Drug Research最新文献

{"title":"Evaluation and Comparison of Citalopram and Venlafaxine for Management of Hot Flashes in Women with Breast Cancer.","authors":"Sasan Yaghoobi Taleghani,&nbsp;Farnaz Etesam,&nbsp;Mohsen Esfandbod","doi":"10.1055/a-2061-7020","DOIUrl":"10.1055/a-2061-7020","url":null,"abstract":"<p><strong>Background: </strong>Breast cancer is the most common cancer in women worldwide. Premature menopause and hot flashes are the main complications of breast cancer treatments. About 40 to 50 percent of breast cancer women who undergo chemotherapy are experiencing premature menopause symptoms, including hot flashes. Some endocrine therapies such as tamoxifen and aromatase inhibitors are associated with induction or aggravating hot flashes. Hot flashes are often debilitating and significantly impair daily functions. Therefore many therapeutic options have been studied so far for the management of this adverse effect. However, there are still some clinical challenges in managing hot flashes in patients with breast cancer.</p><p><strong>Objective: </strong>We aimed to evaluate and compare the efficacy of venlafaxine and citalopram on hot flashes in breast cancer women receiving tamoxifen.</p><p><strong>Design: </strong>We conducted a double-blind, placebo-controlled trial in forty-one, 35 to 65 years old female patients. The study lasted for four weeks, and the follow-up was for two months. Venlafaxine and citalopram treatments started with doses of 37.5 mg or 10 mg, respectively. Venlafaxine and citalopram dosages were increased in the second week to 75 and 20 mg, respectively. The study was conducted during the year 2017.</p><p><strong>Key results: </strong>The results indicated that the total efficacy was significantly different in groups receiving citalopram, venlafaxine, and placebo. Total efficacy in the placebo group, venlafaxine, and citalopram was 14.3, 53.8, and 64.3%, respectively (p=0.02). During the second week, the efficacy in groups receiving citalopram, venlafaxine, and placebo was 57.1, 53.8, and 14.3%, respectively (p=0.04). Generally, both citalopram and venlafaxine were well tolerated. The associated adverse effects were mild to moderate in both groups.</p><p><strong>Conclusions: </strong>Although citalopram was associated with more adverse effects, including constipation, it was more effective in reducing the frequency of hot flashes when compared to venlafaxine or placebo.</p>","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":" ","pages":"465-472"},"PeriodicalIF":2.2,"publicationDate":"2023-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10120776","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Altered Gene Expression of Cytochrome P450 and ABC Transporter in Human Hepatocellular Carcinoma HepG2 Cells Exposed to Bardoxolone Methyl.","authors":"Katsuhito Nagai,&nbsp;Shuhei Fukuno,&nbsp;Takeshi Miura,&nbsp;Eri Yasuda-Imanishi,&nbsp;Hiroki Konishi","doi":"10.1055/a-2111-6649","DOIUrl":"10.1055/a-2111-6649","url":null,"abstract":"Abstract Bardoxolone methyl (BX) is expected to be an innovate therapeutic agent for chronic kidney disease (CKD). The aim of the present study was to examine whether the expression of subtypes of cytochrome P450 (CYP) and ABC transporters was altered in human hepatocellular carcinoma HepG2 cells by exposure to BX. The expression of mRNAs for CYP1A2, CYP2E1, P-glycoprotein, multidrug resistance-associated protein 1–3, and breast cancer resistance protein was significantly increased by exposure of HepG2 cells to BX, while the expression of CYP3A4 mRNA was significantly decreased under the same conditions. BX had no significant effect on the expression of mRNAs for CYP2C9 and CYP2C19 in HepG2 cells. In conclusion, this study demonstrated that the gene expression of several CYPs and ABC transporters in HepG2 cells was altered when exposed to BX, suggesting the need to pay careful attention to drug-drug interactions in patients receiving BX for CKD treatment.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":" ","pages":"473-475"},"PeriodicalIF":2.2,"publicationDate":"2023-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10077515","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Lupeol: A Triterpenoid Isolated from the Stem Bark of Hymenocardia Acida (tul.) Exhibits a van der Waal Antagonism on the Alpha Subunit of Gastric H+K+Atpase - A Promising Antiulcer Principle.","authors":"Adedokun Oluwasegun,&nbsp;Ume Ogochukwu,&nbsp;Ojukwu Ugochukwu,&nbsp;Ismail Mussaddiq,&nbsp;Ayinde Bunyamin","doi":"10.1055/a-2132-6475","DOIUrl":"10.1055/a-2132-6475","url":null,"abstract":"<p><strong>Background: </strong><i>Hymenocardia acida</i> (HA) is one of the numerous medicinal plants in Nigeria with ethnomedicinal history of usage in the treatment of ulcer. The study aimed at isolating antiulcer principle(s) from the stem bark of HA as well as the mechanism of action determination.