Five undescribed compounds were isolated from a 50% ethanol extract of the whole herb of Gerbera delavayi Franch., including one unprecedented skeleton compound comprised of 5-methylcoumarin meroterpenoid (1), two 5-methylcoumarin derivatives (2 and 3), one lignan (4), and one benzofuran derivative (5). Their structures and absolute configurations were characterized by comprehensive analysis of spectroscopic data, including 1D NMR, 2D NMR, IR, UV spectra, HRESIMS data, and single-crystal X-ray diffraction. Meanwhile, a plausible biosynthetic pathway for compound 1 was proposed. The anti-inflammatory activities of all isolated compounds were evaluated by measuring their inhibitory effects on NO production in LPS-stimulated RAW 264.7 mouse monocyte-macrophages. Among these compounds, 1, 3, and 4 exhibited significant anti-inflammatory activity on NO generation, with IC50 values of 10.61 ± 0.40, 22.79 ± 0.38, and 1.80 ± 0.41 μM, respectively.
Twenty-one compounds were isolated and identified from the 80%ethanol extract of Paeoniae Radix Rubra by various chromatographic techniques such as D101 macroporous resin,C18 reversed-phase silica gel,and gel chromatography,combined with modern spectroscopic techniques including infrared spectroscopy(IR),ultraviolet(UV),mass spectrometry(MS),and nuclear magnetic resonance(NMR).These compounds were 3-formyl-5-hydroxy-6-methyl-1H-indole-1-butyric acid(1),3-hydroxymethyl-5-methyl-2,3-dihydrobenzofuran(2),paeoniflorin(3),5-hydroxy-6-methyl-1H-indole-3-carbaldehyde(4),5-hydroxy-3S-hydroxymethyl-6-methyl-2,3-dihydrobenzofuran(5),paeoveitol C(6),galloylpaeoniflorin(7),benzoylpaeoniflorin(8),4-O-galloylpaeoniflorin(9),1-borneol 6-O-[β-D-apiofuranosyl-(1→6)]-β-D-glucopyranoside(10),paeonidanin(11),paeonidanin E(12),paeonidanin B(13),palbinone(14),23-hydroxybetulinic acid(15),hederagenin(16),N-methylhydroxylamine(17),(5Z,9Z)-17-methylnonadeca-5,9-dienoate(18),3,3',4'-tri-O-methylellagic acid(19),β-sitosterylglucoside-6'-octadecanoate(20),and trilinolein(21).Among them,compound 1 was a new compound,and compounds 10 and 17-21 were isolated from the Paeoniae genus for the first time.All the compounds were tested for their anticoagulant activity through three coagulation function indicators:activated partial thromboplastin time(APTT),thrombin time(TT),and prothrombin time(PT).Compounds 1 and 7 showed excellent anticoagulant activity,which was comparable to that of the positive control sodium heparin.Compounds 2,3,5,6,8-13,15,and 19 exhibited good anticoagulant activity,while compounds 4 and 21 demonstrated moderate anticoagulant activity.
