Advances in Pharmacological and Pharmaceutical Sciences最新文献

{"title":"Traditional Uses, Bioactive Compounds, and Pharmacological Investigations of <i>Calendula arvensis</i> L.: A Comprehensive Review.","authors":"Aya Khouchlaa, Aicha El Baaboua, Hamza El Moudden, Fatima Lakhdar, Saad Bakrim, Naoual El Menyiy, Omar Belmehdi, Hicham Harhar, Nasreddine El Omari, Abdelaali Balahbib, Moon Nyeo Park, Gokhan Zengin, Bonglee Kim, Abdelhakim Bouyahya","doi":"10.1155/2023/2482544","DOIUrl":"10.1155/2023/2482544","url":null,"abstract":"<p><p><i>Calendula arvensis</i> L. (Asteraceae) is a famous ornamental and medicinal plant widely distributed in Mediterranean countries and the southern region of Europe. This reputed species is widely used in traditional medicine in the treatment of many disorders and has various bioactivities, especially anti-inflammatory, antiviral, antimutagenic, antimicrobial, insecticidal, antioxidant, and immunomodulatory activities. The present review was conducted to provide a critical review of the comprehensive and current knowledge regarding <i>C. arvensis</i> species, in particular, its taxonomy and geographical distribution, botanical description, medicinal uses, phytochemical compounds, pharmacological properties, and toxicity investigations. The data collected on <i>C. arvensis</i> were obtained using different scientific research databases such as PubMed, SciFinder, SpringerLink, Web of Science, Science Direct, Google Scholar, Wiley Online, and Scopus. Phytochemical screening of different <i>C. arvensis</i> extracts and essential oils showed their richness in bioactive compounds, particularly in fatty acids, sterols, phenolics, flavonoids, saponins, tannins, alkaloids, and terpenoid compounds. The findings of this review showed that the pharmacological activities of <i>C. arvensis</i> confirm its importance and diversity as a traditional remedy for many diseases. This plant presents a wide range of bioactivities, namely, anti-inflammatory, antimicrobial, antitrypanosomial, antitumoral, antimutagenic, and immunomodulatory activities, as well as hemolytic properties and wound treatment. Nevertheless, pharmacokinetic validation and toxicological examinations are required to detect any possible toxicity for future clinical trials.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"2482544"},"PeriodicalIF":2.1,"publicationDate":"2023-01-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9831710/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10533049","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Toxicity, Antibacterial, and Phytochemical Analyses of <i>Antrocaryon klaineanum</i> Pierre Extracts.","authors":"Cédric Sima Obiang,&nbsp;Thiery Ndong Mba,&nbsp;Joseph Privat Ondo,&nbsp;Rick Léonid Ngoua Meye Misso,&nbsp;Juliette Ornely Orango Bourdette,&nbsp;Elvis Otogo N'Nang,&nbsp;Joefred Mbogho Abogho,&nbsp;Elvis Jolinom Mbot,&nbsp;Louis Clément Obame Engonga,&nbsp;Edouard Nsi Emvo","doi":"10.1155/2023/9304681","DOIUrl":"https://doi.org/10.1155/2023/9304681","url":null,"abstract":"<p><p>Medicinal plants are traditionally used in Gabon to treat several types of illnesses. The study's purpose was to determine the toxic, antibacterial, and anti-inflammatory effects of <i>Antrocaryon klaineanum</i> Pierre extracts and to characterize their phytochemical compounds. Toxicity was evaluated on frog tadpoles (<i>Phrynobatrachus africanus</i> Hallowell). The microorganism susceptibility test was performed by the diffusion method, while minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were evaluated using the microdilution technique. Anti-inflammatory activity was tested through protein denaturation and membrane stabilization methods. Chromatography and molecular network techniques were used to characterize chemical compounds. The lethality test showed that the lethal concentration (LC₅₀) increased from 110.03 ± 1.25 to 15.86 ± 2.21 <i>μ</i>g/mL after 24 and 96 hours of exposure. In tadpoles exposed to 7.81 <i>μ</i>g/mL extract, the first mortalities (12.5%) were observed on the fifth day of exposure. A relative decrease in mature erythrocytes exposed to plant extracts was observed. The antibacterial activity shows that the Ak F₂, Ak F₃, and Ak F₄ fractions (from the water-ethanol crude extract) gave the greatest antibacterial activities compared to the other extracts. The water, water-acetone, and water-ethanol extracts showed good inhibition of denaturation. The haemolysis test shows that the extracts exhibited good anti-inflammatory activities. Phytochemical characterisation revealed four major compounds, including monogallate epicatechin and hydroxy-ergostadian. The molecular network revealed five main clusters. Our study shows that <i>A. klaineanum</i> Pierre could be a promising natural product for the isolation of molecules with potential biological activities.