Two new sesquiterpene glycosides, namely 8-hydroxy-dendronobiloside E (1) and dendronobilin D-11-O-β-D-glucopyranoside (2), were successfully extracted from the high-polarity fractions of Dendrobium nobile Lindl. (D. nobile). Comprehensive spectroscopic analyses confirmed their structures as 5β, 8, 12, 15-tetrahydroxycyclocopacamphane 12-O-β-D-glucopyranoside (1), and (2β,3β,5β,12 R*)-2,11,13-trihydroxypicrotoxano-3(15)-lactone-11-O-β-D-glucopyranoside (2). Furthermore, 1 exhibited moderate antiproliferative effects on HeLa cell lines, showing an IC50 of 46.18 µM. Compound 2 was inactive on the proliferation of four types of tumour cells.

Cnidii Fructus (CF) is a Chinese herbal medicine with bioactive immune properties and potential applications in treating ulcerative colitis (UC), but its well-defined bioactive constituents are understudied. The current study aimed to investigate CF's anti-UC bioactivity and elucidate its bioactive constituents via chromatographic analysis, in vitro/in vivo tests, and spectrum-effect analysis. Results showed 10 batches of CF inhibited the inflammatory response induced by lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. High-performance liquid chromatography (HPLC) fingerprint profiles of the 10 batches were established, with 16 common peaks identified. Subsequently, 15 of these peaks (including eight reference-validated compounds) were characterized by ultraperformance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-Q/TOF-MS). Four anti-UC-related compounds were identified via spectrum-effect relationships, namely, diosmin, xanthotoxol, imperatorin, and osthole. Experimental verification confirmed these as key components potentially linked to alleviating inflammatory responses in UC. This study is the first to establish a spectrum-effect relationship for CF's anti-UC effects, identify its critical active constituents, and provide a scientific basis for CF quality control and UC therapeutic development.

Abstract The genus Trollius includes perennial herbaceous plants from the Ranunculaceae family, which holds a prominent place in the realms of food and medicine. This article presents a thorough review of the chemical components isolated and identified from the genus Trollius plants, such as flavonoids, organic acids, volatile oils, and alkaloids, among others. The pharmacological effects of the genus Trollius are also addressed, including its anti-inflammatory, anti-viral, anti-oxidant, and anti-tumor properties. Furthermore, this article collates the medicinal and food application status and prospects of the genus Trollius plants. Clinically, the genus Trollius can be used in Chinese patent medications for ailments such as upper respiratory tract infections, pharyngitis, and tonsillitis. Regarding food, the flowers of the genus Trollius can be fashioned into tea which yields benefits like heat-clearing, detoxifying, yin-nourishing, and internal heat-reducing. Flower extracts can also be natural food additives. Additionally, the genus Trollius plants show potential and promise in the cigarette flavoring and cosmetics industries.

Wine-steaming of Cnidii Fructus is a traditional processing method believed to enhance efficacy, but its mechanistic basis remains unverified. This study integrated HPLC-based chemical profiling with in vivo anti-osteoporotic evaluation in zebrafish to elucidate the effects of processing. Comparative fingerprinting and multicomponent quantification delineated distinct chemical profiles between raw Cnidii Fructus (RCF) and wine-steamed Cnidii Fructus (WCF). Multivariate analysis (PCA, OPLS-DA) pinpointed six differential coumarins. Quantitative analysis confirmed a marked decrease in imperatorin but increases in osthole, alloimperatorin, and xanthotoxol after processing. Critically, the WCF extract demonstrated superior efficacy over RCF in promoting bone mineralization and enhancing alkaline phosphatase (ALP) activity in an osteoporotic zebrafish model. The differential compounds counteracted dexamethasone-induced impairment, with xanthotoxol showing the most potent osteogenic activity, followed by alloimperatorin, diosmin, osthole, and imperatorin. These findings establish that wine-steaming potentiates the anti-osteoporotic activity of WCF by modulating its coumarin composition, providing a chemical and pharmacological rationale for its traditional use and quality control.

