Planta medica最新文献

Sinopodophyllum hexandrum ("Taoerqi") is a traditional Tibetan medicine used for treating inflammation and arthralgia, but its therapeutic basis against rheumatoid arthritis (RA) remains unclear. This study aimed to identify its active anti-RA fraction, analyse its chemical composition, and explore its mechanisms of action. Using a CFA-induced arthritis rat model, the dichloromethane fraction of S. hexandrum (SHD) was evaluated for anti-RA activity. UHPLC-Q-TOF-MS/MS identified 57 compounds, mainly prenylated flavonoids and arylnaphthalene lignans. Network pharmacology predicted their targets, and in vitro assays on TNF-α-induced fibroblast-like synoviocytes confirmed the anti-RA effects of 15 isolates. Enzyme inhibition, molecular docking, surface plasmon resonance, and Western blot validated their interactions with TNF-α and JAK1. Oral administration of SHD significantly reduced paw swelling and neutrophil infiltration in RA rats. These findings suggest that prenylated flavonoids and arylnaphthalene lignans are key active components exerting anti-RA effects, respectively, via TNF-α and JAK1 inhibition, highlighting their potential for further drug development.

Diabetic retinopathy (DR) is a leading cause of blindness, and its pathogenesis is strongly linked to the activation of aldose reductase (AR) under hyperglycemic conditions. Developing effective AR inhibitors (ARIs), particularly from natural sources, remains a critical therapeutic goal. This study investigated the AR inhibitory potential of an 80% ethanol extract from the leaves of Aster tataricus. Using UPLC-Q-Orbitrap-MS, we identified 11 major compounds, with caffeoylquinic acids (CQAs) being predominant. In vitro assays on rat lens aldose reductase (RLAR) revealed that di-caffeoylquinic acids (di-CQAs), particularly 3,5-di-O-caffeoylquinic acid (3,5-DCQA; IC₅₀ = 0.31 µM), were potent noncompetitive inhibitors. Molecular docking simulations provided insights into their binding modes within the enzyme. The therapeutic relevance of these findings was confirmed in vivo using a larval zebrafish model of hyperglycemia, where both the A. tataricus extract and its constituent CQAs significantly suppressed hyaloid-retinal vessel dilation without inducing toxicity. Quantitative HPLC analysis confirmed that 3,5-DCQA was the most abundant di-CQA in the extract. These findings establish the CQA constituents of A. tataricus leaves as promising natural product leads for developing therapeutics to manage early-stage diabetic retinopathy.

Periodontitis is a common chronic inflammatory disease that leads to the progressive destruction of periodontal tissues. Traditional treatments focus on mechanical debridement; however, antioxidants are increasingly being considered as adjuvant therapies to improve clinical outcomes. Mangosteen (Garcinia mangostana L.), a tropical fruit and chemically characterized natural source of xanthones, exhibits potent antioxidant, anti-inflammatory, and antimicrobial properties, making it a promising candidate in phytotherapeutic periodontal interventions.This systematic review aimed to assess the clinical and biochemical effects of mangosteen-based treatments in patients with periodontitis, compared to placebo or conventional therapies.Following PRISMA guidelines, a comprehensive search was conducted in PubMed, Web of Science, and Scopus. Eligible studies included randomized controlled trials, cohort studies, and clinical trials that evaluated the effects of mangosteen on periodontal parameters-probing pocket depth (PPD), plaque index (PI), gingival index (GI), clinical attachment level (CAL), and bleeding on probing (BOP)-as well as biochemical markers such as IL-6, TNF-α, MMP-8, MMP-9, total antioxidant capacity (TAOC), and oxidative stress indicators.Ten studies met the inclusion criteria, involving 422 patients. The use of 4% mangosteen gel as an adjuvant to scaling and root planing (SRP) showed significant clinical improvements in PPD, GI, CAL, and BOP. Biochemically, reductions in IL-6 and MMP-9 and increased TAOC were observed. However, heterogeneity in formulations and methodologies limited comparability.

