Chemistry & Biodiversity最新文献

Emex spinosa (L.) Campd. (E. spinosa) is a plant species belonging to the Polygonaceae family. It is native to the Middle East, North Africa, and Europe and is most commonly seen on the coastlines of Mediterranean countries. Additionally, it occurs primarily throughout Spain, Portugal, Israel, and Morocco. The plant is frequently utilized for managing an extensive variety of illnesses, including indigestion, jaundice, liver troubles, constipation, and liver problems. However, there is a lack of comprehensive resource material on the traditional uses, nutritional benefits, phytochemical, pharmacological, and toxicological assessments of this plant. This review seeks to highlight the traditional uses, chemical composition, and medicinal attributes of Emex spinosa species. Moreover, this study explored the medicinal, chemical composition, and toxicological aspects of E. spinosa. In addition, this investigation aimed to analyze and document all available information and scientific discoveries on the medicinal applications and phytochemical attributes of this plant. Furthermore, the review was carried out using several research and scientific networks, including Scopus, ScienceDirect, PubMed, and Google Scholar. The correctness of the plant names has been checked using plantlist.org. The study findings were assessed, reviewed, and reported using the bibliographic data acquired. In addition, this herb is widely used in traditional healing because of its high phytochemical composition. E. spinosa produces a wide range of secondary metabolites, including alkaloids, flavonoids, and anthraquinones. It also contains coumarins, saponins, sterols, tannins, and volatile oils that have been discovered to be related to their therapeutic properties. These phytochemicals are ideal for potential application to modern therapeutic agents because of their antibacterial, antifungal, cytotoxic, antidiabetic, antioxidant, antiulcer, and anti-inflammatory properties. The secondary metabolites of plants are increasingly being used as scaffolds for medications and for nutritional supplements, including for flavoring. Lastly, toxicological studies have demonstrated the relative safety of moderate doses of E. spinosa extracts. This review explored the geographic distribution, chemical components, and main applications of E. spinosa in order to determine future research interest and conduct clinical studies, where possible, to investigate its medicinal applications.

UC is a globally escalating intestinal disorder with limited safe and effective interventions. This study investigated the synergistic therapeutic effects and mechanisms of Lactobacillus johnsonii 46 (L. johnsonii 46) (a feruloyl esterase-producing strain) and rice bran (LJRB) on DSS-induced UC in C57BL/6J mice. The animal groups were divided into control group (CON), DSS group (MOD), sulfasalazine group (SUL), rice bran group (RBN), L. johnsonii 46 group (LAJ), and LJRB treatment group (RBL). The organ index, disease index, and biochemical indicators of mice were measured, the histopathology of the colon was analyzed. The expression of inflammatory factor, tight junction protein and TLRs/TRAF6/NF-κB signaling pathway genes were detected by Real-Time Quantitative Polymerase Chain Reaction (RT-qPCR). LJRB supplementation exerted superior protective effects compared to single rice bran (RBN) or L. johnsonii 46 (LAJ) intervention: it significantly alleviated DSS-induced weight loss (RBL group: 1.46 ± 0.21 g vs. MOD group: ∼3 g, p < 0.05), restored colon length, and reduced the disease activity index (DAI) by ∼50%. Biochemical and molecular analyses showed LJRB remarkably suppressed serum pro-inflammatory cytokines (IL-1β, TNF-α, IL-6; 40%-60% reduction vs. MOD group) while elevating anti-inflammatory IL-10 (∼35% increase), enhanced colonic antioxidant capacity (reduced MDA by ∼30% and increased SOD, GSH, GSH-Px by 25%-40%), and enriched cecal short-chain fatty acids (SCFAs) with acetic acid (0.99 µmol/g), propionic acid (0.31 µmol/g), and butyric acid (0.21 µmol/g) significantly higher than the MOD group. Mechanistically, LJRB synergistically inhibited the TLRs/TRAF6/NF-κB signaling pathway, as indicated by downregulated mRNA expression of TLR4, MyD88, IKKβ, and NF-κB p65 (30%-50% reduction vs. MOD group) and decreased phosphorylation of IKKβ, IκBα, and NF-κB p65 proteins. Histopathological observations confirmed LJRB preserved colon tissue integrity, reduced goblet cell loss, and alleviated mucosal erosion and edema. Collectively, these findings demonstrate LJRB alleviates UC through multi-targeted mechanisms (anti-inflammation, antioxidation, SCFA production promotion, and nuclear factor kappa-B (NF-κB) pathway inhibition), highlighting its potential as a novel natural dietary supplement for UC prevention and management.