Due to issues of high transmissibility, immune evasion, and drug resistance in SARS-CoV-2 variants, there is an urgent need for novel antiviral drugs. Plant-derived flavonoids such as baicalein (EC₅₀ = 4.5 μM) and baicalin (EC₅₀ = 9.0 μM) exhibit broad-spectrum antiviral potential via RNA-dependent RNA polymerase (RdRp) inhibition. Based on this, our study identified two derivatives through pharmacophore alignment between flavonoid scaffolds and the main protease (Mpro) inhibitor 13b: a psoralen-derived lignan (Comp.1) and a novel isoflavone analog (Comp.2), with dual-targeting capability against SARS-CoV-2 RdRp and Mpro. Computational docking elucidated the binding interactions of compounds with RdRp, Mpro, and the L50F/E166V double mutant Mpro. In vitro assays demonstrated that Comp.1 exhibited micromolar-range inhibitory effects on both RdRp (EC₅₀: 25.45 μM) and Mpro (IC₅₀: 125.4 μM), outperforming Comp.2. Both compounds maintained inhibitory activity against the PF07321332-resistant L50F/E166V double mutant Mpro, with IC₅₀ fold-change values of 1.23 and 1.18, respectively, compared to an 8.62-fold reduction for PF07321332. However, ADMET evaluation indicated that although compounds met basic physicochemical criteria (including molecular weight, TPSA, and compliance with Lipinski's Rule of Five), they still presented critical toxicological liabilities, including high genotoxicity risk (Comp.1: 0.838 probability) and CYP3A4 inhibition (>0.97), necessitating extensive structural optimization. This study confirms that flavonoid derivatives represent promising starting points for developing resistance-aware antiviral agents, though their current profiles classify them as early-stage leads requiring substantial optimization.

alpha,alpha '-Diaryl-substituted carbonyl compounds are important organic intermediates. Current methods for their synthesis mainly focus on aryl aldehydes, carboxylic acids, or aromatic alpha-keto acids. These three are employed as benzoyl radical precursors and reacted with para-quinone methides (p-QMs) through 1,6-conjugate addition/ aromatization to yield alpha,alpha '-diaryl-substituted carbonyl compounds. However, the application of this method is limited due to its harsh reaction conditions and the use of precious metals and expensive ligands. Herein, we present a transition metal photocatalyst and additive-free radical cross-coupling of unstrained ketone with p-QMs to explore alternative synthetic methods with mild reaction conditions and new substrate types. A benzoyl group could be introduced at the benzyl position using dihydroquinazolinone derived from unstrained ketone as a benzoyl radical precursor and reacting it with p-QMs under photocatalysis. We utilized cheap and readily available unstrained ketone as acyl radical sources for the 1,6-conjugate addition of p-QMs to obtain alpha,alpha ' diarylated carbonyl compounds. The transformation shows a broad substrate scope. Various substituted aryl ketones can be obtained. To our surprise, when utilizing trifluoroacetophenone and 2,2-difluoroacetophenone as raw materials for reaction with p-QMs, fluorine-containing compounds were acquired instead of alpha,alpha '-diarylsubstituted carbonyl compounds. Notably, dihydroquinazolinones could participate in the next reaction without complicated posttreatment, and the reaction can be applied on a large scale of 9 mmol.

Two novel protoflavonoids, namely 1'S-2',3'-dihydroprotoapigenone (1) and 1'(αS), 4'(αR)-2',3'-dihydroprotoapigenin-4'-O-β-D-glucoside (2), were successfully isolated from Polytrichum commune Hedw. The planar structures were clarified via integrated spectroscopic analysis including 1D and 2D nuclear magnetic resonance. Absolute stereochemistry of compound 1 was definitively assigned utilising calculated electronic circular dichroism (ECD) spectra and optical rotation (OR) data. Furthermore, cytotoxicity evaluations revealed significant antiproliferative activities against human gastric carcinoma HGC-27 cell, compounds ‌1‌ and ‌2‌ exhibiting concentration-dependent growth inhibition, with IC50 values of 37.68 and 41.11 μM, respectively. Both compounds displayed weak effects on SGC-7901 and BGC-823 cells (IC50 > 100 μM), suggesting selective cytotoxicity profiles.‌.

Forsythia suspensa (Thunb.) Vahl, a widely used medicinal plant, especially its fruits in the green fruit stage, is called "Qingqiao" (QQ). However, the effects of climate change on the quality of QQ have not been reported. Therefore, this study conducts an analysis from the perspective of quality distribution and further proposes future stable distribution areas. In this study, F. suspensa distribution data were collected through field surveys and online sources. Phillyrin and forsythoside A contents from selected QQ production areas were then combined and analyzed via the maximum entropy model alongside stepwise regression equations to assess the potential effects of future climate on QQ quality. The results suggest that under various representative concentration pathway (RCP2.6, RCP4.5, and RCP8.5), the QQ quality areas, which are based on the two key contents, decreased. The environmental factors influencing the phillyrin content were significantly negatively correlated with the soil texture classification and precipitation of the driest quarter, whereas the forsythoside A content was significantly negatively correlated with the mean diurnal range and precipitation of the driest quarter. The stable quality regionalization prediction of F. suspensa is expected to remain mainly in North China, with a northward shift of the centroid suggesting a potential response to global warming. These findings provide a foundation for F. suspensa conservation and sustainable development of these resources.