</p><p><strong>Methods: </strong>Antiulcer screenings of the crude extract, aqueous fraction, and bulked VLC fractions were performed using <i>in vivo</i> and <i>in vitro</i> models. Docking was carried out by using PyRx.</p><p><strong>Results: </strong>Crude extract (HA; 1 mg/mL) and the aqueous fraction of <i>H. acida</i> (HAA; 1 mg/mL) showed an acid neutralizing capacity (MEq) of 0.3948 and 0.4035, respectively which is significantly different from 0.431 MEq showed by negative control (distilled water) at <i>p</i><0.05. BVLC 3 (1 mg/mL) showed a significant value of 0.4049 MEq. However, HA showed a dose-dependent decrease in activity across doses examined, with 100 mg/kg showing an ulcer index of 10.00±2.89 (61.50%) and cimetidine (positive control; 100 mg/kg), also showed the highest ulcer index of 3.67±0.88 (85.9%), which is significantly different from ulcer index of 26.00±6.35 (0.00%) <i>p</i><0.05 observed in the negative control (5% dimethylsulphoxide). The highest ulcer index of 8.00±1.32 (65.10%) was noted in BVLC 3. Bioactive BVLC 3, resulted in an isolated compound (BF3B2A). The compound was suggested to be lupeol, with a docking score of -7.7. It showed a van der Waal interaction with some key amino acid residues in the vonoprazan binding site.</p><p><strong>Conclusion: </strong>The experimental studies justify the ethnomedicinal claim of usage among locals.</p>","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":" ","pages":"448-458"},"PeriodicalIF":2.2,"publicationDate":"2023-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10128363","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"AGE RAGE Pathways: Cardiovascular Disease and Oxidative Stress.","authors":"Neeraj Sharma,&nbsp;Pavan Kumar,&nbsp;Karuna Shanker Shukla,&nbsp;Shubhrat Maheshwari","doi":"10.1055/a-2047-3896","DOIUrl":"https://doi.org/10.1055/a-2047-3896","url":null,"abstract":"<p><p>It is well established that Advanced Glycation End Products (AGEs) and their receptor (RAGE) are primarily responsible for the development of cardiovascular disease. As a result, diabetic therapy is very interested in therapeutic strategies that can target the AGE-RAGE axis. The majority of the AGE-RAGE inhibitors showed encouraging outcomes in animal experiments, but more information is needed to completely understand their clinical effects. The main mechanism implicated in the aetiology of cardiovascular disease in people with diabetes is oxidative stress and inflammation mediated by AGE-RAGE interaction. Numerous PPAR-agonists have demonstrated favourable outcomes in the treatment of cardio-metabolic illness situations by inhibiting the AGE-RAGE axis. The body's ubiquitous phenomena of inflammation occur in reaction to environmental stressors such tissue damage, infection by pathogens, or exposure to toxic substances. Rubor (redness), calor (heat), tumour (swelling), colour (pain), and in severe cases, loss of function, are its cardinal symptoms. When exposed, the lungs develop silicotic granulomas with the synthesis of collagen and reticulin fibres. A natural flavonoid called chyrsin has been found to have PPAR-agonist activity as well as antioxidant and anti-inflammatory properties. The RPE insod2+/animals underwent mononuclear phagocyte-induced apoptosis, which was accompanied with decreased superoxide dismutase 2 (SOD2) and increased superoxide generation. Injections of the serine proteinase inhibitor SERPINA3K decreased proinflammatory factor expression in mice with oxygen-induced retinopathy, decreased ROS production, and increased levels of SOD and GSH.</p>","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":"73 7","pages":"408-411"},"PeriodicalIF":2.2,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10137487","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Effects of SGLT2 inhibitors on the intestinal bacterial flora in Japanese patients with type 2 diabetes mellitus.","authors":"Masataka Kusunoki,&nbsp;Fumiya Hisano,&nbsp;Shin-Ichi Matsuda,&nbsp;Akiko Kusunoki,&nbsp;Naomi Wakazono,&nbsp;Kazuhiko Tsutsumi,&nbsp;Tetsuro Miyata","doi":"10.1055/a-2037-5250","DOIUrl":"https://doi.org/10.1055/a-2037-5250","url":null,"abstract":"<p><p>Selective inhibitors of sodium glucose co-transporter-2 (SGLT2) suppress renal glucose reabsorption and promote urinary glucose excretion, thereby lowering blood glucose. SGLT2 inhibitors have been reported to reduce body weight. However, the mechanism underlying the reduction in the body weight induced by SGLT2 inhibitor treatment remains to be elucidated. In this study, we investigated the effects of SGLT2 inhibitors on the intestinal bacterial flora. A total of 36 Japanese patients with type 2 diabetes mellitus received a SGLT2 inhibitor (luseogliflozin or dapagliflozin) for 3 months, and the prevalences of balance-regulating bacteria and balance-disturbing bacteria in the feces of the patients before and after SGLT2 inhibitor treatment were determined. SGLT2 inhibitor treatment was associated with a significant increase