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BACKGROUND: Metabolic syndrome (MetS) is a precursor to the development of many diseases (atherosclerosis, diabetes, etc.). It is marked by disruptions in glucose and lipid metabolism, along with hypertension. Numerous types of risk factors contribute to the development of the MetS, inflammation and insulin resistance are present throughout the metabolic abnormalities. Chrysanthemum indicum L. is a traditional Chinese plant used for both tea and medicine, known for its high content of total flavonoids, which are important secondary metabolites. Our research led to the extraction of a Buddleoside-Rich Chrysanthemum indicum L. extract (BUDE) which has demonstrated anti-inflammatory properties. Nonetheless, the specific role and mechanism of BUDE in preventing MetS remain unclear. METHODS: The study initially evaluated the role of BUDE in preventing MetS. Subsequently, it investigated the anti-inflammatory properties of BUDE in the liver and pancreas in response to unhealthy diets. It then examined the level of insulin resistance and pancreatic ß-cell function induced by inflammation. Additionally, an lipopolysaccharide (LPS)-induced macrophage inflammation model was used to further investigate the ameliorative effects of BUDE in inflammation. RESULTS: BUDE has hypotensive, hypoglycemic and hypolipidemic effects. It can also resolve the imbalance between macrophage subpopulations, impede the triggering of the NF-κB signaling pathway, reduce the secretion of inflammatory mediators, ameliorate insulin resistance, and safeguard organs such as the liver and pancreas from inflammatory damage. These effects collectively contribute to preventing the development of MetS. DISCUSSION: BUDE has the ability to modulate macrophage-mediated inflammation, leading to improved insulin resistance. Additionally, it delivers antihypertensive, hypoglycemic, and hypolipidemic effects, offering a potential for preventing MetS.

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Objective:To establish a method for determintation of chlorogenic acid and linarin in Yejuhua granules by HPLC.Methods:We applied HPLC methods. The Kromasil 100-5 C18 column (250 mm×4.6 mm,5 μm) was used, the mobile phase was acetonitrile-0.4%H 3PO 4 solution (gradient elution), the flow rate was 1.0 ml/min, the dection wavelenghth was 334 nm and the column temperture was 32 ℃. Results:Chlorogenic acid and buddleoside had good linearity in the ranges of 0.30-1.50 μg ( r2=0.999 1) and 0.12-0.62 μg ( r2=0.999 8), respectively. The average recoveries were 99.70% and 96.67%, with RSD<2%, respectively. Conclusion:The method is simple, rapid, reliable, efficient, and can be used for determination of chlorogenic acid and buddleoside in Yejuhua Granules.

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Linarin, as a natural coumponent belongs to flavonoid glycoside, is widely existed in herbal plants such as chrysanthemum indicum and Mongolian flower, which has a variety of pharmacological effects, such as anti-inflammation, anti-cancer, liver protection, analgesia, antipyretic, anti-oxidation, anti-apoptosis, sedation and sleep, neuroprotection, preventing and treating hypertension, treatingdiabetes, preventing and treating osteoporosis, whitening, skin care and sunscreen. It is difficult to dissolve in water and has poor oral efficacy, but when combined with different substances or combined (forming phospholipid complex), its bioavailability can be improved, so as to improve its pharmacological efficacy.

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As the number of patients with metabolic hypertension (MH) is increasing, there is an essential require for global measures to prevent and treat MH. Flavonoids such as buddleoside (BUD) from Chrysanthemum indicum L. are the main pharmacological components of cardiovascular activities. Previous studies have suggested that the buddleoside-rich Chrysanthemum indicum L. extract (BUDE) can reduce blood pressure in spontaneously hypertensive rats (SHR). However, its effect on MH and how it works remains to be researched. In this study, it was observed that BUDE could lower blood pressure, improve dyslipidemia, and decrease the level of plasma LPS in MH rats. Moreover, BUDE improved intestinal flora and increased the expression of occludin and claudin-1 in the colon, and improved the pathological injury of the colon. Western bolt and qRT-PCR experiments showed that BUDE could down-regulate TLR4 and MyD88 protein and mRNA expression and inhibit phosphorylation of IKKß, IκBα and NF-κB p65 in vessels of MH rats. These results showed that BUDE could regulate intestinal flora, improve intestinal barrier function, reduce the production and penetration of LPS, thereby inhibiting the vascular TLR4/MyD88 pathway, improving vascular endothelial function, and ultimately lowering blood pressure in MH rats. This study provides a new mechanism of BUDE against MH by inhibiting the enteric-origin LPS/TLR4 pathway.