Download This Paper Open PDF in Browser Add Paper to My Library Share: Permalink Using these links will ensure access to this page indefinitely Copy URL Copy DOI

Malus toringoides (Rehd.) Hughes, called "Eseye (Ese)," is a traditional medicinal plant from the Tibet province of China that has proven effective in treating cardiac conditions due to its anti-inflammatory, antioxidative, and antiapoptotic properties. In this study, we explored the underlying protective mechanisms of Ese decoction in isoproterenol (ISO)-induced cardiac fibrosis (CF) and established the fact that treatment with an Ese decoction attenuated tissue injury, decreased the release of IL-1 beta, IL-18, TNF-alpha, and caspase-3, and elevated the Bax/Bcl-2 ratio in CF mice. We also found that with Ese treatment damage to the mitochondrial ultrastructure of myocardium was alleviated, and the level of reactive oxygen species was markedly diminished. Ese inhibited the expression of proteins associated with pyroptosis by the HK1/NLRP3 signaling pathway and also improved CF. Due to the anti-inflammatory, antioxidative, and antiapoptotic characteristics of Ese decoction, we found that Ese protected against ISO-induced CF, by inhibiting inflammation and pyroptosis as mediated by the HK1/NLRP3 signaling pathway. Graphical Abstract Malus toringoides (Rehd.) Hughes decoction alleviates cardiac fibrosis by inhibiting cardiomyocyte inflammation and pyroptosis.

AIMS:Cnidii Fructus (CF) is known for its antibacterial, anti-inflammatory, and antitumor properties, as well as its activities against kidney deficiency and impotence. In this study, we aimed to explore the anti-CRC cancer effect and molecular mechanism of CF via network pharmacology and in vitro antitumor experiments. METHODS:Network pharmacology was used to investigate the anti-CRC mechanism of CF. First, a series of databases was used to screen the active phytochemical targets and anti-CRC core targets. Then, the GO and KEGG pathways were analyzed to predict possible mechanisms. Molecular docking analysis explore core targets-phytochemicals interactions. In vitro antitumor experiments were carried on verifying anti-CRC mechanism of CF. RESULTS:In this study, 20 active ingredient targets and 50 intersecting targets were analyzed by Cytoscape software 3.9.1 to obtain the core genes and phytochemicals. Then, the GO and KEGG pathways of 50 intersecting targets were analyzed to predict possible mechanisms. The results from GO and KEGG indicated that CF has significant antitumor efficacy, which involves many signaling pathways, such as PI3K/AKT and p53. The five core targets and five core phytochemicals were screened for molecular docking to show protein-ligand interactions. According to the results of molecular docking, the compound O-acetylcolumbianetin was selected for the anti- CRC functional verification in vitro. MTT assay showed that O-acetylcolumbianetin significantly inhibited the proliferation of colorectal HCT116 cells in a time- and quantity-dependent manner. O-acetylcolumbianetin can promote the expression of CASP3 protein, induce HCT116 cells apoptosis, thus exert anti-CRC effect. CONCLUSION:This study preliminarily verified the anti-CRC effect and molecular mechanism of CF and provided a reference for Traditional Chinese Medicine anti-tumor subsequent research.

Introduction: This study aimed to clarify the anti-osteoporosis mechanism of Cnidii Fructus (CF) via network pharmacology and experimental verification. Methods: HPLC fingerprints combined with HPLC-Q-TOF-MS/MS analysis confirmed common components (CCS) of CF. Then, network pharmacology was used to investigate the anti-OP mechanism of CF, including potential anti-OP phytochemicals, potential targets, and related signalling pathway. Molecular docking analysis was carried on investigating the protein-ligand interactions. Finally, in vitro experiments were performed to verify anti-OP mechanism of CF. Results: In this study, 17 compounds from CF were identified by HPLC-Q-TOF-MS/MS and HPLC fingerprints and then were further screened key compounds and potential targets by PPI analysis, ingredient-target network and hub network. The key compounds were SCZ10 (Diosmin), SCZ16 (Pabulenol), SCZ6 (Osthenol), SCZ8 (Bergaptol) and SCZ4 (Xanthotoxol). The potential targets were SRC, MAPK1, PIK3CA, AKT1 and HSP90AA1. Molecular docking further analysis indicated that the five key compounds have a good binding affinity with related proteins. CCK8 assays, TRAP staining experiments, and ALP activity assays concluded that osthenol and bergaptol inhibited osteoclast formation and promoted osteoblast bone formation to improve osteoporosis. Conclusion: Based on network pharmacology and in vitro experiments analysis, this study revealed that CF possessed an anti-OP effect, and its potential therapeutic effect may be involved with osthenol and bergaptol from CF.

