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淫羊藿总黄酮纳米混悬剂的制备及体外评价
淫羊藿总黄酮纳米混悬剂的制备及体外评价
丁志远1,2,3，杨 娟1 ，谢 燕1,2,3* (1. 上海中医药大学公共健康学院，上海 201203；2. 江苏康缘药业股份有限公司，江苏连云港 222001； 3. 中药制药过程新技术国家重点实验室，江苏连云港 222001)
摘要 ：为提高淫羊藿总黄酮 (1) 的溶解度和溶出度，该研究分别采用微型化介质研磨法和沉淀 - 高压均质法，以十二烷基硫酸钠 (SDS) 和聚乙烯己内酰胺 - 聚乙酸乙烯酯 - 聚乙二醇接枝共聚物 (Soluplus) 为稳定剂，制备了 3 种淫羊藿总黄酮纳米混悬剂 (1-NSps)。表征结果显示，3 种 1-NSps 粒径均在 200 nm 以下，在 4 ℃下具有良好的物理稳定性。并且，1 制 成纳米混悬剂后，其中各成分的分子结构未发生改变，少量晶型化合物在稳定剂为 Soluplus 的纳米混悬剂中晶型衍射峰减弱、结晶度降低，但在稳定剂为 SDS 的纳米混悬剂中以无定形状态存在。3 种 1-NSps 中淫羊藿苷和淫羊藿次苷Ⅱ的饱和溶解度与稳定剂种类相关。相较于原料药，3 种 1-NSps 中总黄酮的溶出速率和溶出程度均明显增加，在水中 180 min 时的溶出率分别为 75.77％、76.26％和 84.36％ ；与微型化介质研磨法制品相比，沉淀 - 高压均质法制品的溶出更完全。
......淫羊藿次苷Ⅱ (icariside Ⅱ，3) 对照品 ( 成都德思特生物技术有限公司，含量≥98 ％，批 号 DST200518-092)......
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Network analysis combined with pharmacological evaluation strategy to reveal the mechanism of Tibetan medicine Wuwei Shexiang pills in treating rheumatoid arthritis
Tibetan medicine is an important part of traditional Chinese medicine and a significant representative of ethnic medicine in China. Tibetan medicine is gradually recognized by the world for its unique curative effects. Wuwei Shexiang pills (WPW) has been widely used to treat “Zhenbu” disease (Also known as rheumatoid arthritis) in Tibetan medicine, however, its potential bioactive ingredients and mechanism for RA treatment remain unclear. In this study, we used a combination of gas chromatography-mass spectrometry (GC-MS), ultra-performance liquid chromatography coupled with quadrupole time-of-fight mass spectrometry (UPLC-Q-TOF/MS), network analysis and experimental validation to elucidate the potential pharmacodynamic substances and mechanisms of WPW in the treatment of rheumatoid arthritis (RA). The results showed that songoramine, cheilanthifoline, saussureanine C, acoric acid, arjunolic acid, peraksine, ellagic acid, arjungenin and other 11 components may be the main activities of WPW in the treatment of RA. PIK3CA, AKT, MAPK, IL-6, TNF, MMP1, MMP3, and CDK1 are considered as core targets. PI3K-AKT, MAPK, apoptosis, cell cycle, and other signaling pathways may be the key pathways for WPW to play a role in the treatment of RA. Furthermore, we validated the underlying molecular mechanism of WPW predicted by network analysis and demonstrated its possible mechanism through in vivo animal experiments. It was found that WPW could significantly improve the degree of paw swelling, and reduce ankle joint diameter and arthritis index. Further histomorphological analysis showed that WPW could reduce the degree of synovial tissue inflammation and ankle joint cartilage damage. Meanwhile, WPW could down-regulate the levels of IL-6, IL-1β, and IL-17, and increase the levels of IL-10 and IL-4 in the serum of AA rats. TUNEL staining confirmed that WPW could significantly promote the apoptosis of synovial cells. Moreover, the immunohistochemical results showed that WPW decreased the expression of PI3K, AKT, MAPK, MMP1, MMP3, CDK1, and Bcl-2, as well as increased the expression of Bax protein. In conclusion, we successfully combined GC-MS, UPLC-Q-TOF/MS, network analysis, and experimental validation strategies to elucidate the inhibition of inflammation by WPW in AA model rats via PI3K/AKT, MAPK, cell cycle and apoptotic pathways process. This not only provides new evidence for the study of potential pharmacodynamic substances and the mechanism of WPW in the treatment of RA, but also provides ideas for the study of other Tibetan medicine compound preparations.