Moringa oleifera seed husks, the traditional non-medicinal parts of M. oleifera seed, are usually discarded or burned, which pollute the environment and waste resources. In an unprecedented study, the antioxidant and α-glucosidase inhibitory activities of crude extracts from the medicinal and by-product parts of M. oleifera seed were compared and evaluated. The results showed that the scavenging ability of M. oleifera seed husks on 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) free radicals, and the α-glucosidase inhibitory activities were significantly stronger than that of kernels. 24 phenolic compounds, including 1 new compound, 2 new natural products and 21 known phenolic compounds, were isolated from M. oleifera seed husks. Among of them, erythro-guaiacylg-lycerol (23) and threo-guaia-cylglycerol (24) exhibited significant antioxidant activity, and their half-maximal inhibitory concentration (IC50) values for scavenging DPPH and ABTS radicals were 32.39, 7.16 µg/mL and 24.24, 7.35 µg/mL, respectively. 2-(4-hydroxy-3-(4-hydroxybenzyl) phenyl) acetamide (1), p-hydroxybenzoic acid (11), 4,4-dihydroxydiphenylmethane (16) and 4-hydroxy-3-[(4-hydroxyphenyl) methyl] benzeneacetonitrile (17) showed strong α-glucosidase inhibitory activity, with IC50 values of 16.55, 17.45, 25.12, and 14.10 µg/mL, respectively. The structure-activity relationship (SAR) study revealed the importance of the presence of 1,2,4-trisubstituted phenol structural fragment in enhancing the antioxidant and α-glucosidase inhibitory activities of the compounds. Compounds with such structural fragment may be developed into potential hypoglycemic drugs. According to the results, M. oleifera seed husks could be an alternative to develop novel drugs, functional foods and nutritional health products with hypoglycemic effects. The findings also indicate that M. oleifera seed by-products have the potential to be converted into value-added products, thereby contributing to sustainable waste management and environmental protection.
Gerbera piloselloides Herba (GP) is a traditional herb commonly used for asthma in China. Our previous studies have identified a key group of active components-arbutin, marmesin, and luteolin-that demonstrate significant efficacy in asthma treatment, showing promising therapeutic potential. Although we previously investigated the comparative pharmacokinetics (only absorption process) of 11 main components of GP in both control and asthmatic mice, the pharmacokinetics of these 3 active compounds, including absorption, metabolism, and excretion in rats, remain unclear. This study develops an efficient liquid chromatography (LC) method to explore these pharmacokinetic processes. Ultrahigh-performance LC coupled with triple quadrupole mass spectrometry (UPLC-MS/MS) and Q-Exactive hybrid quadrupole-orbitrap high-resolution accurate MS (UHPLC-Q-Exactive Plus HRMS) were employed to detect these compounds and their metabolites in biological samples. The results indicate that arbutin is rapidly absorbed, with a Tmax of 0.22 +/- 0.15 h and a Cmax of 35 477 +/- 6743 mu g/L, and its cumulative urinary excretion rate is 60.136% +/- 9.539%. Marmesin achieves a Cmax of 503 225 +/- 89 848 mu g/L and a T1/2 of 3.58 +/- 0.075 h, with significantly lower cumulative excretion over 36 h compared to the administered dose. Luteolin demonstrates a characteristic double-peak pharmacokinetic profile, with a Cmax of 22.24 +/- 4.84 ng/L. Notably, arbutin is primarily excreted via urine, whereas marmesin and luteolin are predominantly excreted through bile and urine, respectively. A total of 7 metabolites of arbutin, 13 metabolites of luteolin, and 22 metabolites of marmesin were identified in plasma, feces, urine, and bile, which involves such metabolic pathways as oxidation, reduction, methylation, sulfation, acetylation, hydration, glucuronidation, and glutathione conjugation. This establishes a stable, efficient analytical method for assessing the pharmacokinetic profiles of these key GP components, providing valuable insights for their further therapeutic development.
Two new abietane diterpenoids, massonianene A (1) and massonianene B (2), were isolated from the extract of Pinus massoniana. Their structures were elucidated based on HR-ESI-MS, IR, UV, NMR, ECD and X-ray diffraction analysis. Compound 2 exhibited significant inhibitory effect against LPS-induced NO production in RAW 264.7 cells, with an IC50 value of 7.00 ± 1.73 μM.
