Chemistry & Biodiversity最新文献

This study investigates the glucosinolate profiles of various Capparis spp. and Maerua baillonii, from the Capparaceae family, and evaluates the cytotoxic potential of volatile isolates from Capparis spinosa subsp. rupestris. Using UHPLC-DAD-MS/MS, GSLs were identified and quantified across different plant tissues. Glucocapparin, predominant glucosinolate in C. spinosa subsp. spinosa, C. spinosa subsp. rupestris, and M. baillonii, was isolated and analyzed by NMR in its desulfo-form. Notably, glucosinolates were absent in C. richardii and specific tissues of M. baillonii (e.g., leaves and stems), underscoring species and/or tissue-specific variability within Capparaceae. Less common glucosinolates for Capparaceae plants, such as glucocochlearin, glucohirsutin, and glucoarabin were also detected. Methyl isothiocyanate was found to be the main volatile in all isolates obtained through various isolation methods, comprising ca. 80-90% of the total volatiles. Methyl isothiocyanate-rich volatile isolates were tested for cytotoxicity against human breast cancer (MDA-MB-231) and bladder cancer (T24) cell lines using the MTT assay, showing significant activity with IC50 values of 3.81 µg/mL and 5.95 µg/mL, respectively. These findings underscore the anticancer potential of glucocapparin-bearing plants from Capparaceae family.

Cervical cancer remains a significant global health challenge, with high mortality rates and a pressing need for more effective therapeutic options. This study investigates the effects of an ethanolic extract from the fruit of Piper retrofractum (PR) on proliferation and apoptosis in cervical cancer cells. We evaluated the cytotoxicity of the crude ethanolic extract of PR using the sulforhodamine B and colony formation assay. ROS generation, apoptosis, and mitochondrial function were quantified via flow cytometry. The effects on cell migration was assessed using wound healing and Transwell migration assays. The PR extract exhibited a significant inhibitory effect on HeLa cell viability, leading to reduced cancer cell proliferation. The extract induced cell cycle arrest at the G0/G1 phase in a dose-dependent manner and decreased the proportion of cells in the G2/M phase at concentrations of 100 and 250 µg/mL. Additionally, treatment with the PR extract resulted in a marked increase in ROS production, disruption of mitochondrial function, and inhibition of cell migration. These findings suggest that the PR ethanolic fruit extract exerts substantial antiproliferative, antimigratory, and proapoptotic effects on HeLa cells. Consequently, the PR ethanolic fruit extract holds promise as a potential novel therapeutic agent for the treatment of cervical cancer.

The present investigation aims to study the therapeutic effect and to identify the lead molecules from lichen Parmotrema reticulatum (Pr) that can solve the complications associated with arthritis. Purification of Pr extract led to isolation of two lead molecules i.e. Compound A (a Dioxepine derivative) as 3-Hydroxy-9-hydroxymethyl-1,8-dimethyl-11-oxo-11H-dibenzo[b,e][1,4]dioxepine-4,7 dicarboxylic acid 7-methyl ester with molecular formula C19H16O9; molecular weight 388.34. Compound B as 3-Hydroxy-5-methoxy-4-methyl-benzoic acid (a Benzoic methyl ester) with molecular formula C9H10O4; molecular weight 182.2. In-silico investigation specific for inflammation revealed good binding affinity of both the compounds with the targeted proteins. Further continuous administration of Pr and novel compound A & B to CFA (Freund's complete adjuvant) induced arthritis rat revealed reduction in arthritis complication possibly by inhibiting the formation of edema. The variations in relative body weight along with paw swelling and arthritic scores were identified. Inhibition of expressions of RA markers like RF, CRP, TNF-𝛼, IL-1𝛽, IL-6, ALP, AST, ALT and LDH were observed there by inhibiting inflammation of synovial cavity and cartilage damage effectively. Hence from our results it is evident that Pr, Compound A & B has down regulated the inflammatory cytokines and can be a potential candidate to treat arthritis.

Herein, a sustainable solid-state procedure was employed for the synthesis of a water soluble molecule obtained d by linking hyaluronic acid to the hydrophobic quercetin (HA-QCT). The micellar   self-aggregation of the developed conjugate suggested its employment as drug delivery nano-system, considering the numerous biological activities of QCT. Indeed, the spectroscopic characterization (UV-vis and FT-IR) ensured that the QCT maintained  its chemical integrity. In addition, a cytotoxicity test revealed that HA-QCT could be employed as a biocompatible drug vehicle for pharmacological purposes. A preliminary colorimetric test also confirmed that QCT retained its anti-oxidant activity.

This study aimed to evaluate the volatile component profiles and antioxidant activities of propolis samples collected from eight regions of Türkiye. The total phenolic content (TPC) of propolis samples was found to vary between 5333 and 36967 mg GAE/100 g. 2.2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activityof the samples varied from 10.9 to 92.2%, while 2.2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) radical scavenging activity varied from 193.8 to 1026.0 µmol trolox/g. Six of the eight samples exhibited higher antioxidant activities than butylated hydroxytoluene (BHT). The predominant volatile components identified in the majority of the propolis samples were α-pinene, limonene, bornyl acetate, caryophyllene, α-humulene, δ-cadinene, isopentyl acetate, acetic acid, nonanal, m-cymene, and pinocarvone. Principal component analysis (PCA) and hierarchical cluster analyses were applied to the GC-MS data to investigate the trends and clustering in the propolis samples. The propolis samples were divided into four groups using cluster analysis. In the PCA, the first two factors represented 56.39% of the variance. These findings revealed that Turkish propolis has significant antioxidant properties and also contains important volatile compounds. Consequently, Turkish propolis could be considered as a potential candidate for incorporation into pharmaceutical and food products.

