Phytomedicine Plus最新文献

{"title":"In Silico Analysis of novel Phytocompounds targetting Dipeptidyl peptidase 4 Enzyme: A New Link between Prediabetes and its cardio-metabolic complications","authors":"Ipseeta Ray Mohanty ,&nbsp;C. Selvaa Kumar ,&nbsp;Ujwala Maheswari","doi":"10.1016/j.phyplu.2024.100665","DOIUrl":"10.1016/j.phyplu.2024.100665","url":null,"abstract":"<div><h3>Background</h3><div>DPP-4 inhibitors, are widely used clinically for treatment of Diabetes. Increase in circulating DPP4 levels have been well demonstrated in patients with Type 2 Diabetes mellitus. The present study assessed the contribution of DPP-4 axis to the pathophysiology of Prediabetes and its cardiometabolic complications. In addition, in silico analysis of phytocompounds that target DPP 4 enzyme was undertaken to identify novel Phytocompounds with therapeutic potential in Prediabetes.</div></div><div><h3>Methodology</h3><div>A novel experimental model of Prediabetes coexisting with hypertension and dyslipidemia was developed in experimental rats to elucidate the pathophysiological role of DPP-4 in Prediabetes and its resultant cardio-metabolic sequale. In the Prediabetic rats, DPP-4 levels, lipid profile, blood pressure readings, fasting blood sugar values, insulin resistance, beta cell function were measured and compared to Normal Control group. In addition, the DPP-4 Inhibitory activity of Phytocompounds (Arjunetin, Guggulsterone) was studied by molecular docking studies including Root Mean Square Deviation (RMSD), Root Mean Square Fluctuation (RMSF), DPP 4 binding affinity and Protein-ligand simulation between the DPP4 and the Phytocompounds was performed. Results were compared to Vildagliptin, the synthetic DPP-4 inhibitor and metformin (Glucophage), the standard antidiabetic drug used in clinical settings.</div></div><div><h3>Results</h3><div>A statistically significant increase (<em>p</em> &lt; 0.001) in DPP-4 levels along with a decline in bea cell function with increase in Insulin resistance was observed in Prediabetic rats. A positive correlation (<em>p</em> &lt; 0.001) between serum DPP-4 with HbA1c, lipids, and systolic blood pressure was found. The novel model of Prediabetes co-existing with hypertension and dyslipidemia was successfully developed and validated. The silico active site interaction data from simulation studies demonstrated that Arjunetin and Guggulsterone shows effective and stable binding with DPP-4. Arjunetin maintains its contact with Glu205, Glu206, and Asn710 and by interacting with Val207 and His740, it effectively occupies the flanking residues of the active site area. Based on their protein-ligand contact report, Vildagliptin maintains its connection through Tyr547 and during simulation, Guggulsterone interacts with Ser630.</div></div><div><h3>Conclusion</h3><div>The current study offers experimental evidence of DPP-4′s causal role in the development of cardio-metabolic consequences (dyslipidemia and hypertension) of Prediabetes. Arjunetin and Guggulsterone are two Phytocompounds whose potential as promising DPP-4 inhibitors has been further documented using in silico molecular docking studies.</div></div>","PeriodicalId":34599,"journal":{"name":"Phytomedicine Plus","volume":"4 4","pages":"Article 100665"},"PeriodicalIF":0.0,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142663848","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":"Assessing the antiproliferative properties of various teas against the DU-145 prostate cancer cell line: A combined in vitro and in silico investigation","authors":"Joseph Muriuki ,&nbsp;Grace Uwanyagasani ,&nbsp;Edward Maina ,&nbsp;Beatrice Irungu ,&nbsp;Samuel Khamadi ,&nbsp;Raphael Lwembe ,&nbsp;Asma Adan ,&nbsp;Shadrack Barmasai ,&nbsp;Joseph Ndacyayisenga","doi":"10.1016/j.phyplu.2024.100667","DOIUrl":"10.1016/j.phyplu.2024.100667","url":null,"abstract":"<div><h3>Background</h3><div>Phytotherapy emerges as a promising solution to the challenges posed by cancer treatment. Black, green, and purple teas, renowned for their antioxidant properties, exhibit efficacy against various cancers, including prostate cancer.