Cytotoxic sesquiterpene lactones and lignans from <i>Cousinia turkmenorum</i> Bornm (Asteraceae)

Seven sesquiterpene lactones, chlorophyssopifolin E (1), aguerin B (2), repdiolide triol (3), solistitiolide (4), aitchisonolide (5), sinicin B (6), cynaropicrin (7), along with four lignans arctigenin (8), arctiin (9), matairesinol (10), and matairesinoside (11) were isolated for the first time from the aerial parts of Cousinia turkmenorum Bornm. Among the isolated compounds, aguerin B (2) showed the most cytotoxic activity against MCF7 cell lines with IC50 value of 18.9 μM. Findings of this study could be useful for the development of new anticancer agents from nature.</p

Antifibrotic effects of sodium-glucose cotransporter-2 inhibitors: a comprehensive review

Background and aims: Scar tissue accumulation in organs is the underlying cause of many fibrotic diseases. Due to the extensive array of organs affected, the long-term nature of fibrotic processes and the large number of people who suffer from the negative impact of these diseases, they constitute a serious health problem for modern medicine and a huge economic burden on society. Sodium-glucose cotransporter-2 inhibitors (SGLT2is) are a relatively new class of anti-diabetic pharmaceuticals that offer additional benefits over and above their glucose-lowering properties; these medications modulate a variety of diseases, including fibrosis. Herein, we have collated and analyzed all available research on SGLT2is and their effects on organ fibrosis, together with providing a proposed explanation as to the underlying mechanisms. Methods: PubMed, ScienceDirect, Google Scholar and Scopus were searched spanning the period from 2012 until April 2023 to find relevant articles describing the antifibrotic effects of SGLT2is. Results: The majority of reports have shown that SGLT2is are protective against lung, liver, heart and kidney fibrosis as well as arterial stiffness. According to the results of clinical trials and animal studies, many SGLT2 inhibitors are promising candidates for the treatment of fibrosis. Recent studies have demonstrated that SGLT2is affect an array of cellular processes, including hypoxia, inflammation, oxidative stress, the renin-angiotensin system and metabolic activities, all of which have been linked to fibrosis. Conclusion: Extensive evidence indicates that SGLT2is are promising treatments for fibrosis, demonstrating protective effects in various organs and influencing key cellular processes linked to fibrosis.</p

Dereplication of cytotoxic compounds from different parts of <i>Sophora pachycarpa</i> using an integrated method of HPLC, LC-MS and ¹H-NMR techniques

<p><i>Sophora pachycarpa</i> Schrenk ex C.A.Mey. is an annual plant belonging to the family Fabaceae. The cytotoxic activities of methanol-dichloromethane extracts (1:1) of different parts of <i>S. pachycarpa</i> were investigated on DU145 (prostate cancer cell line) and MCF-7 (breast cancer cell line) cell lines. The root extract of <i>S. pachycarpa</i> was the only extract that showed significant cytotoxic activity with IC₅₀ values of 39.88 and 16.49 μg/mL on DU145 and MCF-7 cell lines, respectively. The root extract was then subjected to RP-HPLC for further fractionations. Among the isolated fractions from root extract, only one of them had remarkable cytotoxic effects with IC₅₀ value of 26.43 on MCF-7 and 7.54 μg/mL on DU145 cell lines. Further purification led to isolation of a compound with IC₅₀ values of 5.44 and 2.44 μg/mL on MCF-7 and DU145 cell lines, respectively. Based on ¹H NMR and ¹³C NMR spectra, together with LC-MS, the structure of the purified compound was assigned as the flavonostilbene alopecurone A.</p

Additional file 1 of Effects of Melissa officinalis (lemon balm) consumption on serum lipid profile: a meta-analysis of randomized controlled trials

Supplementary Material

New polyacetylenes from <i>Echinophora cinerea</i> (Boiss.) Hedge <i>et</i> Lamond

<p><i>Echinophora cinerea</i> aerial parts are used in folk medicine to cure gastric diseases and as a food seasoning in cheese and yogurt. Besides several pharmacological effects have been assigned to <i>Echinophora</i> spp., there is no phytochemical investigation on this genus other than our previous publication on flavonoids. An acetone extract of <i>E. cinerea</i> afforded three new (<b>1–3</b>) polyacetylenes, one rare monoterpenoid glycoside as verbenone-5-<i>O</i>-<i>β</i>-D-glycopyranoside (<b>4</b>) and one prenylated coumarin as osthol (<b>5</b>). The structures of all new compounds were elucidated using modern spectroscopic methods, including 2D NMR and mass analyses. The potency of the compounds to induce cell death was determined on SKNMC, PC3 and MCF-7 cell lines using MTT method in which compounds <b>1</b> and <b>2</b> showed moderate cytotoxic effects, especially against PC3 cells.</p

Discovery of non-peptide GLP-1r natural agonists for enhancing coronary safety in type 2 diabetes patients