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2 Materials and methods
2.1 Materials and chemicals
Chemical reference standards of cholic acid (DSTDD004201), chebulagic acid (DST200927-064), chebulic acid (DST200610-244), corilagin (DST210311-012), ethyl gallate (DSTDM006301), benzoic acid (DSTDB012001), linoleic acid (DST200611-211), betulin (DSTDB002701), aconitine (HR1001S4), benzoylmesaconine (DSTDB005601), benzoylaconitine (DSTDB005501), benzoylhypaconine (DSTDB005701), hypaconitine (DSTDC005801), mesaconitine (DSTDX002502), methyl caffeate (DST210427-054) and costunolide (DSTDM003001) were acquired from Chengdu Desite Biotechnology Co.,. (Chengdu, China), and the purity of all standards were above 98%.
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原文链接：https://www.frontiersin.org/articles/10.3389/fphar.2022.941013/full
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An In Vitro Dissolution Determination of Multi-Index Components in Tibetan Medicine Rhodiola Granules
Abstract
The composition of the Tibetan medicine Rhodiola granules (RG) is complex, and the overall quality of RG is difficult to determine. Therefore, establishing a method to determine the multi-component in vitro dissolution of RG is of great significance for quality control. This study uses the second paddle method of the fourth general rule 0931 from the Chinese Pharmacopoeia (2020 edition), compliant with apparatus 2 of the United States Pharmacopeia (USP). The dissolution apparatus was set to a rotation speed of 100 rpm with ultrapure water as the dissolution medium. A sample volume of 1 mL was collected at each timepoint. Furthermore, the cumulative dissolution of gallic acid, salidroside, and ethyl gallic acid in RG at different time points was determined by high-performance liquid chromatography (HPLC). Finally, the dissolution curves were drawn, and the curves were fitted to the GompertzMod, the Gompertz, the Logistic, and the Weibull equations. The results showed that the cumulative dissolution of gallic acid in RG was over 80% at 1 min, the cumulative dissolution of salidroside and ethyl gallic acid was over 65% at 5 min, and the cumulative dissolution of each index component decreased after 30 min. The curve fitting demonstrated that the GompertzMod equation was the best-fitting model for each index component of RG. In conclusion, the dissolution test method described in this protocol is simple, accurate, and reliable. It can characterize the dissolution behavior of the index components in RG in vitro, which provides a methodological reference for quality control of RG and quality evaluation of other ethnic compounds.
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Materials
Name
Company
Catalog Number
Ethyl gallate (HPLC, ≥98%)
Chengdu Desite Biotechnology Co., Ltd.
DSTDM006301
Gallic acid (HPLC, ≥98%)
Chengdu Desite Biotechnology Co., Ltd.
DSTDM000802
Salidroside (HPLC, ≥98%)
Chengdu Desite Biotechnology Co., Ltd.
DST200425-037
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原文地址：jove.com/video/64670
jove.com/video/64670
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Isochlorogenic Acid C Restrains Erk/JNK/NF-κB Signaling to Alleviate Inflammatory Response and Promote Cell Apoptosis
Abstract
Isochlorogenic acid C (ICAC) is found in a variety of natural foods and medicinal plant materials. This study aims to validate the biological activity of isochlorogenic acid C in limiting inflammation by the Erk/JNK/NF-κB pathway. In this study, TNF-α-induced human fibroblast-like synoviocytes and collagen-induced arthritis animal models were used to perceive the potential anti-inflammation mechanism of ICAC. The role of isochlorogenic acid C was evaluated by observing the migration, invasion ability, and apoptotic activity of TNF-α-induced fibroblast-like synoviocytes cells in humans and analysing foot swelling, joint index, and histopathological changes in a collagen-induced RA animal model. The results reveal that ICAC inhibited the proliferation of human fibroblast-like synoviocytes and promoted their apoptosis. ICAC also blocked the nuclear transfer of NF-κB, Erk, and JNK. It was observed that ICAC significantly inhibited the degree of posterior foot swelling in CIA, reducing arthritis scores, bone tissue injury, and articular synovitis. ICAC may promote cell apoptosis and inhibit the hyperactivation of inflammatory cells to alleviate inflammation-induced synovial proliferation through the Erk/JNK/NF-κB pathway.