</div></div><div><h3>Study Design</h3><div>This was an experimental study conducted from the Kenya Medical Research Institute (KEMRI).</div></div><div><h3>Aim of the Study</h3><div>the present study aimed to evaluate the Cytotoxic effect of black, green and purple teas against prostate cancer cell line DU-145 and in silico prediction of Tea catechins interaction with prostate cancer proteins such as 3D-crystal structures of Androgen-receptor(5T8E) and Human p38 MAPK(1KV2).</div></div><div><h3>Methods</h3><div>The study started by quantifying tea catechins (Epigallocatechin gallate (EGCG), Epigallocatechin EGC, Epicatechin gallate (ECG) and Epicatechin (EC) with high-liquid chromatography (HPLC), cytotoxicity analysis of black, green and purple tea crude extracts against DU-145 cell line at 24hr and 48 hrs by Resazurin assay and molecular docking was performed with Autodock Vina 1.1.2 software.</div></div><div><h3>Results</h3><div>EGCG appeared the most predominant catechin with 552.2 ± 10.61 (mg g^-1 DW) while EC was the lowest detected with 118.08 ± 9.45 (mg g^-1 DW). Purple tea extract exhibited high antiproliferative activity with IC50 of 98.69±1.99 µg/ml at 24hr and 91.21±6.91 µg/ml at 48hr, green tea followed with 121 ± 5.97µg/ml at 24hr and 107.1 ± 2.03 µg/ml at 48hr IC50; black tea was the least effective tea at both 24hr and 48hr with IC50 of 290.8 ± 2.46µg/ml and 237.8 ± 5.59µg/ml respectively. Prediction of catechin target genes and Prostate cancer (Pca)-related genes discovered 121 catechin target genes and 34,926 Pca-related genes. EGC exhibited high binding interaction to 5T8E with the lowest affinity of -9.1Kcal/mol followed by EGCG at -8.4 (Kcal/mol then EC with -8.2 (Kcal/mol) and EGC at -8.1 (Kcal/mol). Catechins interaction with 1KV2 was in the following order EGCG (-9.4 Kcal/mol) ˃ECG (-8.2 Kcal/mol) ˃EC (-8.2 Kcal/mol) ˃EGC (-8.1 Kcal/mol).</div></div><div><h3>Conclusion</h3><div>In vitro experiment detected a very significant antiproliferative activity of black, green and purple tea crude extracts against the DU-145 cell line; furthermore, <em>in silico</em> analysis revealed a strong binding interaction with proteins associated with prostate cancer, indicating that black, green, and purple teas, along with catechins, hold promise as potential herbal remedies for combating prostate cancer.</div></div>","PeriodicalId":34599,"journal":{"name":"Phytomedicine Plus","volume":"4 4","pages":"Article 100667"},"PeriodicalIF":0.0,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142663849","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":"Anti-inflammatory, immuno-modulatory, and anti-proliferative effects of 5-mer Oligogalacturonides (OG DP5) from citrus pectin on different types of human cells. Perspectives for treatment of dermal diseases such as atopic dermatitis and psoriasis","authors":"Lény Teyssier ,&nbsp;Lamotte Olivier ,&nbsp;Bonnin Estelle ,&nbsp;Crépeau Marie-Jeanne ,&nbsp;Cussac Didier ,&nbsp;Jeandroz Sylvain ,&nbsp;Wendehenne David ,&nbsp;Pelloux Jérôme ,&nbsp;Jean-Louis Connat","doi":"10.1016/j.phyplu.2024.100666","DOIUrl":"10.1016/j.phyplu.2024.100666","url":null,"abstract":"<div><h3>Background</h3><div>Oligogalacturonides (OG) are natural plant cell wall pectin-derived products with different degrees of polymerisation (DP) and methylation (M) (see <span><span>Yu et al. 2022</span></span>). Their effects as stimulators of plant defence are well documented and they are also known for their potent effects on human health.</div></div><div><h3>Purpose</h3><div>Here, we investigated the anti-inflammatory effects of OG extracted from Citrus on different types of human cells and cell systems representative of several pathologies.