , Relação Estrutura-Atividade
15.
J Steroid Biochem Mol Biol ; 158: 63-75, 2016 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-26807865

RESUMO

Development of target oriented chemotherapeutics for treatment of chronic diseases have been considered as an important approach in drug development. Following this approach, in our efforts for exploration of new osteogenic leads, substituted 3-aryl-2H-benzopyran and 3-aryl-3H-benzopyran derivatives (19, 20a-e, 21, 22a-e, 26, 27, 28a-e, 29, 31a-b, 32 and 33) have been characterized as estrogen receptor-ß selective osteogenic (bone forming) agents. The synthesized compounds were evaluated for osteogenic activity using mouse calvarial osteoblast cells. Four compounds viz20b, 22a, 27and 32 showed significant osteogenic activity at EC50 values 1.35, 34.5, 407 and 29.5pM respectively. Out of these, 20b and 32 were analyzed for their bone mineralization efficacy and osteogenic gene expression by qPCR. The results showed that 20b and 32 significantly increased mineral nodule formation and the transcript levels of BMP-2, RUNX-2 and osteocalcin at 100pM concentrations respectively. Further mechanistic studies of 20b and 32 using transiently knocked down expression of ER-α and ß in mouse osteoblast (MOBs) showed that 20b and 32 exerts osteogenic efficacy via activation of estrogen receptor-ß preferentially. Additionally, compounds showed significant anticancer activity in a panel of cancer cell lines within the range of (IC50) 6.54-27.79µM. The most active molecule, 22b inhibited proliferation of cells by inducing apoptosis and arresting cell cycle at sub-G0 phase with concomitant decrease in cells at S phase.


Assuntos
Antineoplásicos/farmacologia , Benzopiranos/farmacologia , Osteogênese/efeitos dos fármacos , Fosfatase Alcalina/metabolismo , Animais , Antineoplásicos/síntese química , Apoptose/efeitos dos fármacos , Benzopiranos/síntese química , Ciclo Celular/efeitos dos fármacos , Diferenciação Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Receptor alfa de Estrogênio/genética , Receptor beta de Estrogênio/genética , Expressão Gênica/efeitos dos fármacos , Humanos , Camundongos , Osteoblastos/citologia , Osteoblastos/efeitos dos fármacos , Osteoblastos/metabolismo , RNA Interferente Pequeno/genética
16.
Pharm Biol ; 54(4): 740-5, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-26439487

RESUMO

CONTEXT: Argemone mexicana Linn. (Papaveraceae) has been used as traditional medicine in India and Taiwan for the treatment of skin diseases, inflammations, bilious, fever, etc. Some alkaloids of A. mexicana have been screened for their cytotoxicity on different cancer cell lines. OBJECTIVE: The study investigates potential cytotoxic effects of alkaloids isolated from aerial part of A. mexicana on SW480 human colon cancer cell line. MATERIALS AND METHODS: Six alkaloids, 13-oxoprotopine, protomexicine, 8-methoxydihydrosanguinarine, dehydrocorydalmine, jatrorrhizine, and 8-oxyberberine were isolated from the methanol extract of A. mexicana. Cytotoxicity of these alkaloids was studied on SW480 human colon cancer cell line at 1, 25, 50, 75, 100, 125, 150, and 200 µg/mL for 24 and 48 h. Cells were seeded in a 96-well micro-plate at a concentration of 2 × 10(4) cells per well and MTS assay was performed to assess cytotoxicity in terms of cell viability. RESULTS: At 200 µg/mL, protomexicine and 13-oxoprotopine showed mild cytotoxicity (∼24-28%) whereas dehydrocorydalmine exhibited moderate cytotoxicity (∼48%). 8-Oxyberberine was mildly cytotoxic (∼27%) at 24 h but was more potent (∼76%) at 48 h. Jatrorrhizine and 8-methoxydihydrosanguinarine were most potent (∼95-100%) in inhibiting the human colon cancer cell proliferation showing complete reduction in cell viability. DISCUSSION AND CONCLUSION: This is the first study on the effect of these alkaloids on SW480 human colon cancer cell line. This study indicates that some alkaloids of A. mexicana strongly inhibit the cell proliferation in human colon cancer cells, and it might be a basis for future development of a potent chemotherapeutic drug.


Assuntos
Alcaloides/farmacologia , Argemone , Neoplasias do Colo , Citotoxinas/farmacologia , Extratos Vegetais/farmacologia , Alcaloides/isolamento & purificação , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/fisiologia , Citotoxinas/isolamento & purificação , Relação Dose-Resposta a Droga , Humanos , Componentes Aéreos da Planta , Extratos Vegetais/isolamento & purificação
20.
J Oral Maxillofac Pathol ; 18(3): 420-2, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-25948999

RESUMO

Necrotizing sialometaplasia (NS) is a benign, self-limiting inflammatory reaction of salivary gland tissue which may mimic squamous cell carcinoma or mucoepidermoid carcinoma, both clinically and histologically, that creates diagnostic dilemma leading to unwarranted aggressive surgery. Most commonly affected site is the minor salivary glands of the palate. The pathogenesis is unknown but is believed to be due to ischemia of vasculature supplying the salivary gland lobules. A simple incisional biopsy is required to confirm the histological diagnosis and to rule out more serious disease processes. It is a self-limiting disease process and requires no treatment. It will be prudent to do repeat biopsy in case if the lesion does not heal within 3 months.

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