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"9304681"},"PeriodicalIF":2.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10148743/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9399369","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Renoprotective Effect of Thai Patients with Type 2 Diabetes Mellitus Treated with SGLT-2 Inhibitors versus DPP-4 Inhibitors: A Real-World Observational Study.","authors":"Apichaya Chanawong,&nbsp;Suriyon Uitrakul,&nbsp;Supatcha Incomenoy,&nbsp;Natnicha Poonchuay","doi":"10.1155/2023/5581417","DOIUrl":"https://doi.org/10.1155/2023/5581417","url":null,"abstract":"<p><strong>Background: </strong>Recently, there is a lack of studies comparing the renoprotective effects of sodium-glucose cotransporter-2 (SGLT-2) inhibitors and dipeptidyl peptidase-4 (DPP-4) inhibitors. This study therefore aimed to investigate the renoprotective effects of SGLT-2 inhibitors and DPP-4 inhibitors on Thai patients with type 2 diabetes mellitus.</p><p><strong>Methods: </strong>Patient medication records of all patients who used those two antidiabetic classes at Fort Wachirawut Hospital were reviewed. Renal function tests, blood glucose levels, and other baseline characteristics were collected. Continuous variables were compared within the group using the Wilcoxon signed-rank test and between groups using the Mann-Whitney <i>U</i> test.</p><p><strong>Results: </strong>There were 388 and 691 patients with SGLT-2 inhibitors and DPP-4 inhibitors, respectively. The mean estimated glomerular filtration rate (eGFR) of the SGLT-2 inhibitor group was significantly lower from baseline at 18 months of treatment, as well as the DPP-4 inhibitor group. However, the trend of eGFR reduction in patients with baseline eGFR <60 mL/min/1.73 m² was smaller than those with baseline eGFR ≥60 mL/min/1.73 m². In addition, the fasting blood sugar and haemoglobin A1c levels significantly decreased from baseline in both the groups.</p><p><strong>Conclusions: </strong>Both SGLT-2 inhibitors and DPP-4 inhibitors showed the same trends of eGFR reductions from baseline in Thai patients with type 2 diabetes mellitus. However, SGLT-2 inhibitors should be considered in patients with impaired renal function rather than in all T2DM patients.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"5581417"},"PeriodicalIF":2.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10202602/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9518985","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Evaluation of the Combination of Metformin and Rapamycin in an MPP⁺-Treated SH-SY5Y Model of Parkinson's Disease.","authors":"Chureerat Norradee,&nbsp;Kawinthra Khwanraj,&nbsp;Tatcha Balit,&nbsp;Permphan Dharmasaroja","doi":"10.1155/2023/3830861","DOIUrl":"https://doi.org/10.1155/2023/3830861","url":null,"abstract":"<p><p>Metformin (MET) and rapamycin (RAPA) have been reported to protect against neurodegeneration in cellular and animal models of Parkinson's disease (PD). MET, which is a first-line drug for type 2 diabetes, and RAPA are known as mTORC1 inhibitors. MET also acts as an AMPK activator, which leads to the inhibition of mTORC1 activity. mTORC1 is a downstream target of Akt signaling. Inactivation of Akt/mTORC1 and its downstream S6K1 can promote autophagy, a process involved in PD pathogenesis. Based on their mechanisms and potential benefits, we evaluated the potential protective effect of pretreatment with combinations of MET and RAPA in a 1-methyl-4-phenylpyridinium ion (MPP⁺)-treated SH-SY5Y neuronal cell model of PD. The results showed that MET and RAPA combinations lowered cell viability after exposure to MPP⁺. Increased LC3-II levels by MPP⁺ were not altered by MET and RAPA pretreatment. In normal neuronal cells, MET and RAPA pretreatment inhibited the phosphorylation of both Akt and S6K1, and the phosphorylation remained suppressed after MPP⁺ exposure. These findings suggest that when cells were exposed to MPP⁺, suppressed phosphorylation of both Akt and S6K1 by the MET and RAPA combination may lead to an inappropriate autophagic response, resulting in increased cell death.