of the overall prevalence of the 12 types of balance-regulating bacteria. In addition, significant increases in the prevalences of the short-chain fatty acid (SCFAs)-producing bacteria among the balance-regulating bacteria were also observed. Individual analyses of the balance-regulating bacteria revealed that the SGLT2 inhibitor treatment was associated with a significant increase in the prevalence of <i>Ruminococci,</i> which are balance-regulating bacteria classified as SCFAs-producing bacteria. However, SGLT2 inhibitor had no effect on the balance-disturbing bacteria. These results suggested that SGLT2 inhibitor treatment was associated with an overall increase in the prevalence of balance-regulating bacteria. Among the balance-regulating bacteria, the prevalences of SCFAs-producing bacteria increased. SCFAs have been reported to prevent obesity. The results of the present study suggest that SGLT2 inhibitors might induce body weight reduction via their actions on the intestinal bacterial flora.</p>","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":"73 7","pages":"412-416"},"PeriodicalIF":2.2,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10297448","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Correction: Artificial Intelligence for Computer-Aided Drug Discovery.","authors":"Aditya Kate,&nbsp;Ekkita Seth,&nbsp;Ananya Singh,&nbsp;Chandrashekhar Mahadeo Chakole,&nbsp;Meenakshi Kanwar Chauhan,&nbsp;Ravi Kant Singh,&nbsp;Shrirang Maddalwar,&nbsp;Mohit Mishra","doi":"10.1055/a-2105-9762","DOIUrl":"https://doi.org/10.1055/a-2105-9762","url":null,"abstract":"","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":"73 7","pages":"e2"},"PeriodicalIF":2.2,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10132499","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Artificial Intelligence for Computer-Aided Drug Discovery.","authors":"Aditya Kate,&nbsp;Ekkita Seth,&nbsp;Ananya Singh,&nbsp;Chandrashekhar Mahadeo Chakole,&nbsp;Meenakshi Kanwar Chauhan,&nbsp;Ravi Kant Singh,&nbsp;Shrirang Maddalwar,&nbsp;Mohit Mishra","doi":"10.1055/a-2076-3359","DOIUrl":"https://doi.org/10.1055/a-2076-3359","url":null,"abstract":"<p><p>The continuous implementation of Artificial Intelligence (AI) in multiple scientific domains and the rapid advancement in computer software and hardware, along with other parameters, have rapidly fuelled this development. The technology can contribute effectively in solving many challenges and constraints in the traditional development of the drug. Traditionally, large-scale chemical libraries are screened to find one promising medicine. In recent years, more reasonable structure-based drug design approaches have avoided the first screening phases while still requiring chemists to design, synthesize, and test a wide range of compounds to produce possible novel medications. The process of turning a promising chemical into a medicinal candidate can be expensive and time-consuming. Additionally, a new medication candidate may still fail in clinical trials even after demonstrating promise in laboratory research. In fact, less than 10% of medication candidates that undergo Phase I trials really reach the market. As a consequence, the unmatched data processing power of AI systems may expedite and enhance the drug development process in four different ways: by opening up links to novel biological systems, superior or distinctive chemistry, greater success rates, and faster and less expensive innovation trials. Since these technologies may be used to address a variety of discovery scenarios and biological targets, it is essential to comprehend and distinguish between use cases. As a result, we have emphasized how AI may be used in a variety of areas of the pharmaceutical sciences, including in-depth opportunities for drug research and development.</p>","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":"73 7","pages":"369-377"},"PeriodicalIF":2.2,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10133016","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Efficacy and Safety of Valproic Acid in Myelodysplastic Syndrome and Acute Myeloid Leukemia; a Narrative Review.","authors":"Navid Omidkhoda,&nbsp;Sina Mahdiani,&nbsp;Sara Samadi,&nbsp;Hossein Rahimi,&nbsp;Amir Hooshang Mohammadpour","doi":"10.1055/a-2088-3718","DOIUrl":"https://doi.org/10.1055/a-2088-3718","url":null,"abstract":"<p><p>Loads of new therapeutic regimes have been turned up to manage Myelodysplastic syndrome (MDS) and acute myeloid leukemia (AML), particularly in elderly patients who are unfit for intensive chemotherapy. Despite accumulating research, the best MDS and AML management approach is indeterminate. Myelodysplastic syndrome implies a group of various hematopoietic stem cell disorders that may progress to acute myeloid leukemia. These disorders are more frequent in older adults. To the high rate of morbidity and abundant toxicities related to the therapeutic approaches, also, the