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2. Materials and Methods
2.1. Chemicals and Reagents
Isochlorogenic acid C (ICAC), with a purity of 98%, was purchased from Desite Biotechnology Co., Ltd. (Lot: 1092320232, Chengdu, China).……
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原文地址：https://doi.org/10.1155/2023/5547108
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The Interactional Characterization of Lentil Protein Isolate (LPI) with Cyanidin-3-O-Glucoside (C3G) and Their Effect on the Stability and Antioxidant Activity of C3G
Abstract
The interaction between lentil protein isolate (LPI) and cyanidin-3-O-glucoside (C3G) was investigated via with UV–vis spectroscopy, circular dichroism, and fluorescence spectroscopy and the stability of anthocyanin was also evaluated. After LPI mixed with C3G, the turbidity and foaming capacity increased and the particle size and surface charge did not change significantly, while the surface hydrophobicity decreased significantly (p < 0.05). The fluorescence results indicated that C3G quenched the intrinsic of LPI by static quenching and LPI bound with C3G via hydrophobic effects with Ka of 3.24 × 106 M−1 at 298 K. The addition of LPI significantly (p < 0.05) slightly decreased the thermal and oxidation degradation of C3G by up to 90.23% and 54.20%, respectively, while their antioxidant activity was inhibited upon mixing. These alterations of physicochemical properties might be attributed to their structural changes during the interaction. The obtained results would be of help in stabilizing bioactive compounds and the development of functional foods.
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2. Materials and Methods
2.1. Materials and Reagents
Cyanidin-3-O-Glucoside（C3G ）(98% purity) was obtained from Chengdu Lemeitian Pharmaceutical Technology Co., Ltd. (Chengdu, China).
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原文： https://doi.org/10.3390/foods12010104
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A novel ion mobility separation-enabled and precursor ions list-included high-definition data-dependent acquisition (HDDDA) approach: Method development and its application to the comprehensive multicomponent characterization of Fangji Huangqi Decoction
Abstract
To elucidate the chemical composition of a traditional Chinese medicine (TCM) formula necessitates the development of more potent analytical strategies, because of the complexity as a result of the superposition of multiple drugs. Fangji Huangqi Decoction (FHD) is a four-component TCM formula composed by complicated chemical constituents. By using the VionTM ion mobility quadrupole time-of-flight (IM-QTOF) mass spectrometer, we present a novel IM separation-enabled and precursor ions list (PIL)-included high-definition data-dependent acquisition (HDDDA) approach, and apply it to the multicomponent characterization of FHD by coupling to ultra-high performance liquid chromatography. Chromatographic separation was conducted on a CORTECS® UPLC® T3 column, while HDDDA was employed for MS2 data acquisition in both the negative and positive electrospray-ionization (ESI) modes. The PILs of FHD in two ESI modes were created based on the phytochemical knowledge of four component drugs and mass defect filtering, which ultimately could obtain 316 and 258 targeted masses, respectively, from the full-scan MS1 data. Interestingly, the additional inclusion of PILs in HDDDA could improve the coverage on the target components by 12% (ESI–) and 48% (ESI + ). Structural elucidation was performed by in-house database-driven automatic peak annotation using UNIFITM. We could identify or tentatively characterize 203 components from FHD, involving 25 alkaloids, 86 flavonoids, 48 triterpenoids (saponins), 16 lactones, and 28 others). It is the first report regarding the method development of HDDDA that targets the global TCM components characterization, and the findings obtained would benefit the quality control and the secondary development of FHD.
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2. Materials and methods
2.1. Reagents and chemicals
In total, 62 compounds (the chemical structures are given in Fig. 1 and the detainled information offered in Table S1, as Supplementary Materials) involving 16 flavonoids (numberred as 1–16), 15 alkaloids (17–31), 7 saponins (32–38), and 24 others (39–62), purchased from Chengdu Desite Biotechnology Co., Ltd. (Chengdu, China), were used as the reference compounds in this work.
Fig. 1. Chemical structures of the 62 reference compounds.
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https://doi.org/10.1016/j.arabjc.2021.103087
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