</div></div><div><h3>Study design</h3><div>Different concentrations of 5-mer OG (DP5) with different methylation degrees (M: 0, 5, 30 and 70) were tested on cultured human peripheral blood mononuclear cells (PBMC) to see if there were able to decrease LPS-induced IL-1β release. Then, different human cell combination stimulated by specific agonists representative of several pathologies were used to test the effect of the most active OG DP5M0 (0 methylation).</div></div><div><h3>Methods</h3><div>IL-1β was monitored in the PBMC culture medium with ELISA and effects on bio-markers typical of pathologies were studied using the BioMAP Diversity PLUS® method (Eurofins, France).</div></div><div><h3>Results</h3><div>DP5M0 dose-dependently reduced LPS-induced IL-1β release by cultured human peripheral blood mononuclear cells (PBMC). This was not observed for DP5M30 or DP5M70. DP5M0 was also more efficient than prednisolone when tested on 12 different human cell systems representative of known pathologies (BioMAP systems). The T BioMAP system, which consists in an equal combination of B cells and PBMC, shows the best response sensitivity to DP5M0. This latter induces a dose-dependent decrease of the biomarkers of inflammation and of those of immune responses (IL-6, IL-8, IL-2, IL-17A, IL-17F and TNF-α).</div></div><div><h3>Conclusion</h3><div>In view that all these cytokines are involved in keratinocytes proliferation and differentiation, this model system fits with a possible beneficial effect of DP5M0 on atopic dermatitis and psoriasis. DP5M0 also showed anti-proliferative properties in 5 different cell systems. The comparison of the BioMAP profiles of DP5M0 and anti-inflammatory products prednisolone and diclofenac indicates that their modes of action are different. These data argue for a possible use of DP5M0 for treatments of psoriasis diseases as alternative strategy to other developed medicines when the patients do not tolerate them.</div></div>","PeriodicalId":34599,"journal":{"name":"Phytomedicine Plus","volume":"4 4","pages":"Article 100666"},"PeriodicalIF":0.0,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142663850","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 antioxidant and anti-inflammatory properties, bioactive compound profiling, and molecular mechanisms of a multicomponent Thai herbal formulation","authors":"Nalinee Pradubyat ,&nbsp;Thaniya Wunnakup ,&nbsp;Rachanida Praparatana ,&nbsp;Supakit Wongwiwatthananukit ,&nbsp;Suchada Jongrungruangchok ,&nbsp;Thanapat Songsak ,&nbsp;Fameera Madaka ,&nbsp;Teeratad Sudsai","doi":"10.1016/j.phyplu.2024.100662","DOIUrl":"10.1016/j.phyplu.2024.100662","url":null,"abstract":"<div><h3>Background</h3><div>Medicinal plants have long been used as dietary supplements to reduce the risk of chronic diseases, inflammation, cancer, and metabolic syndromes. Traditional remedies possess therapeutic properties, making them promising candidates for further investigation and potential pharmaceutical development.</div></div><div><h3>Aim of the study</h3><div>This study aimed to evaluate the efficacy of Belog Plus (BP), a polyherbal product containing five Thai medicinal plants: <em>Citrus aurantifolia, Cannabis sativa, Tiliacora triandra, Alpinia galanga</em>, and <em>Piper nigrum</em>, combined with safflower seed oil. This study focused on quantifying the total phenolic content (TPC) and total flavonoid content (TFC), and identifying key herbal biomarkers that contribute to its therapeutic properties. In addition to assessing the antioxidant and anti-inflammatory potential of the plant extracts, the study explored the molecular mechanisms underlying their anti-inflammatory activity, offering a comprehensive understanding of BP's efficacy.