Seven flavanones, including two new compounds coupled with styryl units, communins C (1) and D (2), as well as five known compounds, were isolated from Polytrichum commune Hedw. The planar structures of all compounds were determined using extensive spectroscopic analysis. The absolute configurations of two new compounds were assigned by comparing experimental ECD with calculated ECD. The cytotoxicity of all isolates against HCT-116, BGC803, MCF7 and PANC-1 cell lines was evaluated. Communin D exhibited significant cytotoxic activity on BGC803 cells with an IC50 value of 9.3 μM.

Bombyx batryticatus is derived from the dried larva of Bombyx mori Linnaeus infected by Beauveria bassiana (Bals.) Vuillant. Raw Bombyx batryticatus should be stir-fried before oral administration due to its irritation to the gastrointestinal tract. Nevertheless, it is still an arduous task to uncover the intrinsic mechanism of Bombyx batryticatus processing. In this study, we collected two types of Bombyx batryticatus, one being stir-fried and the other serving as a control. Then, an informative approach, which integrated matrix-assisted laser desorption/ionization mass spectrometry imaging (MALDI-MSI) with chemometrics analysis, was established to screen processing-associated markers and reveal in situ spatial distribution patterns of protein-related metabolites. After optimization of experimental conditions, 21 ions were initially detected from Bombyx batryticatus, including amino acids and peptides. In addition, 15 differential markers were screened by orthogonal projection to potential structure discriminant analysis (OPLS-DA), which were localized and visualized in the transverse section of Bombyx batryticatus by MSI. Eventually, it can be demonstrated that the stir-frying process reduces toxicity while potentially boosting specific biological activities of Bombyx batryticatus. In summary, the established strategy could not only clarify the chemical transformation of protein-related metabolites from Bombyx batryticatus before and after frying with wheat bran, but also reveal the significance of Chinese medicine processing technology.

Objective To study the inhibitory effects of some flavonoids on the SARS-CoV-2 main protease. Methods Taking Nirmatrelvir as a positive control compound, the inhibitory activities of the flavonoids hesperidin, luteolin, genistein, calycosin, apigenin, phloretin, apigenin-7-glucoside, genistin, genistein-4’-glucopyranoside and hesperidin on the main protease of SARS-CoV-2 were tested using a sandwich-like fluorescence polarization assay（FP） screening model. Results The positive control Nirmatrelvir inhibited 91%, 76% and 70% of the main protease at the concentrations of 100 μM, 50 μM and 25 μM, respectively, while the flavonoids hesperidin, luteolin, genistein, calycosin, apigenin, phloretin, apigenin-7-glucoside, genistein-4’-glucopyranoside and hesperidin did not show any effective inhibition activity against the main protease at the corresponding drug concentrations. Conclusion Flavonoids have pharmacological activities against SARS-CoV-2 at the cellular level, and their mechanism of action is most likely to be the inhibition of SARS-CoV-2 RNA polymerase, rather than the inhibition of the main protease. The experimental data can provide ideas and references for the development of subsequent anti-SARS-CoV-2 drugs.

目的 筛选蛇床子盐炙的最佳炮制工艺参数,为盐蛇床子的质量控制提供实验依据.方法 以6个指标成分(花椒毒酚、花椒毒素、佛手柑内酯、王草酚、欧前胡素和蛇床子素)的质量分数和外观性状得分的综合评分为指标,采用层次分析法(AHP)-指标权重确定方法(CRITIC)复合熵权确定各评价指标的权重系数,在单因素试验结果基础上,应用Box-Behnken响应面法考察盐水用量、炒制温度和炒制时间对盐炙蛇床子炮制工艺的影响,筛选蛇床子最佳盐炙工艺参数.结果 蛇床子最佳盐炙工艺参数为:每30 g蛇床子,加6 mL食盐水,浸润6 h,于112℃炒制11 min,取出,放凉.结论 采用AHP-CRITIC复合熵权法结合Box-Behnken响应面法进行炮制工艺优化,所拟合的模型显著,工艺验证结果合理稳定,可用于蛇床子盐炙最佳工艺的优选,为盐炙蛇床子炮制工艺标准及质量标准的建立提供参考.