The organotellurane RF07 (RF07) is an organic compound containing tellurium, a rare semi-metal, and its leishmanicidal and antimalarial activity has already been reported in previous studies. This study evaluated the toxic effects of RF07 at 0.42, 21.37, and 42.75 mg/kg using comet assay, micronucleus test, and hematological/biochemical tests in Mus musculus. Female Swiss mice received intraperitoneal RF07. Blood was collected at 24, 48, and 72 h, followed by euthanasia for bone marrow analysis. Results showed RF07 increased DNA damage, clastogenic/aneugenic effects via micronuclei formation, and cytotoxicity through apoptosis in bone marrow erythroid precursors and altering the ratio of polychromatic to normochromatic erythrocytes. RF07 also caused myelosuppression and hepatotoxicity. To our knowledge, this is the first study explore these toxic effects. However, the mechanism remains unclear, requiring further investigation.

Genus Rheum is known for its abundant and therapeutically important phytoconstituents across traditional medicine systems. Their synthesis and accumulation are highly complex, influenced by environmental factors and developmental genetic circuits. This study aimed to identify and quantify specialized metabolites (SMs), assess the impact of altitude and environmental stress, and evaluate total antioxidant potential in five Rheum species from different ecological niches of the NW Indian Himalayas. Among seven extraction solvents tested by HPLC-ESI-MS/MS, ethyl acetate provided the highest yield and was used for all subsequent extractions. LC-QTOF-MS analyses revealed R. spiciforme as the richest in metabolite content, followed by R. australe, R. tibeticum, R. webbianum, and R. moorcroftianum. Intra-specific chemical variability identified elite chemotypes within species. Altitude positively correlated with metabolite accumulation and enhanced antioxidant components, including photopigments, flavonoids, and phenolics. Higher altitudes were associated with increased oxidative stress, reflected by elevated levels of ascorbate peroxidase, catalase, superoxide dismutase, and proline. Five non-enzymatic assays confirmed R. tibeticum and R. spiciforme as having the highest antioxidant potential. Overall, these findings provide novel insights into the interactions between species, environmental factors, and bioactive metabolite synthesis, enhancing our understanding of plant adaptive responses to diverse stress stimuli.

Piper cubeba (P. cubeba), renowned for its antioxidant properties, has traditionally been used to counteract pro-oxidant effects caused by toxicants. This study investigated the potential immunomodulatory and antioxidant activities of γ-irradiated P. cubeba in a model of rheumatoid arthritis (RA) induced by complete Freund's adjuvant (CFA) in female Wistar rats. RA was induced by a single subcutaneous injection of 0.1 mL of CFA into the right hind footpad. For 3 weeks, arthritic rats received an oral dose of methanolic extract of γ-irradiated P. cubeba (50 mg/kg body weight/day). Blood and tissue samples were measured for MMP-1, MMP-3, ACCP, TNF-α, IL-17, IL-10, and NQO1 levels using ELISA, as well as for the oxidative stress marker MDA and the antioxidant enzyme SOD. CFA-induced RA resulted in marked increases in the expression of cyclooxygenase-2 (COX-2), tumor necrosis factor-alpha, oxidative stress markers, and matrix metalloproteinases. Meanwhile, treatment with irradiated P. cubeba reduced the severity of these changes by increasing anti-inflammatory cytokine IL-10 and enhancing FOXP3 expression, a key regulator of T regulatory (Treg) cells, in arthritic rats. These findings demonstrate that irradiated P. cubeba exerts immunomodulatory, antioxidant, and anti-inflammatory effects.

This study presents a comparative analysis of sulfated polysaccharides extracted from Ulva lactuca collected in Tunisia (PSUT) and Morocco (PSUM). FTIR confirmed the presence of sulfate groups, while GC-MS identified diverse sugar components. Both polysaccharides showed strong antioxidant activity, with DPPH and ABTS radical scavenging rates exceeding 50% at the highest concentrations. In a rat model of gastric ulceration, PSUT and PSUM significantly reduced inflammation and lymphocytic infiltration and lowered the activities of 5-lipoxygenase and myeloperoxidase. Treatment also produced clear antioxidant effects, decreasing hydrogen peroxide by 48% and 61% and reducing TBARS by 65% and 71%, respectively. In addition, both polysaccharides inhibited gastric H⁺/K⁺-ATPase and pepsin, contributing to notable anti-acidic effects and improved protection of the gastric mucosa. Mucin levels increased by 82% and 100%, while gastric mucus content rose by 32% and 71% for PSUT and PSUM. Overall, PSUM displayed stronger in vivo anti-inflammatory and gastroprotective activities, whereas PSUT showed slightly higher in vitro antioxidant capacity. These findings confirm that the geographic origin of U. lactuca influences the structural features of its polysaccharides and their biological effects. Although based on a single animal model and dose, this work offers a solid basis for future mechanistic and clinical investigations.

