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ObjectiveTo investigate the protective effect of total lignans of Arctii Fructus on the retinal tissue in the rat model of type 2 diabetes mellitus. MethodWistar rats were randomized into normal， model， solvent， Shuangdan Mingmu Capsules （618 mg·kg-1）， and low-， medium-， and high-dose （100， 200， 400 mg·kg-1， respectively） total lignans of Arctii Fructus groups， with 16 rats in each group. The rat model was established by streptozotocin （STZ） combined with a high-fat diet and administrated with corresponding drugs by gavage once a day for 14 weeks. At the 14th week， blood was sampled for the collection of serum from the abdominal aorta after anesthesia， and bilateral eyeballs were collected and frozen. Hematoxylin-eosin （HE） staining was used to observe the histopathological changes of the retinal tissue in rats. The pathological changes of retinal vascular network in rats were observed by retinal vascular tissue digestion and mounting The levels of vascular endothelial growth factor （VEGF）， tumor necrosis factor-α （TNF-α）， and intercellular adhesion molecule-1 （ICAM-1） in the serum were determined by the ELISA kit. ResultCompared with the normal group， the solvent group showed pathological changes in the retinal tissue， reduced retinal ganglion cells （P<0.01）， and retinal thinning （P<0.01）， decreased E/P value in retinal blood vessels （P<0.01）， and elevated serum levels of VEGF， TNF-α， and ICAM-1 （P<0.01）. Compared with the model group， the total lignans of Arctii Fructus increased the retinal ganglion cells （P<0.01）， thickened the retina （P<0.01）， and lowered the serum levels of VEGF， TNF-α， and ICAM-1 （P<0.05， P<0.01）. ConclusionTotal lignans of Arctii Fructus may lower the VEGF， TNF-α， and ICAM-1 levels to protect the retina.
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In this study, we accurately collected the embryonic parenchyma cells and endocarp stone cells of Arctii Fructus at five different growth stages by laser microdissection. Quantitative analyse of caffeic acid, arctiin and arctigenin in these cells were performed using ultra-fast liquid chromatography-tandem mass spectrometry (UFLC-MS/MS). The results showed that a large amount of arctiin was produced and accumulated in embryonic parenchyma cells from the late flowering stage to mature stage, while much lower content of arctiin was produced and accumulated in endocarp stone cells at these stages. It suggested that the biosynthetic pathways of arctiin were different in embryonic parenchyma cells from endocarp stone cells of Arctii Fructus. Arctigenin was found to be produced and accumulated in both embryonic parenchyma cells and in endocarp stone cells from the late flowering stage to mature stage, but it reached a peak in endocarp stone cells at late flowering stage, then decreased slowly. The concentration of arctigenin was far less than that of arctiin regardless of embryonic parenchyma cells or endocarp stone cells. These results have validated the new method for analysis of dynamic accumulation of arctiin in Arctii Fructus by UFLC-MS/MS with frozen sections and microdissection.
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In our study of the chemical constituents of the dried mature fruits of Arctium lappa L., ten compounds were isolated by various chromatography methods and preparative HPLC. Their structures were elucidated as (7R,8R)-4,7,9,9'-tetrahydroxy-3,3'-dimethoxy-8-4'-oxyneolign-7'-ene-9'-O-β-D-glucopyranoside (1), (7R,8R)-4,7,9,9'-tetrahydroxy-3,3'-dimethoxy-8-O-4'-neolignan-9'-O-β-D-glucopyranoside (2), (7R,8R)- 4,7,9,9'-tertahydroxy-3,3'-dimethoxy-8-4'-oxyneolignan (3), (7S,8R)-dihydrodehydrodiconiferylalcohol-4-O-β- D-glucopyranoside (4), (7S,8R,7'R,8'R)-pinoresinol-4,4'-di-O-β-D-glucopyranoside (5), (8S,7'S,8'R)-4,4',9'- trihydroxy-3,3'-dimethoxy-7',9-epoxylignan-7-oxo-4'-O-β-D-glucopyranoside (6), 2-methoxy-4-hydroxyphenol- 1-O-β-D-xylopyranosyl-(1→6)-O-β-D-glucopyranoside (7), 3-methoxy-4-hydroxyphenol-1-O-β-D-xylopyranosyl- (1→6)-O-β-D-glucopyranoside (8), 4-hydroxy-3-methoxybenzylalcohol-4-O-β-D-xylopyranosyl-(1→6)-O-β-D- glucopyranoside (9) and 2-phenethyl β-primeveroside (10) by their spectroscopic data (IR, UV, CD, MS, HR-ESI-MS, and 1D and 2D NMR) and comparison to literature data. Compound 1 is a new 8-O-4'-neolignan. Compounds 2-10 were isolated from the dried mature fruits of Arctium lappa L. for the first time.