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Objective: The aim of this paper was to observe the effects of buddleoside on hypertensive vascular remodeling through Ang II/AT1 signaling pathway in aorta. Methods: We used SHR model to examine the blood pressure, vertigo time, histomorphology, and collagen fiber distribution of the aorta, and evaluate whether buddleoside could ameliorate the hypertensive vascular remodeling in vivo. Meanwhile, abnormal proliferation and migration of VSMCs induced by Ang II in vitro was used to identify the mechanism. The anti-proliferation effect of buddleoside in VSMCs was observed using MTT assay and crystal violet assay. The anti-migration effect in VSMCs was observed using monolayer-wounding and boyden chamber transwell assay. Furthermore, the protein expression of Ang II, AT1, MMP-2, MMP-9, Src, p-Src, Syk, and p-Syk were examined. Results: The results showed that buddleoside could significantly decrease SBP, DBP, MBP, and vertigo time, and improve the thickened media aorta, hypertrophy and disordered arrangement of VSMCs, distribution of collagen fibers. Buddleoside could also inhibit the proliferation and migration of VSMCs, inhibit the ROS production, and reduce the protein expression of Ang II, AT1, MMP-2, MMP-9, Src, and p-Src. Conclusion: These data supported that buddleoside can ameliorate hypertensive vascular remodeling by inhibiting the proliferation and migration of VSMCs. Its mechanism is mediated by the regulation of Ang II/AT1 signaling pathway.

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The dynamic changes of active components in stems and leaves of Mentha Haplocalycis Herba(mint) at different harvest periods were investigated, and the optimum harvest time of mint was explored. In this study, hesperidin, diosmin, didymin and buddleoside were selected as flavonoids index components of mint, and the QAMS method was established to measure the contents of these flavonoids in mint. The contents of 4 flavonoid glycosides in the mint stems and leaves from three habitats harvested in different time were studied and evaluated comprehensively using statistical analysis and principal component analysis (PCA). The results showed that the contents of 4 components in the leaves are higher than that in the stems despite of habitats and harvest time, and they all exhibited dynamic changes along with the harvest periods within the same habitat. Three harvest periods in mid April, mid September and late October scored higher in comprehensive evaluation in Jiangsu region, the genuine producing area of Mentha Haplocalycis Herba. Combined with the yield and contents of active compounds, the optimum harvest time of mint in Jiangsu region was mid September and late October, which is basically consistent with the traditional harvesting periods.

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We have developed a new method to simultaneously determine five marker compounds in Menthae Herba via HPLC/PDA - including hesperidin (1), rosmarinic acid (2), diosmin (3), didymin (4) and buddleoside (5). The newly developed method was successfully used to analyse for two species (Mentha arvensis L. and Mentha haplocalyx Briq.) of Menthae Herba, and the satisfactory results were obtained from the validation of developed method. The pattern analysis could greatly discriminate between M. arvensis L. and M. haplocalyx Briq. In conclusion, the proposed HPLC/PDA method is suitable for quality evaluation of Menthae Herba.

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The dynamic changes of active components in stems and leaves of Mentha Haplocalycis Herba(mint) at different harvest periods were investigated, and the optimum harvest time of mint was explored. In this study, hesperidin, diosmin, didymin and buddleoside were selected as flavonoids index components of mint, and the QAMS method was established to measure the contents of these flavonoids in mint. The contents of 4 flavonoid glycosides in the mint stems and leaves from three habitats harvested in different time were studied and evaluated comprehensively using statistical analysis and principal component analysis (PCA). The results showed that the contents of 4 components in the leaves are higher than that in the stems despite of habitats and harvest time, and they all exhibited dynamic changes along with the harvest periods within the same habitat. Three harvest periods in mid April, mid September and late October scored higher in comprehensive evaluation in Jiangsu region, the genuine producing area of Mentha Haplocalycis Herba. Combined with the yield and contents of active compounds, the optimum harvest time of mint in Jiangsu region was mid September and late October, which is basically consistent with the traditional harvesting periods.