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"3830861"},"PeriodicalIF":2.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9870674/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10676638","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Interaction of Phospholipid, Cholesterol, Beta-Carotene, and Vitamin C Molecules in Liposome-Based Drug Delivery Systems: An <i>In Silico</i> Study.","authors":"D Hudiyanti,&nbsp;V N R Putri,&nbsp;Y Hikmahwati,&nbsp;S M Christa,&nbsp;P Siahaan,&nbsp;D S B Anugrah","doi":"10.1155/2023/4301310","DOIUrl":"https://doi.org/10.1155/2023/4301310","url":null,"abstract":"<p><p>This paper investigates the interaction within a liposome-based drug delivery system <i>in silico</i>. Results confirmed that phospholipids, cholesterol, beta-carotene, and vitamin C in the liposome structures interact noncovalently. The formation of noncovalent interactions indicates that the liposomal structures from phospholipid molecules will not result in chemical changes to the drug or any molecules encapsulated within. Noncovalent interactions formed include (i) moderate-strength hydrogen bonds with interaction energies ranging from -73.6434 kJ·mol^-1 to -45.6734 kJ·mol^-1 and bond lengths ranging from 1.731 Å to 1.827 Å and (ii) van der Waals interactions (induced dipole-induced dipole and induced dipole-dipole interactions) with interaction energies ranging from -4.4735 kJ·mol^-1 to -1.5840 kJ·mol^-1 and bond lengths ranging from 3.192 Å to 3.742 Å. The studies for several phospholipids with short hydrocarbon chains show that changes in chain length have almost no effect on interaction energy, bond length, and partial atomic charge.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"4301310"},"PeriodicalIF":2.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9833918/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10540506","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"In Silico Models for Anti-COVID-19 Drug Discovery: A Systematic Review.","authors":"Okello Harrison Onyango","doi":"10.1155/2023/4562974","DOIUrl":"https://doi.org/10.1155/2023/4562974","url":null,"abstract":"<p><p>The coronavirus disease 2019 (COVID-19) is a severe worldwide pandemic. Due to the emergence of various SARS-CoV-2 variants and the presence of only one Food and Drug Administration (FDA) approved anti-COVID-19 drug (remdesivir), the disease remains a mindboggling global public health problem. Developing anti-COVID-19 drug candidates that are effective against SARS-CoV-2 and its various variants is a pressing need that should be satisfied. This systematic review assesses the existing literature that used in silico models during the discovery procedure of anti-COVID-19 drugs. Cochrane Library, Science Direct, Google Scholar, and PubMed were used to conduct a literature search to find the relevant articles utilizing the search terms \"In silico model,\" \"COVID-19,\" \"Anti-COVID-19 drug,\" \"Drug discovery,\" \"Computational drug designing,\" and \"Computer-aided drug design.\" Studies published in English between 2019 and December 2022 were included in the systematic review. From the 1120 articles retrieved from the databases and reference lists, only 33 were included in the review after the removal of duplicates, screening, and eligibility assessment. Most of the articles are studies that use SARS-CoV-2 proteins as drug targets. Both ligand-based and structure-based methods were utilized to obtain lead anti-COVID-19 drug candidates. Sixteen articles also assessed absorption, distribution, metabolism, excretion, toxicity (ADMET), and drug-likeness properties. Confirmation of the inhibitory ability of the candidate leads by <i>in vivo</i> or <i>in vitro</i> assays was reported in only five articles. Virtual screening, molecular docking (MD), and molecular dynamics simulation (MDS) emerged as the most commonly utilized in silico models for anti-COVID-19 drug discovery.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"4562974"},"PeriodicalIF":2.