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Objective: To establish HPLC fingerprint for Yinqiao Qingre Tablet (YQT), and analyze the chemical composition of YQT by ESI-Q-TOF MS. Methods: The Kromasil C18 column (250 mm × 4.6 mm, 5 μm) was used with a mobile phase of acetonitrile-0.1% phosphoric acid in gradient elution, the flow rate was 1.0 mL/min, the column temperature was 25℃, and the detection wavelength was 230 nm. Ultra performance liquid chromatography-quadrupole time-of-flight tandem mass spectrometry (UPLC-Q-TOF/MS) was used for qualitative analysis in the positive and negative ion modes. Results: The HPLC fingerprint for 11 batches of YQT and 28 common peaks were obtained, belonging to six medicinal herbs. Among them, seven common peaks came from Forsythiae Fructus, nine common peaks came from Lonicerae Japonicae Flos, six common peaks came from Puerariae Lobatae Radix, three common peaks came from Arctii Fructus, one common peak (peak 2) came from Forsythiae Fructus and Cimicifuga Rhizoma, another two common peaks came from Anemarrhenae Rhizoma and Cimicifuga Rhizoma, respectively. The similarity of 11 batches of YQT was over 0.95.Totally 42 chemical components were identified by UPLC-Q-TOF/MS, 16 of which were identified by references, such as puerarin, daidzin, daidzein, neochlorogenic acid, chlorogenic acid, cryptochlorogenin acid, isochlorogenic acid A, isochlorogenic acid B, isochlorogenic acid C, secoxyloganin, rutin, phillyrin, forsythoside A, arctiin, mangiferin, and timosaponin B II, respectively. Conclusion: This study perfects the system of quality standard and provides the reference for the study of substance basis and quality control of the same type of compound preparations.
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Objective: To study the chemical constituents from the inflorescence bracts of Arctii Fructus. Methods: The compounds were isolated and purified by the methods of silica gel column chromatography, HPLC, and recrystallization, and the structures were elucidated by the means of spectral analysis. Results: Twelve compounds were isolated and identified as daucosterol (1), isofouquierol (2), (22E)-5α, 8-epidioxyergosta-6, 22-dien-3β-ol (3), 3β-hydroxy-21, 22-epoxyursa-20(30)-en (4), 3β, 21β-dihydroxy-20(30)-en-taraxastane (5), oleanolic acid (6), arctigenin (7), carthamogenin (8), caffeic acid (9), 4(14)-eudesmene-8α, 11-diol (10), monogynol A (11), and lupeol (12). Conclusion; Compounds 2-3, 5, 6, 10-11 are obtained from the plants of Arctium L. for the first time, and compound 12 is isolated from the inflorescence bracts of Arctii Fructus for the first time.
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Linoleic acid [LA; 18: 2 (n-6)] is the most abundant polyunsaturated fatty acid in human skin. The exclusion of LA from diet induces epidermal hyperproliferation, which is reversible by the inclusion of LA in diet, and hence, LA is heralded as an essential fatty acid (EFA). Since safflower oil (SO) has been widely recognized as the major dietary source of LA and Arctii Fructus (Arctium lappa L.) is recently reported to contain high level of LA, we compared the antiproliferative effects of SO and Arctii Fructus in this study. Epidermal hyperproliferation was induced in guinea pigs by hydrogenated coconut oil (HCO) diet for 8 wk. During following 2 wk, EFA deficient guinea pigs were fed diets of safflower oil (group HS), water extract of Arctii Fructus (group AW) or organic extract of Arctii Fructus (group AO). Normal control group was fed SO containing diet (group SO) and EFA deficient group was fed HCO containing diet (group HCO) for 10 wk. Epidermal hyperproliferation was reversed in groups AO (55.9% of group HCO) and HS(74.1% of group HCO). However, the thymidine incorporation into epidermal DNA of group HS was greater than of normal control group SO. Epidermal hyperproliferation was not reversed in group AW. The accumulations of LA into phospholipids and ceramides, and of 13-hydroxyoctadecadienoic acid (13-HODE), the potent antiproliferative metabolite of LA in the epidermis of group AO were greater than of group HS. In contrast, the de novo synthesis of ceramides, the major lipids maintaining epidermal barrier, did not differ between all of groups. Together, our data demonstrate that organic extract of Arctii Fructus is more prominent than safflower oil in reversing epidermal hyperproliferation by inducing the higher accumulations of LA and 13-HODE in the epidermis of guinea pigs.