Chemistry & Biodiversity最新文献

The agricultural bioactivity of 7-alkenylcoumarin derivatives was investigated by synthesizing a series of coumarin derivatives containing 7-styryl fragments by introducing a styryl group at the 7-position of the coumarin scaffold through Pechmann cyclization, substitution, bromination, and Wittig reaction. The insecticidal effects and antifungal activities of these compounds against plant pathogenic fungi were evaluated. Bioactivity assessments revealed that compound 5i exhibited the highest larvicidal activity against Aedes aegypti, with a mortality rate of 96% after 24 h of treatment. Compounds 5i, 5e, and 5a displayed the strongest antifungal activity against Colletotrichum musae, with EC50 values of 0.42, 3.44, and 3.67 mg/L, respectively, outperforming the commercial fungicide bromothalonil (9.31 mg/L) and comparable to chlorothalonil (0.74 mg/L). Structure-activity relationship analysis indicated that the presence of a chlorine atom at the 4-position of the phenyl ring was critical for the bioactivity of the compounds. Docking results indicated that compound 5i exhibited the strongest binding affinity for succinate dehydrogenase, providing insights for further mechanistic studies. These findings suggest the significant potential of these compounds as lead candidates for in-depth research and development.

Although therapeutic proteins have achieved recognized clinical success, they are inherently membrane impermeable, which limits them to acting only on extracellular or membrane-associated targets. Developing an efficient protein delivery method will provide a unique opportunity for intracellular target-related therapeutic proteins. In this review article, we summarize the different pathways by which cells take up proteins. These pathways fall into two main categories: One in which proteins are transported directly across the cell membrane and the other through endocytosis. At the same time, important features to ensure successful delivery through these pathways are highlighted. We then provide a comprehensive overview of the latest developments in the transduction of covalent protein modifications, such as coupling cell-penetrating motifs and supercharging, as well as the use of nanocarriers to mediate protein transport, such as liposomes, polymers, and inorganic nanoparticles. Finally, we emphasize the existing challenges of cytoplasmic protein delivery and provide an outlook for future progress.

Type 1 diabetes (T1D) poses a significant global health challenge, with current treatments often proving inadequate. This study provides a comprehensive evaluation of the antihyperglycemic effects of methanolic extract from Algerian Trigonella foenum-graecum L. seeds (MEF) in type 1 diabetic rats, combining both in-vivo and in-silico studies: molecular docking and ADMET. Polyphenol compounds (PCs) identified. Twenty-four male rats divided into four groups: control, normal and diabetic rats treated with MEF. T1D was induced via a single 50 mg/kg streptozotocin injection. MEF was administered orally at a dose of 400 mg/kg b.w. for 28 days, with measurements of body weight and fasting blood glucose. Histopathological examinations of pancreatic tissues were conducted post-treatment. HPLC identified fifteen PCs. We found that six main PCs had strong binding affinities for the IR (-9.463 to -7.893 kcal/mol). The ADMET modeling indicated favorable drug-likeness, oral bioavailability, and no toxicity risk. Significantly, diabetic rats treated with MEF exhibited a marked reduction in fasting blood glucose levels (494.67 mg/dl to 144.17 mg/dl; p < 0.001), along with an increase in body weight and improvements in the pancreatic islets of Langerhans. These findings suggest that MEF possesses substantial antihyperglycemic potential and may play a role in managing T1D complications.

The Chinese tallow tree (Sapium sebiferum (L.) Roxb) (CTT) is a valuable forest resource, and its leaves have long been utilized in Traditional Chinese Medicine for the treatment of various diseases, primarily due to the antioxidant activity of phenolic compounds. In this study, a simple ultrasonic-assisted phenolic extraction method was established using response surface methodology. The highest total phenolic content was obtained by extracting with 40% ethanol (v/v) in a solid-liquid ratio (g/mL) of 1:48 for 20 min at 30°C, employing an ultrasonic bath with a power of 270 W and a frequency of 40 kHz. Using the optimized phenolic extract, a non-target metabolomics approach was adopted to evaluate the antioxidant ingredients of the CTT. Most of the identified phenolic compounds were depleted after reacting with free radicals, indicating their significant contribution to the antioxidant activity of CTT leaves. Among them, gallic acid derivatives, geraniin, and ethyl gallate were identified as the predominant antioxidant ingredients. Overall, a simple ultrasonic-assisted phenolic extraction method was optimized, and the antioxidant ingredients of the valuable CTT leaves were identified. These findings significantly promote the development and application of CTT leaves.

This study investigates the accumulation of toxic heavy metals-cadmium (Cd), chromium (Cr), cobalt (Co), nickel (Ni), lead (Pb), and strontium (Sr)-in potato tubers grown under diverse meteorological and soil conditions in east-central Poland. Conducted from 2021 to 2023 at the Variety Assessment Experimental Station in Uhnin on light acidic soil, the field experiment employed a randomized block design with 3 replications. Forty potato cultivars of varying maturity were evaluated, with agronomic practices adhering to GAP and uniform fertilization applied. Potato tubers were exposed to thermal neutron flux for 2 hours. Gamma radiation detection was conducted using a high-purity germanium (HPGe) detector cooled with liquid nitrogen to enhance resolution. The study highlights significant phenotypic variability in heavy metal accumulation, influenced by genetic, environmental, and genotype × environment interaction factors. Results showed substantial effects of cultivar, year, and their interactions, with varieties (V) accounting for 8.7-36.2% of the variance, environmental factors (Y) contributing 41.2-82.2%, and genotype × environment interactions (V × Y) ranging from 5.5-46.7%. Year-to-year variability was most pronounced for lead, while nickel showed the least variability. Soil pH and humus played a key role in shaping the bioavailability and accumulation of metals in potato tubers.

