Fitoterapia最新文献

Daphnane diterpenoids occurring in plants of the Thymelaeaceae are the focus of natural product drug discovery because of the wide range of their therapeutically biological activities. Considering the limited occurrence in some plants of the Thymelaeaceae, it is imperative to design a strategy for the target isolation of daphnane diterpenoids. In this study, a strategy was developed to filter the data using MZmine, generate the molecular network using the Global Natural Product Social Molecular Network Platform (GNPS), and determine the retention time of target compounds using MS-DIAL. Under the guidance of the approach which integrates the analysis of LC-MS/MS, compounds 1-5, representative diterpenoids from Daphne altaica Pall., were isolated. Their structures were determined through detailed spectroscopic analyses and ECD calculations. The growth-inhibitory activities of the isolated compounds against MCF-7, A549, and HepG2 cell lines was examined. Notably, compound 1 demonstrated the most noticeable cytotoxicity, exhibiting potent growth inhibition activities against A549 and HepG2 cells with IC₅₀ values of 2.89 μM and 5.30 μM, respectively. Further morphological and staining analyses corroborated that compound 1 induced apoptosis in A549 and HepG2 cells, highlighting its potential as a bioactive agent.

Background: Hepatic fibrosis is a wound healing response that leads to excessive deposition of extracellular matrix (ECM) due to sustained liver injury. Hepatic stellate cells (HSCs) are key players in ECM synthesis, with the TGF-β/Smad signaling pathway being central to their activation. Despite advances in understanding the pathogenesis of hepatic fibrosis, effective anti-fibrotic therapies are still lacking.

Methods: This treatise conducts a comprehensive review of the literature on the hepatoprotective effects of natural products, including natural medicine compounds, herbal extracts, and polysaccharides. The focus is on their ability to modulate the TGF-β pathway, which is critical in the activation of HSCs and ECM synthesis in hepatic fibrosis.

Results: The review identifies a variety of natural products that have shown promise in inhibiting the TGF-β/Smad signaling cascade, thereby reducing the activation of HSCs and ECM accumulation. These findings highlight the potential of these natural products as therapeutic agents in the treatment of hepatic fibrosis.

Conclusions: The exploration of natural products as modulators of the TGF-β pathway presents a novel avenue for both clinical and preclinical research into hepatic fibrosis. Further investigation is warranted to fully understand the mechanisms of action and to develop these compounds into effective anti-fibrotic pharmaceuticals.

Genus Acacia comprises around 1500 species. They are widely used to treat inflammation as well as bacterial and fungal infections as they are enriched in phytochemicals, especially phenolics. The aim of this study was to evaluate the antibacterial activity of leaves' methanolic extracts of twelve Acacia species growing in Egypt against Vibrio parahaemolyticus, Salmonella enterica, Listeria monocytogens, Klebsiella pnemoniae, Bacillus aquimaris, Bacillus subtilis, and Escherichia coli. These species are Acacia nilotica (wild and cultivated), Acacia seyal, Acacia auriculiformis, Acacia saligna, Acacia xanthophloea, Acacia tortilis subsp. raddiana (Gabal Elba and Aswan), Acacia tortilis, Acacia laeta (wild and cultivated), and Acacia albida. Furthermore, to study the metabolomic composition and variation among these species using ultra-high-performance liquid chromatography-electrospray ionization quadrupole time of flight mass spectrometry (UHPLC-q-tof-ESI-MS) coupled with multivariate statistical analysis and correlate it to the antibacterial potential. Results showed that Acacia nilotica (AN) has superior antibacterial activity over the other species. In addition, it exhibited a distinct segregation in Principal component analysis (PCA) and partial least square discriminant analysis (PLS-DA). Full profiling of AN using UHPLC-ESI-q-tof-MS revealed 42 phenolics mainly catechins. It was further subjected to bio-guided fractionation and revealed the presence of methyl gallic acid, gallic acid, catechin gallate, and digallate isomers in its most bioactive fraction. These compounds were identical to the compounds annotated as VIPs and were responsible for the segregation of AN in both PCA and PLS-DA analyses. Hence, this study sheds light on the use of chemometrics as an early tool for the detection of bioactive compounds.

Parkinson's disease (PD) is the second most common neurodegenerative disorder in the elderly, currently with no cure. Its mechanisms are not well understood, however α-synuclein protein aggregation plays a central role in the pathogenesis of PD, leading to neurodegeneration. We demonstrated that in a PD model dietary in Caenorhabditis elegans treatment with an extract from the rhizome of Canna coccinea decreased the accumulation of α-synuclein. The extract showed low toxicity to neuro 2a cells and protected them from oxidative damage with H₂O₂ as a model for neurodegeneration. We studied the chemical profile of the extract using liquid chromatography couple to Mass Spectrometry. In order to characterize the herbal extract, we quantified rosmarinic acid as a marker compound and measured its antioxidant activity in vitro. Altogether, apart from its potential as a functional food, Canna coccinea may be an interesting source of secondary metabolites in the development of potential novel anti-neurodegenerative drugs.