Alzheimer's disease (AD) pathogenesis remains poorly understood, with emerging evidence highlighting the role of metal ions, particularly Cu+, and their respective valence states in neurodegeneration. This study introduces the proprietary fluorescent probe NRNM, designed for the selective detection of Cu+ in the brain. Utilizing an "AND" logic gate strategy, the probe exhibits robust fluorescence exclusively in pathological environments characterized by lipid accumulation, allowing for precise identification of Cu+ imbalance. Spectral analysis confirmed its stability and selectivity in vitro, with a detection limit as low as 55 nM. In vivo assessments demonstrated its capacity to cross the blood-brain barrier (BBB) and bind to Cu+ in AD mouse models. Notably, a significant correlation between Cu+ levels, lipid accumulation, and amyloid plaque formation was observed across different age groups. Fluorescence lifetime imaging microscopy (FLIM) revealed distinct spatiotemporal distributions of Cu+ during AD progression, with the average fluorescence lifetime increasing from 1.80 ns at the early stage to 2.67 ns at the late stage and Cu+ was found to be heterogeneously distributed in different brain regions, indicating a dynamic interaction between Cu+ and neurodegenerative processes. Overall, this study proposes that the developed probe provides a valuable tool for elucidating the role of Cu+ in AD.
The chemical investigation of the Potentilla kleiniana led to the isolation of a new seco-nortriterpene, kleinianene (1), and eight known compounds including one phenylpropanoid glycoside (2), one lignan glycoside (3), one ellagic acid derivative (4), one phenylacetic acid derivative (5), one C21-steroid (6), one polyhydroxyalkylpyrazine derivative (7), one quinoline derivative (8), and one phenolic acid (9). Their structures were elucidated by extensive spectroscopic methods and comparison with literature data. Moreover, the antiinflammatory activity of 1 was evaluated by measuring its inhibitory effect on NO production in LPSstimulated RAW 264.7 macrophages. The obtained result showed a moderate inhibition effect of NO release with IC50 value of 26.88 +/- 0.36 mu M. All the above compounds were isolated from P. kleiniana for the first time and five compounds (2 and 5-8) were first reported from the family Rosaceae. Furthermore, the chemotaxonomic significance of the isolated compounds was discussed briefly.
Pancreatic ductal adenocarcinoma (PDAC) is a clinically challenging cancer because of the difficulty in diagnosis and its resistance to chemotherapy. Focal adhesion kinase (FAK) is found overexpressed in PDAC, and targeting FAK has been proved to impede the progress of PDAC. However, most of FAK inhibitors were reported to bind with FAK in a DFG-in conformation, leading to a limited anti-tumor effect in clinical studies. Herein, to develop FAK inhibitors targeting the inactive DFG-out conformation, a series of large aromatic rings were selected to improve the interaction with Phe565 of the DFG motif. Compound 26 was designed to effectively inhibit FAK and the proliferation of PANC-1 cells with IC50 of 50.94 nM and 0.15 mu M, respectively. Besides, compound 26 was proved to strongly suppress the proliferation, colony formation, migration, and invasion in FAK-overexpressing PDAC cells. This inhibitor was confirmed to induce the apoptosis and G2/M arrest in PANC-1 cells through the suppression of FAK/PI3K/Akt signal pathway. Meanwhile, compound 26 was found to simultaneously inhibit FAK with DFG-out conformation and JAK3/Aurora B (IC50 of 9.99 nM and 0.49 nM, respectively). In vivo, compound 26 effectively inhibited the tumorigenesis and metastasis of PDAC with desirable biosafety. Overall, these results suggested that compound 26 was a promising candidate for the treatment of PDAC.
Phytochemical investigation of the whole plant of Gerbera delavayi afforded four new glycosides including three coumarin glycosides, Gerbelavinside A (1), Gerbelavinside B (2) and Gerbelavinside C (3) and one acetophenone glycoside, Gerbelavinside F (4). The structures of isolated compounds were elucidated by analysis of 1D and 2D NMR, HR-ESI-MS, acid hydrolysis, as well as comparing with the literature. The isolated compounds were examined the effects of nitric oxide (NO) production inhibition in lipopolysaccharide (LPS)-induced RAW264.7 macrophage cells, and Gerbelavinside C presented a certain inhibitory activity.