Four new cassane derivatives (1-4), along with five known compounds (5-9) were isolated from the seeds of Caesalpinia mimosoides. Their gross structures were elucidated by means of comprehensive spectroscopic analysis (UV, NMR, HRESIMS) as well as electronic circular dichroism (ECD) calculations. Compounds 1-3 possessing norcassane-type skeleton were observed, which was rare structural type in the Caesalpinia genus. The results of biological activity evaluation showed that compounds tested could inhibit the production of NO in LPS-induced RAW 264.7 cells, especially compound 8 exhibited excellent inhibitory activity, implied that these compounds may be potential anti-inflammatory candidates.

Pectin, a plant-derived polysaccharide, is highly valued for its gelling, thickening, and stabilizing properties, with extensive applications in the food and pharmaceutical industries. This review provides a comprehensive analysis of pectin's structure, categorized by its degree of methyl esterification (DM) and key components, including homogalacturonan (HG) and rhamnogalacturonans (RG-I and RG-II). The influence of diverse extraction methods, such as subcritical water and microwave-assisted techniques, on its structure and functionality is critically examined. Furthermore, the review investigates the absorption, distribution, metabolism, and excretion (ADME) profiles of pectin, emphasizing how structural factors like molecular weight, DM, and neutral sugars impact bioavailability and interactions with gut microbiota. Notably, this review highlights emerging research methodologies, offering novel insights into pectin's pharmacokinetics. By addressing these interrelationships, the review underscores pectin's potential applications in functional foods, personalized nutrition, and targeted therapeutics and identifies key knowledge gaps for future research.

Pachysandra (the family Buxaceae) is a small genus containing medicinal plants. This brief communication first describes its phytochemistry and pharmacological activities. More than 140 metabolites were separated, and steroidal alkaloids-based pregnane skeletons were the main compounds obtained. (+)-Axillaridine A, epipachysamines B and D-E, pachysandrines B-D, pachysamines A-B, pachystermine A, and (+)-spiropachysine are likely primary metabolites. Various compounds were identified as previously undescribed compounds. Non-alkaloids, such as sterols, triterpenoids, mono-phenols, coumarins, megastigmanes, and lignans, were also identified. Pachysandra steroidal alkaloids showed potential for drug development as they exhibited anticancer, antimicrobial, antiestrogenic, and gastric protective activities. The amine substituents at carbons C-3 and C-20 might cause differences in pharmacological results. The underlying mechanisms, such as the PI3K/Akt/mTOR signaling pathway, were proposed to explain pharmacological activities. Pachysandra phytotoxins exhibited antioxidative and antidiabetic activities. Synthetic products of Pachysandra steroidal alkaloids had higher cytotoxic effects than the natural compounds.

Biofouling, which is the accumulation of organisms on undersea structures, poses significant global, social, and economic issues. Although organotin compounds were effective antifoulants since the 1960s, they were banned in 2008 due to their toxicity to marine life. Although tin-free alternatives have been developed, they also raise environmental concerns. This underscores the need for effective, nontoxic antifouling agents. We previously synthesized N-(4-aminobutyl)propylamine (xylemin) and its structural analogs. In this study, we assayed the antifouling activity and toxicity of xylemin, its structural analogs, and related polyamines toward cypris larvae of the barnacle Amphibalanus amphitrite. Xylemin and its Boc-protected analog exhibited antifouling activities with 50% effective concentrations (EC₅₀) of 4.25 and 6.11 µg/mL, respectively. Four xylemin analogs did not show a settlement-inhibitory effect at a concentration of 50 µg/mL. Putrescine, spermidine, spermine, and thermospermine, which are xylemin-related polyamines, did not display antifoulant effects (EC₅₀ > 50 µg/mL). All evaluated compounds were nontoxic at a concentration of 50 µg/mL. These findings indicate that the size and structure of the N-alkyl group are essential for the antifouling activity of xylemin. Therefore, xylemin and its analogs hold promise as nontoxic, eco-friendly antifouling agents, offering a sustainable solution to biofouling in marine environments.

Cervical cancer is one of the cancers commonly found in the female reproductive system and is associated with obesity. However, the exact connection mechanisms remain unclear. Screening of key therapeutic targets and natural products with good anti-tumor activity has become a crucial strategy for cancer therapy. Cryptotanshinone has anti-inflammatory and anti-cancer properties. Key therapeutic targets and related low-toxicity natural active ingredients were identified as crucial components in cancer treatment strategies. Therefore, network pharmacology and cellular biology techniques were used to screen and validate key targets in obesity-related cervical cancer and to elucidate the mechanisms. The results indicated that C-X-C motif chemokine ligand 8 (CXCL8) might be modulated by cryptotanshinone. The knockdown of CXCL8 significantly reduced Hela cell viability to 15.29 ± 4.59% compared with the control group (p<0.01), which consequently inhibited both cell proliferation and lipid droplet formation. Moreover, cryptotanshinone (20, 40, and 80 μM) significantly reduced CXCL8 expression and inhibited the NOD-like receptor signaling pathway in Hela cells compared with the control group (p<0.01). Therefore, this study manifested that cryptotanshinone potentially played an important role in obesity-related cervical cancer. This study provided the important experimental basis for further exploring the pathogenesis and prevention of obesity-related cervical cancer.