Chemistry & Biodiversity最新文献

The present study investigated the phytochemical composition of Thymus capitatus L. essential oil (TCEO) harvested in Morocco using GC/MS-MS analysis. The study of the antioxidant activity revealed that TCEO exhibits a good activity in DPPH, ABTS, and FRAP assays as the obtained values were 67.34 ± 1.54, 96.88 ± 2.76 µg/L, and 99.07 ± 1.57 µg/mL, respectively. The antibacterial activity revealed that TCEO was most active toward the 2 Gram positive bacteria (S. aureus and L. monocytogenes). TCEO displayed markedly lower IC50 values, 111.79 ± 2.88 μg/mL for α-amylase and 70.42 ± 1.68 μg/mL for α- glucosidase than those of acarbose (389.04 ± 1.65 and 187.82 ± 2.62 μg/mL, respectively). TCEO exhibited an IC50 value of 42.58 ± 1.72 μg/mL, indicating moderate inhibitory potency, while quercetin demonstrated a significantly stronger effect with an IC50 of 11.81 ± 0.90 μg/mL. In terms of anti-tyrosinase activity, TCEO showed an IC50 of 85.55 ± 2.51 μg/mL, which is notably more effective than quercetin's IC50 of 242.99 ± 2.67 μg/mL. The study of neuroprotection ability revealed that TCEO exerted a good effect as the inhibition of AChE was 12.36 ± 0.93 mg GALAE/g while that of BChE was 3.59 ± 0.64 mg GALAE/g.

Five undescribed acylated oleanane saponins (1-5), together with five known compounds (6-10) were isolated from the leaves of Camellia hakodae. Their chemical structures were determined by infrared, high-resolution electrospray ionization mass spectrometry, and one-dimensional and two-dimensional nuclear magnetic resonance spectra. Compounds 1-10 significantly inhibited α-glucosidase with IC₅₀ values ranging from 2.11 ± 0.18 to 10.42 ± 0.41 µM.

Plant metabolism encompasses primary and secondary pathways, with secondary metabolism yielding diverse natural products crucial for plant adaptation and ecosystem interactions. Among these products, plant-derived alkaloids are bioactive compounds of significant pharmacological interest, traditionally extracted using conventional solvents known for their environmental and health hazards. Historically, alkaloid extraction relied on acid-base methods, which separate these compounds based on their solubility under different pH conditions. Since the 19th century, extraction techniques have evolved from traditional methods to modern approaches such as supercritical fluid extraction (SFE), microwave-assisted extraction (MAE), ultrasound-assisted extraction (UAE), and the use of ionic liquids (ILs) and deep eutectic solvents (DESs). These advanced methods optimize yield, reduce extraction times, and enhance sustainability by minimizing solvent use and environmental impact. This review explores the evolution of alkaloid extraction methodologies from 2014 to 2023, emphasizing eco-friendly techniques. It discusses the principles and applications of SFE, MAE, UAE, ILs, and DESs in extracting alkaloids from plants, highlighting their pivotal role in modern natural product chemistry. These advancements underscore ongoing efforts to develop efficient and sustainable practices in alkaloid extraction, essential for pharmaceutical and medicinal applications.

Seven previously undescribed manoalide-related sesterterpenes, named cacomalides A-G (1-7), were isolated from the marine sponge Cacosponges sp. collected in the South China Sea. The planar structures and absolute configurations of these compounds are unambiguously determined through comprehensive methods, including HRESIMS analysis, 1D and 2D NMR data analysis, empirial rules of 1H and 13C NMR shifts, DP4+ analysis and ECD spectra. The activity testing of the compounds using zebrafish models and cacomalide A (1) exhibited anti-inflammatory activity.

Glucoraphenin (GRE), a glucosinolate in Raphanus sativus L. seeds and roots, can degrade into isothiocyanates through myrosinase. However, myrosinase in R. sativus roots and seeds is inactivated during cooking, allowing GRE to enter the body in its unmodified form and exert bioactivity. Therefore, investigating the biotransformation of GRE by intestinal flora and the activity of GRE and its metabolites is essential. In this study, fresh fecal samples from healthy SD rats were collected to prepare an intestinal flora culture medium, which was incubated with GRE under anaerobic conditions. GRE metabolite was isolated through Sephadex LH-20 column chromatography, and the structure was identified using HPLC coupled with time-of-flight mass spectrometry (HPLC-TOF/MS) and NMR. Additionally, fluorescence labeling and the number of intestinal peristalsis were employed to assess the effect of GRE and its metabolite on intestinal motility in zebrafish models. Results indicated that GRE can be metabolized in vitro by rat intestinal flora, producing glucoraphasatin (GRH). NMR and MS analysis confirmed GRH's structure as 4-methylthio-3-butenyl glucosinolate. Both GRE and GRH were found to enhance intestinal peristalsis in zebrafish. This study elucidates GRE's metabolic pathway in intestinal flora and suggests that GRE and GRH may be functional components to promote intestinal motility.