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To study the relaxation effect of buddleoside combined with luteolin on aortic rings in SD rats and its mechanism. The effect of buddleoside alone(7.5×10⁻6g•mL⁻¹), luteolin alone(7.5×10⁻6g•mL⁻¹) and the combination of buddleoside and luteolin(1∶4) on norepinephrine-induced contractility of complete, endothelium-denuded, and L-NAME and indomethacin-pretreated thoracic aorta in SD rats were observed in the in vitro ring tension test. Western blot was used to detect p-Akt and p-eNOS protein expressions in the thoracic aorta. The experimental results showed that buddleoside combined with luteolin could significantly increase the relaxation rate of blood vessels and endothelium and L-NAME-pretreated vascular rings compared with the two single administrations. And buddleoside combined with luteolin could also significantly increase p-Akt and p-eNOS protein expressions.The results suggested that the combination of buddleoside and luteolin could effectively relax the blood vessel, and the mechanism may be to increase the synthesis and release of NO and reach the role of relaxing blood vessel by activating PI3K/Akt/NO signaling pathway and enhancing the activity of eNOS.

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To study the relaxation effect of buddleoside combined with luteolin on aortic rings in SD rats and its mechanism. The effect of buddleoside alone(7.5×10⁻⁶g•mL⁻¹), luteolin alone(7.5×10⁻⁶g•mL⁻¹) and the combination of buddleoside and luteolin(1∶4) on norepinephrine-induced contractility of complete, endothelium-denuded, and L-NAME and indomethacin-pretreated thoracic aorta in SD rats were observed in the in vitro ring tension test. Western blot was used to detect p-Akt and p-eNOS protein expressions in the thoracic aorta. The experimental results showed that buddleoside combined with luteolin could significantly increase the relaxation rate of blood vessels and endothelium and L-NAME-pretreated vascular rings compared with the two single administrations. And buddleoside combined with luteolin could also significantly increase p-Akt and p-eNOS protein expressions.The results suggested that the combination of buddleoside and luteolin could effectively relax the blood vessel, and the mechanism may be to increase the synthesis and release of NO and reach the role of relaxing blood vessel by activating PI3K/Akt/NO signaling pathway and enhancing the activity of eNOS.

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Objective To establish the quality control ofBaiduyin syrup.Methods The TLC was used to identity Radix paeoniae rubra, Radix Scutellariae. The quantitative determination of baicalin and buddleoside was completed by HPLC.Results The spots on TLC plates were distinct and high resolution. Compared with the negative samples, the contrast medicinal materials or control products showed that there were no spots of the same color in the corresponding position. The linear ranges of baicalin and buddleoside were 0.2179-2.1790 μg (r2=0.999 9), 0.1319-1.3190 μg (r2=0.999 7). TheRSD were 1.51% and 2.01%. Conclusions The established quality control method is simple, accurate and reproducible, which can be used for the quality control ofBaiduyin syrup.

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Objective: To establish a new method for the quantitative analysis of multi-components by single-marker (QAMS) to simultaneous determine seven components in Chrysanthemum indicum. Methods: The chlorogenic acid was used as internal marker to calculate the relative correlation factors (RCF) of caffeic acid, luteolin-7-O-glucoside, 3,5-O-dicaffeoylquinic acid, buddleoside, luteolin, and apigenin by high performance liquid chromatography (HPLC). The repeatability of RCF was investigated. The contents of seven components were determined by the external standard method and QAMS respectively. Results: The reproducibility of RCF was perfect. The value calculated by QAMS was consistent with the external standard method. Conclusion: The QAMS method for simultaneously measuring the content of seven components is feasible and accurate to evaluate the quality of Chrysanthemum indicum.