The extraction of polyphenols from myrtle (Myrtus communis L.) fruits using a conventional solid-liquid extraction was optimized using a single factor experiment approach. The influence of several parameters such as type of solvent (50% acetone, 50% methanol, 50% ethanol and water), solvent concentration (30-100%; v/v), solvent acidity (0-0,1 N), temperature (20-40°C) and time (30-360 min) on the yield extraction of total phenolic content (TPC), total flavonoid content (TFC), total proanthocyanidin content (TPAC), and on the antioxidant activity : DPPH-radical scavenging activity (DPPH-RSA), ABTS-radical scavenging activity (ABTS-RSA) and ferric reducing power (FRP) was studied. The results showed that 50% acetone, 40°C and 180 min were the best conditions for extracting TPC (87 mg GAE/g DW), TFC (12 mg QE/g DW), and TPAC (76 mg CE/g DW). Myrtle berries extracted with these conditions also exhibited the strongest antioxidant activity: DPPH-RSA (7166 mg TE/g DW), ABTS-RSA (164 mg TE/g DW), and FRP (69 mg AAE/g DW). Pearson correlation coefficients showed a good positive correlations between TPC, TFC and TPAC and antioxidant activities (DPPH-RSA, ABTS-RSA and FRP), mainly under the effect of solvent type (0.93 < r < 0.99) and solvent concentration (0.91 < r < 0.99).

Boscia coriacea Graells (BC), Grewia erythraea (Schweinf.) Chiov. (GE), Ochradenus baccatus Delile(OB), and Orthosiphon pallidus Royle ex Benth. (OP) are medicinal plants used in Djibouti. They were evaluated to determine their total phenolic content (TPC), flavonoid content (TFC), and phytochemical profile using HPLC-MS/MS. Additionally, their antioxidant capacity was assessed through five various methods. Enzymatic activities were also measured, focusing on acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-amylase, α-glucosidase, and tyrosinase. OP extract had the highest TPC and exhibited the best antioxidant capacity, while OB and BC extracts had the highest TFC. Twenty-seven compounds were identified and quantified by LCMS. GE extract demonstrated the highest AChE activity, while OP extract had the highest BChE activity. BC was most active against α-amylase and α-glucosidase, and only GE and OP extracts showed tyrosinase inhibition Invitro. In silico analysis, the compounds were optimized and docked to the human tyrosinase-related protein 1 using AutoDock Vina, with ADME to evaluate their suitability based on key therapeutic criteria. Chlorogenic, neochlorogenic, gallic acids and quercetin emerged as promising tyrosinase inhibitors. These plants can be a viable source in the prevention and treatment related to tyrosinase enzyme inhibition.

Fibrosis is a pathological process characterized by excessive extracellular matrix (ECM) deposition and proliferation fibrous tissue, a condition associated with various chronic diseases, such as liver cirrhosis,  inflammation of the lungs, and myocarditis. Clinical treatment options for fibrotic diseases are currently limited and have poor efficacy. However, recent studies have increasingly demonstrated that polysaccharides exhibit significant antifibrotic activity by modulating cell proliferation and migration, inhibiting inflammation and oxidative stress associated fibrosis, and regulating gut microbiota. This review provides an overview of recent advances in polysaccharide research for antifibrosis and offers new perspectives on the treatment of fibrotic diseases.

Malaria disease is an infectious disease, endemic to tropical and sub-tropical regions causing half a million people's deaths every year. Bioactive compounds derived from medicinal plants are used to treat malaria disease. H. cannabinus and C. capsularisare two edible medicinal plants abundant in distribution in the Assam region, India. In this study, in-vitro and in-silico investigations were performed to explore the anti-malarial activity of the plant extracts against Plasmodium falciparum with its validation of hemocompatibility on human RBC. We report H. cannabinus and C. capsularis extracts possess highly potent antimalarial activity against Plasmodium falciparum with IC50 values of 3.80 ± 0.3 μg/mL and 7.90 ± 0.8 μg/mL, respectively. The plant extracts showed growth inhibition of A549 lung adenocarcinoma cells, no toxicity on noncancerous Vero cells, and no hemolytic activity on human RBCs. The GC-MS analysis detected bioactive compounds 2-pyrazoline-3-carboxylic acid; 5-hydroxy-1-(4-methyl benzoyl)-5-phen 5-oxo-1-phenyl-4H-pyrazole-3-carboxylic acid; 9-oximino-2,7-diethoxyfluorene; and nonane-diamide, n, n'-di-benzoyloxy in H. cannabinus; and, (+)-sesamin; tetrahydropyran-4-carboxylic acid, 4-phenyl-, (3-chloro-4-methylphenyl; and safrole in C. capsularis. In the in-silico study, antimalarial compounds in the extracts were predicted with good binding affinities of docking score < -7.5 kcal/mol on Falcipain-2, and Cyt C2 proteins that help the growth and invasion of P. falciparum.

Pharmacological studies have shown that podophyllotoxin (PTOX) has anti-tumor, antiviral and anti-inflammatory effects. More and more derivatives of PTOX, such as VM-26, NK-611 and GL-331, have gradually been synthesized and widely used in clinical practice. Sinopodophyllum hexandrum rhizome is rich in PTOX, which is much higher than other PTOX source plants. At present, research on S. hexandrum mainly focuses on artificial cultivation, chemical compositions, pharmaceutical value and the biosynthesis pathway of PTOX. However, the researches are relatively scattered and systematic review on PTOX is very limited. Therefore, this study performed a comprehensive investigation in terms of the plant origin source, content profile, and biological activities, in order to provide an integrated reference for in-depth research and clinical application of PTOX in the chemistry and pharmacy fields, which can promote the innovative utilization of S. hexandrum resources and research and development of new anticancer drugs.