Chemical constituents of 70% ethanol extract of Alangium chinense subsp. pauciflorum were investigated. The 70% ethanol extract of A. chinense subsp. pauciflorum was isolated and purified by D-101 macroporous resins, silica gel, Sephadex LH-20 and other methods. As a result, nineteen compounds were isolated and identified as 4-cyclohexene-1α,2α,3α-triol-1-O-β-D-glucoside(1), 1β,4α,6α,13-tetrahydroxy-eudesm-11(12)-ene(2), sucrose(3), 1'-O-benzyl-α-L-rhamnopyranosyl-(1″→6')-β-D-glucopyranoside(4), bis(2-ethylhexyl)benzene-1,2-dicarboxylate(5),(Z)-10-heneicosenoic acid(6), di-O-methylcrenati(7), methyl-α-D-fructofuranoside(8), β-daucosterol(9), syringic acid(10), vanillicacid(11), octacosanol(12), isoarborinol(13), 2,7-dihydroxy-6-methyl-4-(1-methylethyl)-1-naphthalenecarboxylate(14),vanillin(15), coniferyl aldehyde(16), 9(11)-dehydroergosterolperoxide(17), 5α,8α-epidioxy-(22E,24R)-ergosta-6,22-dien-3β-ol(18), β-sitosterol(19), respectively. Compounds 1 and 2 were new compounds, compounds 5-11, 13, 15-18 were isolated from Alangium for the first time.The anti-inflammatory activity of compourd 1 was determinded by the LPS-induced RAW264.7 macrophage inflammation model. The results showed that the new compound 1 has a certain inhibitory effect on LPS-induced NO production of RAW264.7 cells, and the inhibitory rate was 54.57%.
As an important antiviral target, HIV-1 integrase plays a key role in the viral life cycle, and five integrase strand transfer inhibitors (INSTIs) have been approved for the treatment of HIV-1 infections so far. However, similar to other clinically used antiviral drugs, resistance-causing mutations have appeared, which have impaired the efficacy of INSTIs. In the current study, to identify novel integrase inhibitors, a set of molecular docking-based virtual screenings were performed, and indole-2-carboxylic acid was developed as a potent INSTI scaffold. Indole-2-carboxylic acid derivative 3 was proved to effectively inhibit the strand transfer of HIV-1 integrase, and binding conformation analysis showed that the indole core and C2 carboxyl group obviously chelated the two Mg2+ ions within the active site of integrase. Further structural optimizations on compound 3 provided the derivative 20a, which markedly increased the integrase inhibitory effect, with an IC50 value of 0.13 μM. Binding mode analysis revealed that the introduction of a long branch on C3 of the indole core improved the interaction with the hydrophobic cavity near the active site of integrase, indicating that indole-2-carboxylic acid is a promising scaffold for the development of integrase inhibitors.
Selenium nanoparticles (SeNPs), as a potential cancer therapeutic agent, have attracted extensive attention due to their high anticancer activity and low toxicity. Polysaccharides could be the modifiers and stabilizers to improve the stability and dispersibility of SeNPs in aqueous solution. This study aimed to investigate the physicochemical characterization, stability, and anti-pancreatic cancer cell activities of SeNPs stabilized by a heteroxylan PVP3-1 extracted from the clusters of Prunella vulgaris Linn. Our results showed that PVP3-1 with Mw of 154 kDa was composed of →4)-β-D-Xylp(1→, →2, 4)-β-D-Xylp(1→, t-α-L-Araf(1→ and 4-MeO-α-D-GlcpA(1→. Red, zero-valent, and uniform spherical SeNPs with an average diameter of about 60 nm and high stability in aqueous solution were constructed successfully by polysaccharide PVP3-1. Anti-pancreatic cancer cell activity assays showed that PVP3-1-SeNPs could inhibit the proliferation and migration of pancreatic cancer cells in vitro. Furthermore, PVP3-1-SeNPs induced apoptosis and autophagy of pancreatic cancer cells through inhibiting mTOR signaling pathway. In conclusion, these results indicated that PVP3-1-SeNPs could be potential anti-tumor nanoparticles for treating pancreatic cancer.