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Buddleoside (also known as linarin) as the major flavonoid in Chrysanthemum morifolium Ramat., has been reported to possess a wide range of pharmacological activities. The human intestinal microbiota might have an important impact on drug metabolism and ultimately on the drug oral bioavailability. However, the interaction of the buddleoside with human intestinal bacteria remains unknown. In this study, the conversion of buddleoside by different bacteria from human feces was firstly investigated. A reliable, sensitive and rapid analytical method, ultra performance liquid chromatography was established and successfully applied to investigate the metabolites and metabolic profile of buddleoside by human intestinal bacteria. Among the isolated bacteria, four strains including Escherichia sp. 4, Escherichia sp. 34, Enterococcus sp. 45 and Bacillus sp. 46 showed more powerful conversion capability. Based on the accurate mass data and the characteristic MS(n) product ions, the parent and six metabolites were detected and tentatively identified compared with blank samples. The metabolites were produced by four main metabolic pathways including deglycosylation, acetylation, methylation and hydroxylation. Buddleoside could be firstly converted to its aglycon acacetin (M2) by the majority of the isolated intestinal bacteria. Subsequently, M2 was further metabolize to its methylated (M3), acetylated (M4), hydroxylated (M5) and hydrogenated product (M6). However, acacetin-7-glucosid (M1) was obtained only from the minor bacterial samples like Bacillus sp. 46. To further explain the metabolism of buddleoside, the ß-d-glucosidase and α-l-rhamnosidase activities of four strains were analyzed. Bacillus sp. 46 could only produce α-l-rhamnosidase, while the other three strains showed two kinds of enzyme activities. Furthermore, the activities of α-l-rhamnosidase and ß-d-glucosidase reached the highest level at 12-18h and 10-12h, respectively. The metabolic routes and metabolites of buddleoside produced by human intestinal microflora were firstly reported in this paper. The results will be very helpful for the further investigation of the pharmacokinetic research of buddleoside and to unravel how it works in vivo.

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Objective: To develop an HPLC-DAD method for the simultaneous determination of liquiritin, ammonium glycyrrhizinate, vitexicarpin, pulegone, ferulic acid, chlorogenic acid, 3,5-dicaffeoyl quinic acid, berberine hydrochloride, kaempferol, and buddleoside in Boyun Tuiyi Pill (BTP). Methods: Shim-pack VP-ODS C18 column (250 mm × 4.6 mm, 5 μm) was adopted. The mobile phase was composed of methanol-acetonitrile (50:50, A) and 0.05% phosphoric acid (B) with gradient elution. Gradient elution: 0-5.0 min, 50% A; 5.0-30.0 min, 50%-80% A; 30.0-32.0 min, 80%-50% A; and 32.0-40.0 min, 50% A; Injection volume was 10 μL. The flow rate was 1.0 mL/min and the column temperature was 40℃. Results: liquiritin, ammonium glycyrrhizinate, vitexicarpin, pulegone, ferulic acid, chlorogenic acid, 3,5-dicaffeoyl quinic acid, berberine hydrochloride, kaempferol, and buddleoside were separated well. The linear calibration curves were obtained in 2-20 μg/mL for liquiritin, r = 0.999 2; 20-200 μg/mL for ammonium glycyrrhizinate, r = 0.999 5; 3-30 μg/mL for vitexicarpin, r = 0.999 4; 2-20 μg/mL for pulegone, r = 0.999 7; 1.2-12.0 μg/mL for ferulic acid, r = 0.999 5; 3.5-35.0 μg/mL for chlorogenic acid, r = 0.999 2; 8-80 μg/mL for 3,5-dicaffeoyl quinic acid, r = 0.999 3; 9-90 μg/mL for berberine hydrochloride, r = 0.999 3; 2-20 μg/mL for kaempferol, r = 0.999 6; and 3-30 μg/mL for buddleoside, r = 0.999 5. The average recoveries of the 10 constituents were 99.1%, 101.1%, 100.2%, 99.4%, 101.9%, 98.5%, 100.5%, 101.7%, 100.8%, and 99.7% with RSD of 0.62%, 0.79%, 0.77%, 0.83%, 0.47%, 0.38%, 0.97%, 1.05%, 0.86%, and 1.11%. The contents of six batches of the liquiritin, ammonium glycyrrhizinate, vitexicarpin, pulegone, ferulic acid, chlorogenic acid, 3,5-dicaffeoyl quinic acid, berberine hydrochloride, kaempferol, and buddleoside were 0.505-0.685, 1.793-2.012, 0.227-0.268, 0.183-0.206, 1.258-1.324, 0.348-0.381, 0.648-0.720, 1.544-1.722, 1.543-1.627, and 3.434-3.883 mg/pill, respectively. Conclusion: The method is rapid and has high sensitivity, high accuracy, and good specificity. It can be applied to the quality control of BTP.