Quinazoline-based scaffolds are well recognized for their therapeutic potential, particularly in the development of anticancer agents targeting tyrosine kinase-mediated signaling pathways. In the present study, a series of novel quinazoline derivatives bearing cyclopropane-1,1-dicarboxamide moieties were designed, synthesized, and evaluated for their anticancer activity against human colorectal cancer (CRC) cell lines. The synthesized compounds were structurally characterized using 1H and 13C NMR spectroscopy and high-resolution mass spectrometry. Their in vitro antiproliferative activity was assessed against HT-29 and COLO-205 cell lines using the MTT assay, with cabozantinib serving as the reference standard. Several compounds demonstrated promising cytotoxic activity, with compound SQ14 exhibiting the most potent inhibitory effect, comparable to the standard drug. Molecular docking and molecular dynamics simulations were performed to elucidate binding interactions and stability within the active site of the target protein, revealing favorable binding orientations and key intermolecular interactions. Furthermore, in silico ADMET analysis supported the drug-like nature and acceptable pharmacokinetic profiles of the lead compounds. Overall, the integrated experimental and computational findings suggest that the newly synthesized quinazoline derivatives, particularly SQ14, represent promising candidates for further development as potential anticancer agents against CRC.

The non-flavonoid polyphenol, resveratrol, has a wide range of biological properties and the potential to form many different products. Resveratrol acts on multiple biological targets and is a potent antioxidant in a variety of pathological conditions. The aim of this review is to provide a comprehensive overview of the latest research on the chemistry, biosynthetic pathways, methods of preparation, and biological properties, specifically, anticancer and antioxidant properties of resveratrol, as well as the nuances of pharmacokinetics with a special emphasis on bio-enhancement approaches. Insights into different delivery systems showed the dynamic landscape of resveratrol delivery and addressed the challenges and innovations in improving bioavailability. This review will provide a comprehensive overview of resveratrol's potential as an antioxidant and anticancer agent, its pharmacokinetics, and extraction methods, as well as various synthetic routes for its synthesis. Therefore, it will pave the way for future research and clinical applications in combating cancer and oxidative stress-related diseases and contribute to advancements in healthcare and medicine.

Carbonic anhydrase IX (CA IX) is overexpressed in many solid tumors, contributing to cancer cell proliferation, survival, invasion, and metastasis. Sulfonamide-based compounds have emerged as potential anticancer agents by inhibiting this enzyme. In this study, we investigated the anticancer potential of a previously synthesized sulfonamide derivative, MMH-I, focusing on its CA IX-targeted activity and therapeutic efficacy in both in vitro and in vivo models of breast cancer. Cytotoxicity was assessed using MTT assays in 4T1 breast cancer cells, while apoptosis was evaluated by acridine orange/ethidium bromide staining and Annexin V detection. In vivo studies analyzed tumor tissues for CA IX expression, as well as Vimentin, E-Cadherin, and Caspase-3 levels. H&E staining and plasma metabolomic analysis were performed to assess tissue morphology and metabolic alterations. The compound significantly reduced tumor volume, induced apoptosis, and altered cancer-related gene expression and metabolic profiles. Overall, this study provides a detailed in vivo and metabolic evaluation of MMH-I in breast cancer, highlighting its potential as a CA IX-targeted therapeutic candidate and supporting further investigation of sulfonamide-based combination strategies against hypoxic tumors.

Acne vulgaris is a multifactorial skin disorder involving sebaceous gland dysfunction, hormonal imbalances, bacterial overgrowth, and inflammation. While various cosmeceutical products target these mechanisms, there remains a strong demand for natural alternatives with multi-target actions. Citrus hystrix, a traditional medicinal plant, exhibits notable anti-inflammatory properties, suggesting its potential for acne treatment. This study assessed the in vitro biological activities of C. hystrix peel extracts and essential oil by examining their effect on Propionibacterium acnes and inflammatory targets. In vitro assays demonstrated that extract polarity significantly affected the observed bioactivities, resulting in distinct activity profiles among the extracts. The hexane extract (34.12% ± 2.56%) and essential oil (43.65% ± 8.44%) exhibited greater 5α-reductase inhibition at 100 mg/mL compared to the ethanolic extract (15.64% ± 1.66%). Conversely, the ethanolic extract more effectively inhibited IL-1β, nitric oxide, and PGE₂ production. In addition, P. acnes growth inhibition was observed across all samples. These findings highlight C. hystrix as a promising multi-target anti-acne agent. Further research should explore formulation strategies, skin penetration, and clinical efficacy.