</div></div><div><h3>Methods</h3><div>The ethanolic extract of BP and its components were assessed for antioxidant potential using DPPH, FRAP, and H₂O₂ induced oxidative stress. The anti-inflammatory activity was evaluated using the Griess reaction assay, and the mechanisms were explored through mRNA and protein expression analysis. The TPC and TFC were measured using the Folin–Ciocalteu (F–C) assay and the aluminium chloride colorimetric assay, respectively, while herbal biomarkers were identified using LC-MS/MS analysis.</div></div><div><h3>Results</h3><div>The results revealed that the ethanolic extract of BP (6.25–100 µg/ml) exhibited a potent anti-inflammatory effect through nitric oxide inhibition (IC₅₀ 24.4 μg/ml) and significantly reducing the expression of inflammatory genes iNOS, COX-2, IL-6, and TNF-α. Additionally, it significantly reduced the expression of inflammatory proteins iNOS and COX-2 at concentrations of 6.25–25 µg/ml. Among the individual components, <em>C. aurantifolia, A. galanga</em>, and <em>P. nigrum</em> showed potent anti-inflammatory effects with IC₅₀ values of 35.7, 6.5, and 23.3 μg/ml, respectively. The TPC and TFC results demonstrated significant levels of phenolic (80.6 µg GAE/mg) and flavonoid (47.4 µg catechin/mg) compounds. Additionally, the LC-MS/MS analysis identified a variety of bioactive compounds known for their anti-inflammatory properties.</div></div><div><h3>Conclusion</h3><div>These findings support BP's potential use as a dietary supplement to mitigate the risk of chronic inflammatory diseases, with its ethanolic extract containing bioactive phenolic and flavonoid compounds that significantly suppress iNOS and COX-2 protein expressions.</div></div>","PeriodicalId":34599,"journal":{"name":"Phytomedicine Plus","volume":"4 4","pages":"Article 100662"},"PeriodicalIF":0.0,"publicationDate":"2024-10-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142534297","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":"Protective effect of essential oil of Foeniculum vulgare Mill. against bleomycin-induced pulmonary fibrosis and oxidative stress in rat","authors":"Marwa Khammassi ,&nbsp;Anouar Abidi ,&nbsp;Naoures Ochi ,&nbsp;Aida Ayadi ,&nbsp;Yassine Mabrouk ,&nbsp;Ismail Amri ,&nbsp;Vincenzo De Feo ,&nbsp;Hichem Sebai ,&nbsp;Flavio Polito","doi":"10.1016/j.phyplu.2024.100660","DOIUrl":"10.1016/j.phyplu.2024.100660","url":null,"abstract":"<div><h3>Background</h3><div>Wild fennel (<em>Foeniculum vulgare</em> Mill.) is a very common plant used in traditional medicine to treat several diseases. In recent years, scientific research proved its biological properties. However, the protective effect of fennel against bleomycin-induced pulmonary fibrosis (BLM-IPF) is not yet study.</div></div><div><h3>Purpose</h3><div>Fennel essential oil (FEO) composition was characterized and its protective effect was assessed.</div></div><div><h3>Methods</h3><div>GC–MS was employed to determine the chemical composition of fennel essential oil. The antioxidant activity was evaluated using TAC, DPPH, RAP and ABTS assays. After inducing fibrosis by bleomycin, several biological assays were used to evaluate the protective effect [proteins content, malondialdehyde MD, thiol group, superoxide dismutase (SOD) and catalase (CAT)].</div></div><div><h3>Results</h3><div>FEO was rich in estragole (77.55 %), fenchone (9.23 %), <del>and</del> limonene (9.23 %), <del>and</del> phenolic compounds and showed a significant antioxidant potential. The effects on BLM-IPF were revealed by disruption and alteration of oxidative stress biomarkers in lung, liver and kidney. Treatment of rats with FEO improved abnormal fluctuations in protein and thiol levels, decreased oxidative stress in terms of MDA and also restored the response of the antioxidant system, measured in terms of SOD and CAT, in lung, liver and kidney. The biological activity was recorded in a dose response manner. The potential of FEO in limiting the progress of the histopathologic effects of BLM-IPF was confirmed by microscopic histological observations, with a reduction of the fibrosis score and the inflammatory index in the FEO treated lung tissue.