This study explores the computational discovery of non-peptide agonists targeting the Glucagon-Like Peptide-1 Receptor (GLP-1R) to enhance the safety of major coronary outcomes in individuals affected by Type 2 Diabetes. The objective is to identify novel compounds that can activate the GLP-1R pathway without the limitations associated with peptide agonists. Type 2 diabetes mellitus (T2DM) is associated with an increased risk of cardiovascular disease (CVD) and mortality, which is attributed to the accumulation of fat in organs, including the heart. Glucagon-like peptide-1 receptor agonists (GLP-1RAs) are frequently used to manage T2DM and could potentially offer cardiovascular benefits. Therefore, this study examines non-peptide agonists of GLP-1R to improve coronary safety in type 2 diabetes patients. After rigorous assessments, two standout candidates were identified, with natural compound 12 emerging as the most promising. This study represents a notable advancement in enhancing the management of coronary outcomes among individuals with type 2 diabetes. The computational methodology employed successfully pinpointed potential GLP-1R natural agonists, providing optimism for the development of safer and more effective therapeutic interventions. Although computational methodologies have provided crucial insights, realizing the full potential of these compounds requires extensive experimental investigations, crucial in advancing therapeutic strategies for this critical patient population. Communicated by Ramaswamy H. Sarma</p

Sesquiterpene lactones from <i>Centaurea rhizantha</i> C.A. Meyer

<p>Two new sesquiterpene lactones, rhizantholide A (<b>1</b>) and rhizantholide B (<b>2</b>), together with five known compounds (<b>3-7</b>) have been isolated from the aerial parts of <i>Centaurea rhizantha</i> (Asteraceae). Sesquiterpene lactones belong to guaianolide class, and rhizantholide B is a rare guaianolide characterized by a free primary alcoholic function at C-10 along with a 3β,10β-epoxy function. Their structures have been established on the basis of 1D and 2D NMR experiments, as well as HR-ESIMS. The antimicrobial activity of compounds <b>1-7</b> has been evaluated against Gram-positive and Gram-negative strains. Only deacylcynaropicrin 8-<i>O</i>-[3′-hydroxy-2′-methylpropionate] (<b>5</b>) showed moderate antibacterial activity against <i>Staphylococcus aureus</i> with a MIC/MBC value of 500 μg/mL. All isolated compounds have been also evaluated for their cytotoxic activities against cancer cells. Among them, compound <b>5</b> showed the highest cytotoxic activity with IC₅₀ values in the range 5.02–16.76 μg/mL.</p

HPLC-Based Activity Profiling for Antiprotozoal Compounds in the Endemic Iranian Medicinal Plant <i>Helichrysum oocephalum</i>

In a screening of Iranian plants for antiprotozoal activity a dichlomethane extract from the aerial parts of Helichrysum oocephalum showed in vitro antiprotozoal activity against Plasmodium falciparum and Leishmania donovani, with IC50 values of 4.01 ± 0.50 and 5.08 ± 0.07 μg/mL, respectively. The activity in the extract was tracked by HPLC-based activity profiling, and subsequent targeted preparative isolation afforded 24 compounds, including pyrones 22–24, phloroglucinol derivatives 12–19, and compounds containing both structural motifs (1–11, 20, and 21). Of these, 15 compounds were new natural products. The in vitro antiprotozoal activity of isolates was determined. Compound 3 showed good potency and selectivity in vitro against L. donovani (IC50 1.79 ± 0.17 μM; SI 53)

GC/MS profiling of the essential oils from <i>Ferula xylorhachis</i> Rech.f. roots and aerial parts and assaying their antimicrobial activity against human skin pathogens

The plants of the genus Ferula (Apiaceae), with more than 180 species found worldwide, have been a source of numerous bioactive secondary metabolites. In this study, we isolate the essential oils from different parts of an Iranian endemic species Ferula xylorhachis Rech.f. -for the first time- by hydro-distillation and further characterized their chemical profile by GC/MS analysis. In addition, we evaluated their antimicrobial properties against a set of skin pathogens, namely Staphylococcus aureus, Pseudomonas aeruginosa and Candida albicans. GC/MS analysis of the essential oils resulted in the identification of seventy-two compounds representing 98% and 90.2% of all volatile compounds in the aerial parts and the roots, respectively. Some of these compounds, mainly the monoterpenes and aliphatic hydrocarbons, were also detected in headspace GC/MS analysis of the dried plant parts. The oil compositions were dominated by the monoterpene hydrocarbons in the aerial parts, and aliphatic hydrocarbons in the roots. The principal chemical constituents were sabinene (17.6%), α-pinene (16.2%) and n-nonane (14%) in the essential oil from the aerial parts, and n-nonane (56.5%), 10s,11s-himachala-3(12),4-diene (6.9%) and β-himachalene (2.3%) in the essential oil from the roots. While the essential oils did not show activity against tested bacterial strains, they both exhibited antifungal activity against C. albicans at varying concentrations, which was promising in the case of roots essential oils which exhibited an MIC of 250 μg/mL. Based on our findings, the topical use of F. xylorhachis roots essential oils could be considered an alternative therapy for superficial infections caused by Candida species.</p

Sesquiterpene Coumarins from <i>Ferula gumosa</i>

A new sesquiterpene coumarin, gumosin (1), two new sesquiterpene coumarin glycosides, gumosides A (2) and B (3), and 10 known compounds, namely, cauferoside (4), feselol (5), conferoside, ferilin, ferocaulidin, ligupersin A, conferol, and daucosterol, and the phenolic compounds acantrifoside E and 4-hydroxybenzoic acid 4-(6-O-sulfo)glucopyranoside, were isolated from a methanolic extract of Ferula gumosa roots. The structures of 1−3 were elucidated by spectroscopic data interpretation. The cytotoxic activity of the sesquiterpene coumarin derivatives was evaluated against a small panel of cancer cell lines