Shenxiong glucose injection (SGI) containing a water extract from the roots of Danshen and Ligustrazine hydrochloride, is the main drug used for the prevention and treatment of acute myocardial ischemia (AMI) in China. Based on the characteristics of drug clinical applications, this study aims to uncover the compatibility mechanism of SGI by investigating pharmacokinetic (PK) and pharmacodynamic (PD) differences between Danshen glucose injection (DGI), Ligustrazine glucose injection (LGI) and SGI groups after multiple dosing during the pathological state from the perspective of metabolic enzymes. Compared to the LGI group, the absorption (Cmax) and exposure (AUC) of ligustrazine increased significantly, and the protein expression of CYP1A2, CYP2C11 and CYP3A2 in the SGI group decreased significantly. Furthermore, the PK and PD experimental data for Danshen and ligustrazine in AMI rats were fitted to obtain a PK-PD binding model with three components. PK-PD parameter analysis showed that in the SGI group the IC50 values of ligustrazine and danshensu on AST, CK-MB, cTn-I and the IC50 values of rosmarinic acid on AST and CK-MB were lower than the DGI or LGI group. It is speculated that Danshen inhibited CYP1A2, CYP2C11 and CYP3A2 mediating the metabolism of ligustrazine and decreased the expression of these three isozymes, which further affected the in vivo process of ligustrazine. Moreover, the combination of Danshen and ligustrazine could have better regulating effect on AST, CK-MB and cTn-I. This preliminary study has provided a scientific basis for understanding the compatibility mechanism of SGI from the viewpoint of the regulation of CYP enzymes in the PK-PD model.
A new naphthoquinone, patulumnaphthoquinone A (1) and three new glycosides, patulumside B (2), patulumside C (3) and patulumside D (4) were isolated from the 30% ethanol extract of the fresh ripe fruits of Hypericum patulum Thunb. using column chromatography techniques. The structures of these compounds including absolute configurations were elucidated on the basis of HRESIMS, NMR spectroscopic analyses, calculated electronic circular dichroism spectra and comparison with the literatures.
Potentilla kleiniana belongs to the family Rosaceae,which distributes in Central Asia,East Asia and Southeast Asia.In China,this plant is mainly found in east,south and southwest provinces.P.kleiniana has been prescribed for the treatment of various diseases in the field of traditional Chinese medicine,such as cough,fever,tuberculosis,mastitis,rheumatoid arthritis.Our previous study found that P.kleiniana had a certain cytotoxicity on tumor cells.The purpose of this paper was to investigate the chemical constituents of P.kleiniana and their cytotoxicity on tumor cells.The 60%ethanol extract of P.kleiniana were isolated by D-101 macroporous adsorptive resins,silica gel,Sephadex LH-20,Toyopearl HW-40F,semi-preparative high performance liquid chromatography and other methods,and their chemical structures were elucidated on the basis of physicochemical properties,NMR and HR-ESI-MS analysis.Meanwhile,all these compounds were evaluated for cytotoxicity against human cervical cancer cell line Hela.The results were as follows:(1)Thirteen lignans were isolated and identified as(+)-pionresinol(1),(+)-8-hydroxypinoresinol(2),(+)-syringaresinol(3),(+)-medioresinol(4),(+)-pionresinol-4-O-β-D-glucopyranoside(5),(+)-8′-hydroxypinoresinol-4-O-β-D-glucopyranoside(6),(+)-8′-hydroxypinoresinol-4′-O-β-D-glucopyranoside(7),(+)-pinoresinol-8′-O-β-D-glucopyranoside(8),schilignan F(9),(+)-pionresinol-4,4′-O-bisglucopyranoside(10),(+)-lariciresinol-4′-O-β-D-glucopyranoside(11),neoolivil-4-O-β-D-glucopyranoside(12),3,3′-bis[3,4-dihydro-4-hydroxy-6-methoxy-2H-1-benzopyran](13).Among them,compounds 1-4,7,8,10,12,13 were isolated from genus Potentilla for the first time,and compounds 5,6,9,11 were isolated from P.kleiniana for the first time.(2)Cytotoxicity studies showed that compounds 1,3 and 4 display certain inhibitory activities against Hela cells with IC50 values of(69.94±1.89),(66.25±2.11),(59.81±1.73)μmol·L-1,respectively.Therefore,the study enriches the chemical constituents of P.kleiniana,and provides a material basis for the development of anti-cervical cancer drugs.