Two new benzophenone derivatives (1 and 2), named Pogonatone C and pogonatone D, were isolated from the moss Pogonatum spinulosum. Their structures were elucidated by spectroscopic data analyses. The cytotoxicity of compounds for HepG2, HCT-116, A-549 and PANC-1 cells line was also evaluated by using the MTT method. Pogonatone C (1) displays high cytotoxicity on PANC-1 cell with IC50 value of 9.2 μM.

目的:综述中药蛇床子的炮制概况、化学成分以及药理作用研究进展,为蛇床子不同炮制品的临床合理应用及质量标准研究提供参考依据.方法:借助爱如生古籍库、中国知网、Scifinder等中外文数据库,查阅中药蛇床子的炮制历史沿革、化学成分及药理作用相关文献资料,梳理归纳,并形成综述.结果:古代文献记载的蛇床子炮制方法较多,但现行药品标准多以净制为主;现代研究工艺的研究集中在蛇床子素炮制前后的含量变化;其所含的香豆素类、色原酮类、挥发油类等成分在治疗心血管疾病、抗肿瘤、抗炎、抗骨质疏松、治疗神经性疾病等方面,具有一定药理作用.结论:据记载蛇床子生品有小毒,多外用,但临床也有内服治疗骨质疏松等病症的报道,故不同炮制品的临床应用有待研究;炮制前后的香豆素类成分变化明显,有可能是蛇床子增效减毒的内在机理之一;本综述可为中药蛇床子后续的炮制作用机理、药效物质基础和药理作用研究提供参考.

目的 研究中药废渣生物有机肥对北沙参生长发育、产量及质量的影响.方法 通过观察不同施肥处理T1(生物有机肥)、T2(生物有机肥∶化肥=2∶1)、T3(生物有机肥∶化肥=1∶1)、CK(单施化肥)对北沙参的根长、茎粗、鲜重、干重、折干率、补骨脂素、欧前胡素、异欧前胡素、多糖含量、产量和经济效益的影响,评价生物有机肥对北沙参生长发育、产量及质量的影响.结果 与CK比较,施加中药废渣生物有机肥北沙参的根长分别增加了20.44％、12.58％、8.84％,茎粗分别增大了62.77％、35.11％、15.96％,鲜重分别增加了74.62％、47.11％、25.53％,干重分别增加了87.63％、53.28％、26.01％,折干率分别增加了7.24％、4.02％、0.19％,产量分别增加了31.55％、26.49％、15.29％,经济效益分别增加了65.41％、44.78％、8.13％;T1处理组对北沙参香豆素和多糖含量影响最大,补骨脂素含量较CK增加了0.00115 mg/g,欧前胡素含量较CK增加了0.00071mg/g,异欧前胡素含量较CK增加了0.00075 mg/g,多糖含量较CK增加了9.29％.结论 施加中药废渣生物有机肥不仅可以明显增加北沙参的生理生化指标,同时能显著提高北沙参的产量和经济效益,具有较好的推广应用价值.

Objective: To optimize the processing technology with wine of Cnidii Fructus.Methods: The contents of xanthotoxol, xanthotoxin, bergapten, imperatorin and osthole were simultaneously determined by HPLC;Total coumarin content was determined by UV spectrophotometry.The weight coefficient was calculated by AHP-entropy weight method, and the effects of adding alcohol amount, roasting temperature and roasting time on the quality of wined Cnidii Fructus were investigated by multi-index comprehensive score combined with response surface method.The processing technology of wined Cnidii Fructus was optimized.Results: The optimum wine processing parameters were as follows: adding 6 mL rice wine per 30 g Cnidii Fructus for 1 h, roasting temperature 130 ℃,roasting time 30 min.Three batches of samples were prepared in parallel with the obtained conditions, and the calculated comprehensive scores were 89.66,88.57,88.46,respectively, and the RSD was 0.74%.Conclusion: The optimal processing technology of wined Cnidii Fructus is stable and feasible, and the method for the determination of five components in wined Cnidii Fructus is quickly and reliably.This experiment can provide reference for the processing technology of Cnidii Fructus and the quality control of wined Cnidii Fructus.