Phyllodium pulchellum (L.) Desv., a little-explored medicinal plant of the family Papilionoideae is a deciduous woody shrub with large circular bifoliolate and persistent leafy bracts. The present investigation compares the phytochemical profile of methanolic extracts of P. pulchellum leaf (PPL) and green leafy bract (PPB) using HR-LCMS, and their antioxidant and antimicrobial activities. Interestingly, PPB extract revealed higher contents of phenol and flavonoids and behaves as a potent free radical scavenger in both DPPH (IC 50 = 15.96 ± 0.67 μg/ml) and ABTS (IC50 = 56.18 ± 1.7 μg/ml) assays. Furthermore, PPB shows prominent antimicrobial impact on four different human pathogenic bacterial strains. From in silico investigation, it is evident that the methanolic extracts of PPB and PPL have a positive correlation with antibacterial activity. Methanolic PPL and PPB extracts yielded 55 chemical components, including many novel and unidentified phyto-compounds. Molecular docking approach is adopted to examine the antibacterial qualities of isolated phytometabolites, which offers untapped therapeutic potential of these compounds.

A rare tri-nor-non-paspaline indole diterpenoid (penpaxin A, 1), a new 1,3-dioxolane derivative (penpaxin B, 9), and 19 known compounds (2-8 and 10-21), were isolated from the deep-sea-derived Penicillium paxilli MCCC 3A01133. The structures of the new compounds were established by detailed analyses of the NMR, HRESIMS, and ORD data. 3-Deoxo-4b-deoxypaxilline (5) and paspaline (7) exhibited potent inhibition on RSL3 induced ferroptosis with the EC50 values of 2.88 and 0.21 μM, respectively.

Grounded on the significance of pyrimidines as antibacterial, anticancer, anti-viral, and antioxidant activities and in continuation of our work on pyrimidines as anti-inflammatory and anti-viral agents, here reporting the synthesis of pyrimidine analogs 3 (a-c) and 4 (a, b). The structure of purified compounds was confirmed using spectral techniques such as IR, NMR, and Mass spectra. These compounds were docked with horse heart cytochrome c (1hrc) and the SARS-CoV-2 enzyme (7t9l) to find their binding interaction with the mentioned proteins. Further, druglike properties of potent compounds were studied using SWISS ADME. Among the synthesized compounds, molecular docking studies of 3b and 4a have shown binding affinities of -8.9 kcal/mol and -9.0 kcal/mol for 1hrc higher than bioactive small molecule embelin which has a binding affinity of -7.4 kcal/mol. For the SARS-CoV-2 enzyme (7t9l), the binding affinity of 3b and 4b were -7.4 kcal/mol and -7.2 kcal/mol compared to the pyrazole compound, has a binding affinity of -6.3 kcal/mol. Based on the results, compounds were further screened for antioxidant potential using the DPPH method. However, the antioxidant activity of these two compounds is comparable to that of embelin and pyrazole analog.

Chronic inflammation can lead to various diseases, including gastric ulcers, highlighting the need for effective therapeutic strategies. The traditional use of Chamaerops humilis in Moroccan folk medicine for treating gastrointestinal disorders underscores its potential as a valuable natural remedy. This study rigorously evaluates the anti-inflammatory and gastroprotective effects of the aqueous extract of Chamaerops humilis (AECH) through a series of well-established animal models, including carrageenan-induced paw edema, xylene-induced ear edema, and ethanol/HCl-induced gastric ulcers. The results reveal that AECH significantly reduces inflammation and ulcer severity in a dose-dependent manner, demonstrating potent efficacy in decreasing paw and ear edema while markedly mitigating ulceration induced by ethanol/HCl exposure. Notably, AECH achieved up to 100% inhibition of ulcer lesions at higher doses. These findings not only validate the traditional applications of Chamaerops humilis but also highlight its promising role as a natural therapeutic agent for managing inflammatory conditions and gastric ulcers.

Background: Cheilocostus speciosus (J. Koenig) C. Specht, commonly known as "Crepe-ginger", is a traditional plant with edible flowers utilized in folk medicine. This study employs crepe-ginger flowers to evaluate their role in boosting liver immunity, hepatoprotective actions through oxidative stress management.

Methods: Cheilocostus speciosus flower's methanolic extract (CSF-ME) was subjected to In-vitro anti-oxidant effects were evaluated using DPPH and ABTS and in-vivo by catalase (CAT) assays which ameliorated CCl4-induced hepatic injury evident by histopathological analysis. The chemical assay was evaluated via phytochemical screening and GC-MS/MS analysis followed by in-silico studies.

Results: The antioxidant assay DPPH (IC50 =179.36 µg/ml) and ABTS (IC50 = 198.27 µg/ml) showed remarkable scavenging activity. Hepatotoxicity experiments demonstrated that CSF-ME improved liver function by positively regulating AST, ALT, ALP, bilirubin, creatinine, LDL, CHO, TG, HDL, and catalase levels. Besides, histopathological analysis revealed normal hepatocyte integrity and microstructures after treatment. Besides, phytochemical screening revealed prospective phytochemical groups while GC-MS/MS analysis recognized forty compounds resulting in auspicious outcomes employing computer-aided studies.

Conclusion: The findings indicated that the CSF-ME possesses promising hepatoprotective,   and antioxidant prospects which demand further extensive research to develop novel lead compounds from this natural source.