Background: Polygonum orientale L. (PO) has demonstrated notable efficacy in treating coronary heart disease. Previous research identified eight key active components in PO for cardiomyocyte protection, but the underlying mechanisms remained unclear; Methods: Network pharmacology and molecular docking were used to identify potential target proteins of PO’s active components. Experimental models assessed the cardioprotective effects and mechanisms; Results: Network analysis and molecular docking revealed that the active components exhibited the highest binding affinity with SOD2, indicating it as a key element in the cardiac protection of PO. In vivo, PO extract improved myocardial structure and function, and increased SOD2 protein levels. In vitro, the active components of PO (Mixture) mitigated oxidative stress and apoptosis, upregulating SIRT3 and decreasing acetylated SOD2, leading to increased SOD2 and reduced ROS levels. The observed effects were reversed by a SIRT3 inhibitor, indicating the involvement of the SIRT3/SOD2 signaling pathway; Conclusions: This comprehensive approach elucidated the critical mechanisms underlying the cardioprotective properties of PO’s bioactive constituents, highlighting the regulation of the SIRT3/SOD2 signaling pathway as a new mechanism for PO’s anti-cardiovascular disease effects, and suggesting the Mixture’s potential as a promising drug candidate.
Ethnopharmacological relevance: Functional dyspepsia (FD) is a disorder caused by abnormal gut-brain axis regulation and is highly prevalent in China. Cynanchum auriculatum (CA) is often used to treat FD in the ethnic minority areas of Guizhou. Although several CA-based products are currently available in the market, it is un-clear which components of CA are efficacious and what their oral absorption mechanism is.Aim of the study: This study aimed to screen anti-FD components of CA based on the spectrum-effect relationship. In addition, the study evaluated the intestinal absorption mechanism of these components using transporter inhibitors.Materials and methods: The fingerprinting of compounds from CA extract and plasma after oral administration was conducted using ultra-high-performance liquid chromatography quadrupole-time-of-flight tandem mass spectrometry (UHPLC-Q-TOF-MS). The intestinal contractile parameters were then measured in vitro using the BL-420F Biofunctional Experiment System. Multivariate statistical analysis of the result of spectrum-effect relationship assessment was used to elucidate the correlation between prominent peaks of CA-containing plasma and intestinal contractile activity. The effect of ATP-binding cassette (ABC) transporter inhibitors, such as the P-gp inhibitor verapamil, the MRR inhibitor indomethacin, and the BCRP inhibitor Ko143, on the directional transport of the predicted active ingredients was assessed in vivo.Results: Twenty chromatographic peaks were identified in the CA extract. Of these, three were C21 steroids, four were organic acids, and one was a coumarin, and acetophenone by comparing with reference compounds. Additionally, it is discovered that there are totally 39 migratory components in CA-containing plasma, which was found to significantly promote the contractility of the isolated duodenum. Moreover, multivariate analysis of the spectrum-effect relationship demonstrated that 16 characteristic peaks (3, 6, 8, 10, 11, 13, 14, 18, 21, m1-m4, m7, m15, and m24) in CA-containing plasma were significantly associated with the anti-FD effect. These com-pounds included seven prototype compounds, i.e., cynanoneside A, syringic acid, deacylmetaplexigenin, ferulic acid, scopoletin, baishouwubenzophenone, and qingyangshengenin. The inhibition of ABC transporters demonstrated that the inhibitors verapamil and Ko143 significantly increased (P < 0.05) the uptake of scopoletin and qingyangshengenin. Thus, these compounds may be substrates for P-gp and BCRP. Conclusions: The potential anti-FD components of CA and the effect of ABC transporter inhibitors on these active components were preliminarily clarified. These findings lay a foundation for subsequent in vivo studies.