treatment would be challenging. The clinical effectiveness of valproic acid, a histone deacetylase inhibitor, in MDS and AML patients is unknown, even though it has demonstrated positive activities to promote differentiation and apoptosis in cancer cells. We investigated the clinical research on the effects of valproic acid in conjunction with various drugs, including low-dose cytarabine, all-trans retinoic acid, DNA-hypomethylating agents, hydrazine, and theophylline. We conclude that VPA is a safe and effective treatment option for MDS and AML patients, particularly when used in conjunction with all-trans retinoic acid, DNA-hypomethylating drugs, and hydralazine. However, more randomized clinical studies are required to identify an ideal regimen.</p>","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":"73 7","pages":"378-387"},"PeriodicalIF":2.2,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10141686","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Arsenic trioxide-induced cytotoxicity in A549 cells: The role of necroptosis.","authors":"Maryam Jamil,&nbsp;Afshin Mohammadi-Bardbori,&nbsp;Omid Safa,&nbsp;Amin Reza Nikpoor,&nbsp;Azizollah Bakhtari,&nbsp;Mahnoosh Mokhtarinejad,&nbsp;Saghar Naybandi Zadeh,&nbsp;Amir Shadboorestan,&nbsp;Mahmoud Omidi","doi":"10.1055/a-2076-3246","DOIUrl":"https://doi.org/10.1055/a-2076-3246","url":null,"abstract":"<p><strong>Introduction: </strong>Lung cancer is one of the deadliest cancers globally. Arsenic trioxide (ATO) is still present as a highly effective drug in treating acute promyelocytic leukemia (APL). Chemotherapy resistance is one of the major problems in cancer therapy. Necroptosis, can overcomes resistance to apoptosis, and can promote cancer treatment. This study examines the necroptosis pathway in A549 cancer cells exposed to ATO.</p><p><strong>Methods: </strong>We used the MTT test to determine the ATO effects on the viability of A549 cells at three different time intervals. Also, the reactive oxygen species (ROS) and mitochondrial membrane potential (MMP) were performed in three-time intervals. The effect of ATO on apoptosis was evaluated by Annexin V / PI staining and, the RIPK1 and MLKL gene expression were measured by Real-Time PCR.</p><p><strong>Results: </strong>The ATO has dose and time-dependent cytotoxic effects, so at 24, 48, and 72 h, the IC50 doses were 33.81 '11.44 '2.535 µM respectively. A 50 μM ATO is the most appropriate to increase the MMP loss significantly at all three times. At 24 and 48 h after exposure of cells to ATO, the ROS levels increased. The RIPK1 gene expression increased significantly compared to the control group at concentrations of 50 and 100 μM; however, MLKL gene expression decreased.</p><p><strong>Conclusions: </strong>The A549 cells, after 48 h exposure to ATO at 50 and 100 μM, induces apoptosis and necroptosis. Due to the reduced expression of MLKL, it can be concluded that ATO is probably effective in the metastatic stage of cancer cells.</p>","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":"73 7","pages":"417-425"},"PeriodicalIF":2.2,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10198331","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Phytopharmaceuticals and Herbal Approaches to Target Neurodegenerative Disorders.","authors":"Anas Islam,&nbsp;Anuradha Mishra,&nbsp;Rabia Ahsan,&nbsp;Syed Fareha","doi":"10.1055/a-2076-7939","DOIUrl":"https://doi.org/10.1055/a-2076-7939","url":null,"abstract":"<p><p>Neurodegeneration is characterized as the continuous functional and structural loss of neurons, resulting in various clinical and pathological manifestations and loss of functional anatomy. Medicinal plants have been oppressed from ancient years and are highly considered throughout the world as a rich source of therapeutic means for the prevention, treatment of various ailments. Plant-derived medicinal products are becoming popular in India and other nations. Further herbal therapies shows good impact on chronic long term illnesses including degenerative conditions of neurons and brain. The use of herbal medicines continues to expand rapidly across the world. The active phytochemical constituents of individual plants are sometimes insufficient to achieve the desirable therapeutic effects. Combining the multiple herbs in a particular ratio (polyherbalism) will give a better therapeutic effect and reduce toxicity. Herbal-based nanosystems are also being studied as a way to enhance the delivery and bioavailability of phytochemical compounds for the treatment of neurodegenerative diseases. This review mainly focuses on the importance of the herbal medicines, polyherbalism and herbal-based nanosystems and its clinical significance for neurodegenerative diseases.</p>","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":"73 7","pages":"388-407"},"PeriodicalIF":2.2,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10198354","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}