</div></div><div><h3>Conclusion</h3><div>These results, proved that FEO could attenuate BLM-induced PF, thus suggesting that the latter could serve as a potential therapeutic approach for PF.</div></div>","PeriodicalId":34599,"journal":{"name":"Phytomedicine Plus","volume":"4 4","pages":"Article 100660"},"PeriodicalIF":0.0,"publicationDate":"2024-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142534293","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":"Pharmacognostic standardization and phytochemical evaluation of Ficus rumphii blume leaves in Thailand","authors":"Thanaphorn Limpabandhu ,&nbsp;Maneewan Suwatronnakorn ,&nbsp;Ansella Amanda Epifani Widoyanti ,&nbsp;Somchai Issaravanich ,&nbsp;Onuma Zongrum ,&nbsp;Anchalee Prasansuklab","doi":"10.1016/j.phyplu.2024.100661","DOIUrl":"10.1016/j.phyplu.2024.100661","url":null,"abstract":"<div><h3>Background</h3><div><em>Ficus rumphii</em> Blume has long been used in ethnomedicinal practices and is regarded as one of the medicinal plants in Thai traditional herbal formulas for diabetes treatment. At present, published data on pharmacognostic study of this plant for its identity, quality, and purity is still limited.</div></div><div><h3>Objective</h3><div>This study aimed to establish the pharmacognostic standardization parameters of <em>Ficus rumphii</em> leaves in Thailand.</div></div><div><h3>Methods</h3><div>The pharmacognostic study of <em>F. rumphii</em> leaves collected from 12 different sources throughout Thailand was conducted according to the methods described in WHO guidelines including macroscopic, microscopic, physicochemical parameters, phytochemical screening, and TLC fingerprint.</div></div><div><h3>Results</h3><div>Macroscopic and microscopic characteristics of <em>F. rumphii</em> leaves were reported in this study. Physicochemical parameters showed the value of loss on drying (6.87 ± 0.79 %), total ash (16.28 ± 5.76 %), acid insoluble ash (7.54 ± 4.53 %), water content (9.58 ± 2.49 %), water extractive matters (4.71 ± 1.75 %) and ethanol extractive matters (1.30 ± 0.52 %). Preliminary phytochemical screening of hexane, ethanol, and aqueous extracted revealed the presence of phenolic, flavonoid, diterpene, triterpene, steroid, saponin, and cardiac glycoside which were confirmed by TLC fingerprint profiles of ethanolic extract of this plant.</div></div><div><h3>Conclusion</h3><div>This study is the first report on the pharmacognostic specification of <em>F. rumphii</em> leaves in Thailand, which could be used as a reference for quality control and the species identification of this plant material.</div></div>","PeriodicalId":34599,"journal":{"name":"Phytomedicine Plus","volume":"4 4","pages":"Article 100661"},"PeriodicalIF":0.0,"publicationDate":"2024-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142534295","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":"Development of thermosensitive hydrogel mouthwash loaded with Zingiber zerumbet extract for enhanced oral thrush treatment","authors":"Kampanart Huanbutta ,&nbsp;Pornsak Sriamornsak ,&nbsp;Thachtham Chatchaipan ,&nbsp;Kornrawee Tuntipimonpun ,&nbsp;Chatchaya Mongkhon ,&nbsp;Napapat Rattanachitthawat ,&nbsp;Anusorn Thampithak ,&nbsp;Tanikan Sangnim","doi":"10.1016/j.phyplu.2024.100655","DOIUrl":"10.1016/j.phyplu.2024.100655","url":null,"abstract":"<div><h3>Background</h3><div>Oral thrush, caused by <em>Candida albicans,</em> is currently treated under guidelines by using topical antifungal pharmaceutical formulations such as lozenges and liquid gargles. Using these drugs may cause irritation and adverse reactions. Moreover, there is a short exposure time to reach the lesion, which may result in low effectiveness of the treatment. Therefore, the research group aimed to develop mouthwash solutions that can form gel at oral temperature containing <em>Zingiber zerumbet</em> rhizome extracts, which work as an active substance inhibiting fungi.