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Objective: To establish the chromatography fingerprint of Schisandra chinensis Chewable Tablets (SCCT) with HPLC-DAD and to evaluate SCCT from 10 different batches. Methods: Luna C18 column (250 mm×4.6 mm, 5 μm) was used, mobile phase was acetonitrile-0.05% phosphate, flow speed was 1.0 mL/min, temperature of column was set at 35℃, detected wavelength was at 220 nm, and injection volume was 20 μL. Results: The chromatography fingerprint of SCCT from 10 different batches was established. In the chromatography fingerprint with HPLC-DAD of SCCT, 39 common peaks were demarcated and the similarities of SCCT were between 0.914-0.999. Schizandrin, schisandrol B, schisantherin A, schisandrin B, schisandrin C, salvianic acid A sodium, salvianolic acid B, cryptotanshinone, tanshinone IIA, 3, 4-dihydroxyhenzaldehyde, luteoloside, and buddleoside were identified. Conclusion: The method is accurate, reliable and with good reproducibility, and can be used as the evidence for the quality evaluation of SCCT.

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ETHNOPHARMACOLOGICAL RELEVANCE: Flos Chrysanthemi is used in a variety of diseases in traditional Chinese medicine including hypertension, and the total flavonoids (rich in luteolin (LUT) and buddleoside (BUD)) of Flos Chrysanthemi is known to modulate vascular functions and reduce the blood pressure. However, the active flavonoids and their synergistic effects on anti-hypertension are still unclear. To investigate the combined anti-hypertension effects of LUT and BUD enriched extracts on spontaneously hypertensive rats (SHR), as well as the anti-hypertensive mechanism of LUT&BUD mixture. MATERIALS AND METHODS: CODA Mouse & Rat Tail-Cuff Blood Pressure System was used to measure the systolic blood pressure (SBP) and diastolic blood pressure (DBP) of SHR after treated with extracts contains with LUT and/or BUD. The expressions of Ang II, PRA, ALD, ET, PGI2 and TXB2 were investigated by ELASA. Serum NO concentration was measured by the method of Nitric acid reductase. RESULTS: A single administration of LUT, BUD, or LUT:BUD=1:1 significantly reduced SBP by about 3.35 mmHg, 4.39 mmHg and 15.42 mmHg, respectively. Chronic administration of LBM (at 60 mg/kg; p.o. for 30 days) reduced both SBP and DBP by 4.04% and 5.24% of the vehicle group, respectively. Oral administration of LBM at 60 mg/kg inhibited the serum levels of ANG, ALD and ET, but increased serum NO concentration. CONCLUSION: This study shows the synergistic anti-hypertension effects of LUT and BUD in SHR. The effects of LBM on blood pressure are associated with RAAS and endothelial system. Thus, our experiments suggest that the combination of luteolin and buddleoside from Flos Chrysanthemi are potentially useful for the therapeutic treatments for hypertension.

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Objective To establish a method for content determination of Buddleoside in Compound Yinpujiedu Tablet. Method HPLC method, Agilent Eclipse XDB-C18 column (4.6 mm?250 mm, 5 ?m) was used, mobile phase was methanol-4% glacial acetic acid (47∶53), and the detecting wavelength was set at 334 nm. Result The standard curve was linear within the range of 2.24～44.8 ?g. The average recovery and RSD were 97.8% and 1.52%, respectively. Conclusion This method is accurate, reliable, and can provide a scientic index for quality control of Compound Yinpujiedu Tablet.