Background Gerberae Piloselloidis Herba (GPH) exhibits notable efficacy in alleviating allergic asthma. Previous studies in our research have identified a mixture of luteolin, arbutin, and marmesin as effective components of GPH in treating allergic asthma. However, the underlying mechanism remains unclear. This study aims to elucidate the molecular mechanism of these active components. Method Using an ovalbumin (OVA)-induced allergic asthma mouse model, various treatment groups were administered, including GPH, the active component mixture (termed "Mixture") containing luteolin, arbutin, and marmesin, and a positive drug (dexamethasone, DEX). Relevant indices were assessed, including behavioral characteristics, inflammatory cell counts, cytokine levels, histopathological examination of lung tissue, apoptosis, and expression of key proteins such as Caspase-3, Bax, Bcl-2, PI3K, p-PI3K, Akt, and p-Akt. The effect of the Mixture on the PI3K/Akt signaling pathway was further verified using the PI3K inhibitor LY294002. Results The Mixture significantly alleviated asthma symptoms, decreased IgE levels, cytokine levels (IL-4, IL-5, IL-13 and TNF-α), and the number of inflammatory cells in serum or bronchoalveolar lavage fluid (BALF), leading to the alleviation of lung pathological lesions. Additionally, the Mixture reduced the expression of Bax and Caspase-3 while increasing Bcl-2 expression, resulting in mitigated apoptosis in lung tissue. Furthermore, there appeared a decrease in the levels of PI3K and p-PI3K, as well as the ratio of p-Akt to Akt in the Mixture group, indicating the suppression of PI3K and Akt phosphorylation. Interestingly, the effects of the Mixture were comparable to those of GPH, LY294002, or the combination of LY294002 with the Mixture. Conclusion The study confirms that the Mixture containing luteolin, arbutin, and marmesin indeed alleviates allergic asthma induced by OVA in mice by suppressing the PI3K/Akt signaling pathway. These findings highlight the potential of the GPH-derived Mixture as a novel therapeutic for the treatment of allergic asthma.
This study aimed to provide scientific evidence for predicting quality markers(Q-markers) of Xuebijing Injection by establishing high-performance liquid chromatography(HPLC) fingerprints of 25 batches of Xuebijing Injection and determining the contents of 9 major components, as well as conducting network pharmacology research. Thirty common peaks were identified by fingerprints of 25 batches of Xuebijing Injection samples, and 12 chromatographic peaks were determined, with similarity ranging from 0.970 to 0.999. Principal component analysis(PCA) showed that the cumulative variance contribution rate of the 12 principal components was 95.83%, and orthogonal partial least squares-discriminant analysis(OPLS-DA) revealed that 10 components variable importance projection(VIP) values were greater than 1. Network pharmacology analysis indicated that tryptophan, senkyunolide Ⅰ, hydroxysafflor yellow A, gallic acid, ferulic acid, protocatechuic aldehyde, rosmarinic acid, kaempferol-3-O-glucoside and neochlorogenic acid may be potential Q-markers of Xuebijing Injection. The contents of the above 9 index components were determined in 25 batches of Xuebijing Injection samples by HPLC. Six compounds including hydroxysafflor yellow A, kaempferol-3-O-glucoside, senkyunolide Ⅰ, ferulic acid, rosmarinic acid, and protocatechuic aldehyde were used as Q-markers for Xuebijing Injection through five aspects of measurability, effectiveness, compatibility, specificity and content determination.