Linderae Radix, a traditional Chinese medicine known for its anti-inflammatory, antirheumatic, and analgesic effects, contains norisoboldine (NOR) as its primary bioactive component. NOR exhibits significant anti-inflammatory effects in preclinical studies, particularly in rheumatoid arthritis and inflammatory bowel disease. Despite the various pharmacological activity of NOR, its metabolism and biotransformation patterns in vivo have yet to be elucidated. This study aimed to systematically elucidate the in vivo metabolic pathways of NOR, the excretion patterns of its metabolites, and the primary metabolic enzyme subtypes involved. Biosamples were collected from rats following oral administration of NOR (30 mg/kg). UPLC-Q-TOF-MS/MS was used to identify NOR metabolites in plasma, tissues, and excreta. Differences in the distribution of metabolites across excretion pathways were compared. Chemical inhibition assays and human recombinant enzyme experiments were conducted to determine the key cytochrome P450 (CYP450) enzyme subtypes involved. A total of 14 metabolites were identified, including 8 phase I metabolites and 6 phase II conjugates; the major metabolic reactions were hydrolysis, glucuronidation, sulfation, and dehydrogenation. The glycosylated conjugates (M13 - M15) predominantly underwent renal excretion via urine, whereas the hydrophobic metabolites (M2 - M9) were primarily eliminated through fecal routes due to limited aqueous solubility. The identification of CYP450 enzyme subtypes indicated that CYP3A1/2 and CYP2C11 were the key functional subtypes mediating NOR biotransformation. This study provides the first comprehensive characterization of NOR metabolism, demonstrating that CYP3A1/2 and CYP2C11 catalyze its conversion into 14 metabolites. These findings provide a theoretical basis for the clinical development of NOR and metabolic research on similar compounds.

There is an urgent need for new naturally occurring and/or naturally derived chemical structures for drug development. The biotransformation of two bioactive guaiane-type sesquiterpene lactones, ludartin and estafietin, by filamentous fungi of the genera Aspergillus and Penicillium and by extremophile bacteria of the genera Rhodococcus, Acinetobacter, Streptomyces, and Citricoccus led to the isolation of three new and four known derivatives. The structures were determined based on data obtained from HRESIMS and 1D/2D NMR spectroscopy. The predominant reactions from both eukaryotic and prokaryotic biocatalysts were stereoselective epoxide opening and chemical and regio- and stereoselective double bond reduction, though the fungi were more efficient than the bacteria. Substrates and six selected metabolites were subjected to in vitro evaluation for antiproliferative effects against six human solid tumor cell lines. The derivative 3α,4β-dihydroxy-estafietin showed significant activity against HBL-100, HeLa, and SW1573 cell lines, justifying a more specific, in-depth evaluation of its scope as an anticancer candidate molecule.

Genista, a genus in the Fabaceae family mainly found in the Mediterranean, includes 25 species in Algeria where 11 are native. Locally, these species are used medicinally to treat gastrointestinal disorders, hyperglycemia, and respiratory infections and as diuretics. This systematic review investigates the phytochemical diversity and pharmacological potential of the Algerian Genista species. A comprehensive literature search was conducted in ScienceDirect, Scopus, Web of Science, PubMed, and Google Scholar up to December 2024, with no start date restrictions. The inclusion criteria focused on studies involving Genista species collected from Algeria that investigated the identification and/or quantification of specific phytochemical profiles and/or pharmacological activities, using extracts, residues, fractions, or essential oils. Thirty-two studies met the criteria, covering nine Genista species and identifying 132 compounds across major classes such as phenolic acids, flavonoids, terpenoids, alkaloids, saponins, and fatty acids. Total phenolic content (TPC) reached 690.32 mg gallic acid equivalent (GAE)/g, and total flavonoid content (TFC) was up to 318 mg quercetin equivalent (QE)/g. The highest antioxidant activity showed an IC₅₀ of 3.65 µg/mL. Antibacterial effects were strongest against Staphylococcus aureus, with a 19 mm inhibition zone and minimum inhibitory concentration (MIC) values as low as 10 µg/mL. Hepatoprotective effects showed over 80% inhibition, while cytotoxicity had IC₅₀ values as low as 5 µg/mL. Anti-inflammatory activity reached 96.54%. These findings highlight the diverse pharmacological activities of the genus and its potential for therapeutic applications. However, many bioactivities, such as antidiabetic, antispasmodic, gastroprotective, and immunomodulatory effects, remain underexplored, highlighting the need for further rigorous research.

Herbal medicinal products (HMPs) prepared from the fruit of Silybum marianum are mainly used in the treatment of liver diseases and dyspeptic symptoms. Despite its long-standing use and good clinical safety profile, the safety assessment of such HMPs requires special attention to toxicological aspects that are difficult to detect clinically, especially genotoxic effects. The genotoxic potential of certain S. marianum extracts has been evaluated previously; however, some in vitro assays gave inconsistent results, which is why an EU list entry was not recommended by the Herbal Medicinal Product Committee (HMPC) of the European regulatory agency EMA. To provide a more comprehensive dataset for the evaluation of the genotoxic potential, six dry extracts covering the entire polarity range of extraction solvents were chosen in accordance with the "bracketing and matrixing" approach recommended by the HMPC. These extracts were subjected to the bacterial reverse mutation test, as specified in the OECD test guideline 471, which was performed both as a pre-incubation and plate incorporation assay. When testing up to 5 mg per plate or up to the solubility or cytotoxicity limits, none of the extracts showed signs of mutagenicity, suggesting that extracts of S. marianum fruit have no genotoxic potential. Within reasonable limits, these results may be extrapolated to other extracts based on the aforementioned "bracketing and matrixing" approach.