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10287514/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9749759","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Changes in Protease-Activated Receptor and Trypsin-1 Expression Are Involved in the Therapeutic Effect of Mg²⁺ Supplementation in Type 2 Diabetes-Induced Gastric Injury in Male Adult Rats.","authors":"Nasrin Mehranfard,&nbsp;Hossein Rezazadeh,&nbsp;Nepton Soltani,&nbsp;Azadesadat Hosseini Dastgerdi,&nbsp;Mahtab Ghanbari Rad,&nbsp;Maedeh Ghasemi","doi":"10.1155/2023/5703718","DOIUrl":"https://doi.org/10.1155/2023/5703718","url":null,"abstract":"<p><strong>Purpose: </strong>Gastric inflammation is common and usually severe in patients with type 2 diabetes mellitus (T2DM). Evidence suggests protease-activated receptors (PARs) are a link between inflammation and gastrointestinal dysfunction. Given that magnesium (Mg²⁺) deficiency is a highly prevalent condition in T2DM patients, we assessed the therapeutic role of Mg²⁺ on the factors involved in gastric inflammation in T2DM.</p><p><strong>Methods: </strong>A rat model of T2DM gastropathy was established using a long-term high-fat diet + a low dose of streptozocin. Twenty-four rats were divided into control, T2DM , T2DM + insulin (positive control), and T2DM + Mg²⁺ groups. At the end of 2-month therapies, changes in the expression of gastric trypsin-1, PAR1, PAR2, PAR3, PI3K/Akt, and COX-2 proteins were measured by western blot. Hematoxylin and eosin and Masson's trichrome staining were used to detect gastric mucosal injury and fibrosis.</p><p><strong>Results: </strong>The expression of trypsin-1, PAR1, PAR2, PAR3, and COX-2 increased in diabetes, and Mg²⁺/insulin treatment strongly decreased their expression. The PI3K/p-Akt significantly decreased in T2DM, and treatment with Mg²⁺/insulin improved PI3K in T2DM rats. Staining of the gastric antrum tissue of the insulin/Mg²⁺-treated T2DM rats showed a significantly minimal mucosal and fibrotic injury compared with those of rats from the T2DM group.</p><p><strong>Conclusion: </strong>Mg²⁺ supplement, comparable to insulin, via decreasing PARs expression, mitigating COX-2 activity, and decreasing collagen deposition could exert a potent gastroprotective effect against inflammation, ulcer, and fibrotic development in T2DM patients.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"5703718"},"PeriodicalIF":2.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10205415/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9896929","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Effects of Walnut Bark Extract on the Human Platelet Aggregation, Adhesion, and Plasmatic Coagulation In Vitro.","authors":"Asmae Amirou,&nbsp;El Mahdi Razzok,&nbsp;Abdelkhaleq Legssyer,&nbsp;Abderrahim Ziyyat,&nbsp;Mohammed Aziz,&nbsp;Mohamed Bnouham,&nbsp;Younes Zaid,&nbsp;Mohamed Berrabah,&nbsp;Hassane Mekhfi","doi":"10.1155/2023/5644803","DOIUrl":"https://doi.org/10.1155/2023/5644803","url":null,"abstract":"<p><p>Thrombosis is the formation of a clot within a blood vessel. Antithrombotic drugs are used for treating thrombosis, which can be the cause of hemorrhage. Currently, there is a need to discover novel antithrombotic drugs. Walnut is widely used to treat a wide range of health complaints. In this study, walnut bark extract was tested in hemostasis parameters: platelets adhesion, aggregation, and plasmatic coagulation in human blood. The crude aqueous extract of walnut bark was prepared by infusion and tested <i>in vitro</i> on hemostasis. Through blood collection from healthy volunteer donors, we studied different parameters of the primary hemostasis: platelet adhesion on the collagen-coated surface under flow, ADP, collagen, thrombin, and arachidonic acid-induced platelet aggregation, and of the secondary hemostasis by measuring prothrombin time (PT) and activated partial thromboplastin (APTT) parameters. All experiments are realized in the absence and presence of the extract and repeated at least twice. The obtained data showed that the extract (1 and 2 mg/mL) significantly (<i>p</i> < 0.001) reduced the activated platelet adhesion on the collagen-coated surface. In the same way, the effect of the extract on platelet aggregation seems to depend on its concentration and on the nature of the agonist. The strongest inhibition of aggregation was observed in the case of collagen at 1 mg/mL, while there was no observed effect on arachidonic acid-induced aggregation. Moreover, the extract (1 mg/mL) affects the extrinsic, intrinsic, and common pathways of the human blood coagulation cascade by extending significantly (<i>p</i> < 0.001), both PT and APTT times. This study provides evidence that walnut bark extract, by its antiadhesive, antiaggregant, and anticoagulant activities, could be considered as a serious source of biological compounds for the prevention and treatment of thrombosis.