</div></div><div><h3>Methods</h3><div>The development process began with the extraction of substances from <em>Zingiber zerumbet</em> rhizome using hexane and the analysis of the active substance by HPLC. Antifungal and anti-inflammatory activities of the extracts were evaluated. Hydrogel mouthwash was prepared by varying the type and concentration of polymer, solvent, and mucoadhesive agent. The optimized formulation was then evaluated for its properties.</div></div><div><h3>Results</h3><div><em>Zingiber zerumbet</em> rhizome extracts, containing 16.29±0.39 % zerumbone, demonstrated both antifungal and anti-inflammatory activities against <em>Candida albicans</em>. The extract also had anti-inflammatory activity when tested by the proteinase inhibitory test, with a percentage inhibition of 86.15±10.96 %. Two thermosensitive hydrogels, poloxamer P407 and P188, were applied and compared as gel-forming agents. It was found that the optimized formulation is composed of 15 % (w/w) poloxamer P407, 0.05 % (w/w) carbopol as a mucoadhesive agent, and 5 % (v/v) ethanol. Transition time and transition temperature of the optimized thermosensitive hydrogel formula were 27.76±1.25 s and 36±1.00 °C, respectively. The viscosity at shear rate 1 S^-1 and 25 °C of the optimized formulation was 0.13±0.06 Pa.s, which is suitable for pouring out of the bottle and gargling.</div></div><div><h3>Conclusion</h3><div>This study demonstrates a novel approach to developing thermosensitive hydrogel mouthwash formulations, leveraging <em>Zingiber zerumbet</em> rhizome extracts for enhanced therapeutic efficacy against oral candidiasis. These formulations offer prolonged contact time with affected areas, potentially improving treatment outcome.</div></div>","PeriodicalId":34599,"journal":{"name":"Phytomedicine Plus","volume":"4 4","pages":"Article 100655"},"PeriodicalIF":0.0,"publicationDate":"2024-10-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142433265","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 vitro leishmanicidal activity of Hancornia speciosa latex against Leishmania (Leishmania) amazonensis","authors":"Julyanna Oliveira Castro ,&nbsp;Danielle de Sousa Lopes ,&nbsp;Saulo Luís Capim ,&nbsp;Paola Miranda de Souza ,&nbsp;Thamires Queiroz-Oliveira ,&nbsp;Victor Soares Cavalcante-Costa ,&nbsp;Thiago Castro-Gomes ,&nbsp;Graziela Dos Santos Paulino ,&nbsp;Maria Roméria da Silva ,&nbsp;Tiago Antonio de Oliveira Mendes ,&nbsp;Carlos Priminho Pirovani ,&nbsp;Luiz Alberto Mattos Silva ,&nbsp;Izaltina Silva Jardim Cavalli ,&nbsp;Juliana de Oliveira Cruz ,&nbsp;Jane Lima dos Santos","doi":"10.1016/j.phyplu.2024.100658","DOIUrl":"10.1016/j.phyplu.2024.100658","url":null,"abstract":"<div><h3>Background</h3><div>Leishmaniasis is a neglected tropical disease whose available treatment has limitations. <em>Hancornia speciosa</em> Gomes, a tree native to Brazil, has been studied for its medicinal properties, including antimicrobial and healing properties. However, its effect on parasites of the <em>Leishmania</em> genus still needs to be elucidated.</div></div><div><h3>Purpose</h3><div>To evaluate the leishmanicidal activity for potential therapeutic use of <em>H. speciosa</em> latex and its fractions on <em>Leishmania (Leishmania) amazonensis</em> promastigotes and amastigotes, as well as to analyze its cytotoxic effects on RAW264.7 cells and murine peritoneal macrophages.</div></div><div><h3>Methods</h3><div>The anti-promastigote activity of latex and its fractions was evaluated by cell viability assays via MTT in <em>L. (L.) amazonensis</em> and monitoring the parasite's growth kinetics by counting under light microscopy. To evaluate anti-amastigote activity, RAW264.7 cells and murine peritoneal macrophages infected with amastigotes were analyzed using microscopy, immunofluorescence, and flow cytometry assays. The cytotoxicity of latex and its fractions was evaluated in these cells via MTT assay.