Cardiovascular diseases are the leading causes of deaths worldwide. Complementary therapies, such as medicinal plants, have become increasingly common among treatment options. We propose to investigate the cardioprotective effects of the ethanol-soluble fraction obtained from the aerial parts of Baccharis milleflora in hypertensive rats. Cladodes of B. milleflora were collected, and the aqueous extract was obtained by infusion. The infusion was then treated with ethanol, resulting in the ethanol-soluble fraction of B. milleflora, which was analyzed by LC-DAD-MS. The MS and MS/MS data obtained from the ethanol-soluble fraction of B. milleflora was submitted to the Global Natural Products Social Molecular Networking platform to generate the molecular network, and three main clusters were detected. Wistar-Kyoto and spontaneously hypertensive rats were divided into different experimental groups, including naïve, control (vehicle), hydrochlorothiazide (25 mg/kg), and ethanol-soluble fraction of B. milleflora (30, 100, and 300 mg/kg). The treatment lasted for 28 days. At the end of the treatment, the animals underwent evaluation of renal function, electrocardiographic profile, blood pressure, mesenteric vascular reactivity, serum biochemical parameters, and histopathological analysis. The molecular pathways involved in pharmacological activity were also investigated. After 28 days, animals treated with ethanol-soluble fraction of B. milleflora 30 mg/kg showed a significant antioxidant, diuretic, and antihypertensive response, as well as reversed endothelial dysfunction and left ventricular hypertrophy induced by hypertension. Treatment with a non-selective NO synthase inhibitor, cGMP inhibitor, or non-selective K+ channel blocker suppressed the antihypertensive effects of ethanol-soluble fraction of B. milleflora. Our findings showed that B. milleflora is a species with cardioprotective activity when administered for a prolonged period to hypertensive rats.

Radiation therapy (RT) remains a fundament of cancer treatment, yet its effectiveness is often hindered by normal tissue toxicity and radiation-induced fibrosis. Recent research has highlighted the promise of bioactive-phytochemicals in enhancing the therapeutic index of RT-sensitizing tumor cells to radiation while safeguarding healthy tissues. This reflects a growing interest in integrating natural compounds with conventional cancer therapies to achieve synergistic effects. To summarize recent advances, identify the research gaps, and evaluate future directions, a comprehensive review was conducted using data from the NCBI and PubChem databases, focusing on preclinical and clinical studies exploring the role of phytochemicals in cancer radiotherapy. The findings stated that the phytochemicals such as curcumin, resveratrol, quercetin, genistein, and EGCG have been shown to sensitize cancer cells to radiation by amplifying DNA damage, promoting apoptosis, and inhibiting key signaling pathways including PI3K/Akt, ATM, and NF-κB. Simultaneously, these compounds exhibit protective effects on normal tissues by activating antioxidant responses (e.g., Nrf2/ARE), reducing oxidative stress, and alleviating radiation-induced fibrosis through modulation of CTGF and TGF-β pathways. Emerging agents like astilbin, puerarin, and isorhamnetin have also demonstrated notable radiosensitizing and antifibrotic potential. However, challenges such as poor bioavailability, dose inconsistencies, and patient-specific variability remain significant barriers to clinical translation. In conclusion, the dual context-dependent actions of phytochemicals emphasize the need for personalized therapeutic strategies, optimized dosing, and advanced delivery systems. Furthermore, integrating nanotechnology may hold particular promise for enhancing the precision and effectiveness of phytochemical-based interventions in radiation oncology.

We present ¹H and ¹³C nuclear magnetic resonance (NMR) chemical shifts for the most common flavonoids, a class of natural products widely present in the plant kingdom. Our data are acquired in three common NMR solvents: methanol d₄, dimethyl sulfoxide d₆, and pyridine d₅ and may be used as a reference for isolated compounds, for detecting flavonoids within mixtures like plant extracts as shown in an example, as reference data for natural product databases, for refined training of prediction software, and for machine learning in resonance assignment and NMR-based structure elucidation. Solvent- and substitution-induced resonance shifts are discussed.