Four previously undescribed diterpenoids (2-5) were isolated from the bark of Torreya grandis, along with ten known analogues. The structures of the compounds were elucidated using NMR, HR-ESIMS, and ECD calculation. The cytotoxic effects of the isolated compounds on HCT-116, AsPC-1, and HepG2 cells were evaluated using the MTT assay. Compound 6 exhibited significant cytotoxicity against HepG2 cells. Further experiments revealed that compound 6 could arrest the G2 phase process in HepG2 cells through the JAK2/STAT3 signaling pathway.

The genus Thesium, family Santalaceae, comprises about 350 species, and, although many of them are used as functional food and in traditional medicine, there are limited studies evaluating their pharmacological potential. The present study was designed to evaluate the chemical profile, antioxidant, and enzyme inhibition potential of aerial parts and roots of T. bertramii Azn. Extracts were rich in phenolics: MeOH and aqueous extracts of the aerial parts showed the highest total phenolic and flavonoid contents and the best antioxidant activity in most assays. Ethyl acetate extracts of both organs exerted comparable anti-butyrylcholinesterase activity, while their methanol extracts displayed comparable anti-tyrosinase activity. The highest acetylcholinesterase inhibitory activity was recorded from the root's ethyl acetate extract, while that of the aerial parts revealed the best α-amylase and α-glucosidase inhibitory activity. Chemically, the aerial parts were dominated by quercetin derivatives, feruloylquinic acids, caffeoylquinic acids, and elenolic acid glucoside. Roots showed a lower diversity of compounds with elenolic acid, quercetin glycoside, and kaempferol glycoside as major compounds. Additionally, network pharmacology analyses (KEGG and STRING) identified critical molecular pathways and hub genes, including IL6, TNF, BCL-2, and JUN, indicating the multi-target potential of T. bertramii in cancer and cardiovascular diseases. In conclusion, this study assessed the chemical and biological properties of T. bertramii for the first time, and the obtained results indicated the potential of this species as a valuable source of bioactive molecules for the pharmaceutical, food, and cosmetic industries.

The genus Geum (family Rosaceae) comprises about 70 species, of which several species have been characterized from Eurasia as notably as folk medicines for the treatment of anti-inflammatory, antiseptic, diuretics and astringent. Phytochemical analysis indicated that Geum species produce monoterpenoids, sesquiterpenes, triterpenoids, flavonoids, tannins, phenylpropanoids, and others compounds. Additionally, modern studies have found they possess diverse pharmacological activities such as antioxidant, anti-inflammatory, neuroprotective, antimicrobial, anti-diabetic, cardiovascular, and antitumor effects. Regardless of the remarkable medical potential of Geum extracts, clinical studies are limited and need to be performed to produce safer and less expensive plant-based drugs. This literature review aims to provide a comprehensive overview of Geum species, covering their traditional uses, phytochemistry, and pharmacological activities, and to summarize the current research status to better understand the application value of Geum plants in modern phytotherapy.

Background: The medicinal folk plant Tithonia diversifolia A. Gray has traditionally been used to treat hepatitis and liver cancer. However, the anti-fibrotic effect of this plant extract and its main active substances remain unclear.

Objective: This study aims to elucidate the anti-fibrotic effect of T. diversifolia ethanol extract, identify the main active substances, and explore their possible molecular mechanisms.

Methods: Firstly, carbon tetrachloride (CCl₄) was injected intraperitoneally to induce liver fibrosis in mice to investigate the protective effect of T. diversifolia ethanol extract. Then, thirty compounds in this extract were identified through liquid chromatography-mass spectrometry (LC-MS/MS) analysis, column chromatography, and spectroscopic analysis. In addition, the anti-fibrotic effect of sesquiterpene lactone compounds were investigated on TGF-β-induced hepatic stellate cell activation.

Results: The T. diversifolia ethanol extract significantly inhibits symptoms of carbon tetrachloride-induced liver fibrosis and the collagen deposition in pathological tissues by suppressing the protein expression of various pro-fibrotic factors. A comprehensive profile of thirty-one compounds was established, including nine sesquiterpenes, six phenolic acids, six fatty acids, five phenylpropanoids, and three flavonoids. Notably, one previously unreported sesquiterpene lactone, namely 1β-ethoxydiversifolin 3-O-methyl ether (1), together with twenty-nine known compounds were obatined. Sesquiterpene Tagitinin C shows significant anti-fibrotic effects on TGFβ1-induced HSC-T6 activation by inducing cell apoptosis and regulating the TGF-β1/Smad pathway.

Conclusion: The above results indicate that the T. diversifolia extract can effectively alleviate liver fibrosis, with sesquiterpene lactones being a major component. In the future, the germacranolides-type of sesquiterpene lactone Tagitinin C can be developed as a precursor compound for anti-fibrotic therapy.

Seven benzylisoquinoline alkaloids, including three new (1-3) and four known compounds (4-7), were isolated from the embryo of Nelumbo nucifera (Plumula Nelumbinis). Their structures were elucidated by UV, IR, HRESIMS, 1D and 2D NMR, and ECD spectra, as well as optical rotations. All compounds were tested for the antioxidant activity. Compounds 1-7 prevented Fe²⁺ induced lipid peroxidation in mouse liver microsomes, with the inhibitory rates of 76.1, 75.7, 60.0, 82.9, 75.5, 83.8 and 85.3 %, respectively.