</div></div><div><h3>Results</h3><div>The <em>H. speciosa</em> latex and its fractions showed anti-promastigote activities in <em>L. (L.) amazonensis</em>, reducing its proliferation and viability and altering its morphology. These did not interfere with the viability of RAW264.7 cells and peritoneal macrophages. Crude latex and <em>F</em> &lt; 10 kDa at 5 % reduced the infection of intracellular amastigotes in peritoneal macrophages to 32 % and 18 % after 24 h of treatment, respectively. Under the same conditions, the <em>F</em> &gt; 10 kDa fraction showed 82 % of infected cells. The evaluation of the latex composition showed that the <em>F</em> &gt; 10 kDa fraction has the highest concentration of carbohydrates, followed by phenolic compounds and proteins. In contrast, the <em>F</em> &lt; 10k Da fraction presented fewer phenolic compounds and carbohydrates.</div></div><div><h3>Conclusions</h3><div>These results indicate that <em>H. speciosa</em> crude latex and <em>F</em> &lt; 10 kDa have intense leishmanicidal activity against <em>L. (L.) amazonensis</em> promastigotes and amastigotes internalized by macrophages. Additionally, the lack of cytotoxicity indicates that <em>H. speciosa</em> latex is a strong candidate for new alternative treatments for leishmaniasis.</div></div>","PeriodicalId":34599,"journal":{"name":"Phytomedicine Plus","volume":"4 4","pages":"Article 100658"},"PeriodicalIF":0.0,"publicationDate":"2024-10-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142534292","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":"Adrenal hypertrophy in rats caused by 90-day force-feeding concomitant with the non-toxic effects of Antrodia cinnamomea","authors":"Chi-Tan Hu ,&nbsp;Guan-Jhong Huang ,&nbsp;Jayson John Taub ,&nbsp;Ching-Feng Weng ,&nbsp;David Yul ,&nbsp;Huei Long","doi":"10.1016/j.phyplu.2024.100659","DOIUrl":"10.1016/j.phyplu.2024.100659","url":null,"abstract":"<div><h3>Background</h3><div><em>Antrodia cinnamomea (A. cinnamomea)</em>, a medicinal fungus native to Taiwan, has been used for decades by folk medicine practitioners to treat liver damage, cancer, and inflammation-related afflictions in Taiwan. The observation of adrenal hypertrophy in rats over a 90-day feeding wild <em>A. cinnamomea</em> test has been reported, however no investigation or conclusive evidence is further provided yet.</div></div><div><h3>Purpose</h3><div>This study aimed to explore the cause of adrenal hypertrophy in rats fed <em>A. cinnamomea</em> (in a 90-day study) followed by Harvey's strategy, considering potential effects on the routinely evaluated stress-sensitive organ systems (adrenal and thymus), without directly assessing the HPA axis function.</div></div><div><h3>Study Design</h3><div>A 90-day study using Sprague-Dawley (SD) rats was conducted in accordance with the \"Regulations on Food Management and Labelling of <em>A. cinnamomea</em>\" by Taiwan FDA, which adhere to the OECD guidelines for the testing of chemicals (Test No 408) specification.</div></div><div><h3>Methods</h3><div>The rats were oral gavaged with raw dish-cultured <em>A. cinnamomea</em> (RDAC) at a dosage of 250 mg kg^-1/day for 13 weeks. The evaluation methods included clinical examinations, body weights, food consumption, haematology, coagulation, clinical biochemistry, gross visual observations and macroscopic examinations, organ weights, and histopathology.</div></div><div><h3>Results</h3><div>No adverse effects from RDAC were found, establishing a no-observed-adverse-effect level of 250 mg kg^-1/day in rats over a 3-month period. Adrenocortical hypertrophy was observed, but the increase in adrenal-gland-to-brain-weight ratio was not statistically significant (<em>p</em> &gt; 0.05). Changes in biological stress markers, including organ and total body weights, changes in leukocyte counts, as well as reduced food consumption behaviour, serve as evidence to suggest that the hypertrophy was likely not due to adrenocortical steroidogenic inhibition by RDAC. Female rats exhibited a stronger stress response. RDAC suppressed the cell infiltration of Harderian glands.