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"5644803"},"PeriodicalIF":2.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9831691/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10532574","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Formulation of New Chewable Oral Dosage Forms of Meclizine and Pyridoxine Hydrochloride.","authors":"Wafa M Al-Madhagi,&nbsp;Arwa Alshargabi,&nbsp;Abdulkarim K Y Alzomor,&nbsp;Olla Sharhan","doi":"10.1155/2023/5512379","DOIUrl":"https://doi.org/10.1155/2023/5512379","url":null,"abstract":"<p><p>Nausea and vomiting are symptoms associated with a lot of diseases and oral tablets may be unprofitable for patients especially those suffering from nausea and vomiting. Therefore, this study aimed to formulate a new meclizine and pyridoxine combination formula for chewable tablets and provide rapid drug absorption and decrease motion sickness. The new chewable formulation has been prepared to provide fast action, is more acceptable, and could be used for all age categories. Seven trials haves been carried out to prepare to find the suitable one where formula 7 of the chewable gum preparation exhibited good taste and hardness, while the gelatin formulation give an accepted formula after four trials with better taste and good acceptance. The prepared formulations give a dissolution profile of meclizine (95.53-102.8%) and pyridoxine (99.25 ± 115%) and assay (98 + 0.05-99.3 ± 0.8%) for meclizine and (97 ± 0.9-100.0 ± 0.08%) for the pyridoxine in three prepared formulations of chewable tablets. Followed by the evaluation, the formulation and testing them on human volunteers are carried out to confirm their effect to ensure acceptance and fast actions. The finding is promising for preparing a new route of administration of meclizine and pyridoxine combination to be used in the market.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"5512379"},"PeriodicalIF":2.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10404153/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10006869","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Chemical Profiles and <i>In Vitro</i> Cholinesterase Inhibitory Activities of the Flower Extracts of <i>Cassia spectabilis</i>.","authors":"Suciati,&nbsp;Erlinda R Laili,&nbsp;Wiwied Ekasari,&nbsp;Kuatman,&nbsp;Nitra Nuengchamnong,&nbsp;Nungruthai Suphrom","doi":"10.1155/2023/6066601","DOIUrl":"https://doi.org/10.1155/2023/6066601","url":null,"abstract":"<p><strong>Background: </strong><i>Cassia spectabilis</i> is a flowering plant containing various metabolites that provide potential for pharmacological activities. The current study aimed to investigate the ethanolic and water extracts of <i>C. spectabilis</i> as cholinesterase inhibitor as one of the target treatments for Alzheimer's disease. The chemical composition of the extracts was also studied to determine which components are responsible for the bioactivity.</p><p><strong>Methods: </strong>The cholinesterase inhibitory activity assay was carried out by the modified Ellman's method against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). LC-MS/MS analysis was carried out to investigate the chemical profiles of the extracts, followed by a molecular networking study by GNPS.</p><p><strong>Results: </strong>Both extracts showed inhibition against AChE and BChE in a dose-dependent manner, with the higher potency exhibited by the ethanolic extract with IC50 values of 7.88 and 3.78 <i>μ</i>g/mL. The chemical analysis and molecular networking study of the flower extracts revealed similarity between the ethanolic and water extracts. Piperidine alkaloids were identified in both extracts, while the sphingolipid compounds were found in the ethanolic extract.</p><p><strong>Conclusion: </strong>The water and ethanolic extracts of <i>C. spectabilis</i> flowers displayed potency for Alzheimer's disease treatment. The presence of piperidine alkaloids in the extract may be responsible for the cholinesterase inhibitory activity. The higher potency of the ethanolic extract compared to the water extract is possibly due to the higher amount of piperidine alkaloids in the ethanolic extract. Further study is needed to quantify the concentration of alkaloids in the extracts.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"6066601"},"PeriodicalIF":2.8,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9991480/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9437749","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}