</div></div><div><h3>Conclusion</h3><div>The adrenocortical hypertrophy in SD rats was likely a non-pharmacological stress response due to the unpleasant bitter taste of RDAC, potentially exacerbated by the force-feeding procedure. This study is the first evidence to elucidate the mechanism of adrenal gland hypertrophy in rats fed <em>A. cinnamomea</em> without directly assessing the HPA axis function. This underscores the safety of <em>A. cinnamomea</em> and advocates for further pharmacological research.</div></div>","PeriodicalId":34599,"journal":{"name":"Phytomedicine Plus","volume":"4 4","pages":"Article 100659"},"PeriodicalIF":0.0,"publicationDate":"2024-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142534294","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":"HPLC analysis, molecular docking of phenolic compounds and screening of antioxidant and cytotoxic potential of Diospyros malabarica bark extract","authors":"Sirajum Munira ,&nbsp;Mst. Shahnaj Parvin ,&nbsp;Mahci Al Bashera ,&nbsp;Shahnaz Parvin ,&nbsp;Md. Ekramul Islam ,&nbsp;Md. Junaid Haruni","doi":"10.1016/j.phyplu.2024.100657","DOIUrl":"10.1016/j.phyplu.2024.100657","url":null,"abstract":"<div><h3>Background</h3><div><em>Diospyros malabarica</em>, a flowering tree native to the Indian Subcontinent and Southeast Asia, is widely utilized in ayurvedic medicine. This plant is known to contain numerous bioactive compounds. As a result of its traditional uses and medicinal properties, we aim to evaluate the pharmacological properties of its bark both experimentally and <em>in silico</em>.</div></div><div><h3>Methods</h3><div>Polyphenolic compounds in the extracts were identified using High-Performance Liquid Chromatography (HPLC). The antioxidant potential of the extracts was assessed through various methods, including DPPH radical scavenging, reducing power assay, total antioxidant capacity, and protection against oxidative DNA damage. Cytotoxic activity was evaluated using A549 cell growth inhibition and the brine shrimp lethality bioassay. To predict the binding modes of the active compounds within the target protein, molecular docking analysis was conducted.</div></div><div><h3>Results</h3><div>HPLC analysis on EAF confirmed the presence of six polyphenolic compounds including Catechin hydrate, Catechol, (-) Epicatechin, Syringic acid, Rutin hydrate and Kampherol. Antioxidant assay revealed that etylacetate fraction (EAF) showed stronger antioxidant activity as well as better protective effect on oxidative damage to DNA than other fractions. According to docking studies, compounds found in EAF by HPLC showed an impressive propensity for binding to Topoisomerase II. In the brine shrimp assay, different fractions showed moderate cytotoxicity, with LC₅₀ values of 20.63 (CHF), 32.3 (EAF), and 58.17 (NHF) μg/ml, compared to 1.27 μg/ml for vincristine sulfate. Cytotoxicity against A549 human lung cancer cell line, the percentage of cell viability of CHF and EAF (300 μg/ml) were 34.5 and 41.5, respectively. In silico analysis, rutin hydrate exhibited the strongest binding affinity (-9.0 kcal/mol) with Topoisomerase II.</div></div><div><h3>Conclusion</h3><div>The in-vitro study and docking result demonstrates the possession of significant antioxidant and cytotoxic potential of <em>D. malabarica</em> bark extract which could be helpful for anticancer drug development program.</div></div>","PeriodicalId":34599,"journal":{"name":"Phytomedicine Plus","volume":"4 4","pages":"Article 100657"},"PeriodicalIF":0.0,"publicationDate":"2024-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142534296","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}