MAIN GROUP CHEMISTRY
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2022
·Vol. 21
·期 1
·315-328
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IF 0.641
Jiang Wen,Zhou Xiaohua,Ni Ke
Soxhlet extraction method was used to extract imperatorin from Angelica dahurica, and the extraction ratio under different extraction condition was optimized to attain the best condition. Then, XAD-16 macroporous resin was selected as the optimal resin to boost the extraction ratio of imperatorin. Afterwards, the higher purity of imperatorin (96.84±0.2%) was separated by preparative HPLC system. Next, the photocatalytic reaction between the above imperatorin and collagen which the highest levels in skin was investigated using UV-vis spectroscopy, amino acid analysis and HPLC analysis. The results showed that imperatorin reacted with collagen only under ultraviolet light which caused the denaturation of collagen, and three new products were generated. The ultraviolet products were isolated by preparative HPLC system and separately detected by high-resolution mass spectrum. The possible UV photocatalytic reaction mechanism between imperatorin and collagen is that ultraviolet light induces the increase of the activity of the imperatorin to react with the tyrosine in the collagen, resulted in the denaturation of collagen and reestablish of the normal epidermal tissue in skin.
研究领域:
药理学
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生物化学
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DOI
高影响因子
PHYTOTHERAPY RESEARCH
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2025
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IF 6.3
Jingyi Hu,Feng Xu,Lei Zhu,Yuan Cui,Ryan Au,Yanan Li,Yiheng Tong,Hong Shen
Angelica dahurica radix (ADR), the root of the botanical family Apiaceae (genus Angelica , species Angelica dahurica ( Hoffm .)), has been used to treat colitis in clinical practice. The immunomodulatory effects of ADR are attributed to its polysaccharides (RP). However, its mechanism of action has not been elucidated. In this study, RP's structure was determined through nuclear magnetic resonance analysis. Dextran sulfate sodium-induced colitis in mice was utilized to assess the therapeutic efficacy of RP, while experiments involving fecal microbiota transplantation (FMT) and antibiotic treatment were performed to investigate the contribution of gut microbiota to RP's protective function. Non-targeted metabolomics was utilized to identify potential targets for elucidating the underlying mechanisms. RP is likely composed of (→4)-α-D-Glcp-(1→ and →4)-α-D-Galp-(1→). It effectively alleviated DSS-induced colitis by restoring the balance of the gut microbial community, a finding validated through FMT and antibiotic intervention experiments. Imidazole propionate (ImP) emerged as a potential target for RP's efficacy in treating colitis, which inhibits the activation of peroxisome proliferator-activated receptor gamma (PPAR-γ). Our findings suggest that RP may confer protection against colitis by activating the PPAR-γ signaling pathway through alleviating the constraint imposed by ImP.
研究领域:
药理学
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微生物学
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免疫学
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DOI
PubMed
高影响因子
International Journal of Nanomedicine
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2018
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IF 4.37
Hongwei Lin,Qingchun Xie,Xin Huang,Junfeng Ban,Bo Wang,Xing Wei,Yanzhong Chen,Zhufen Lu
Aim The aim of this work was to develop a novel vesicular carrier, ultradeformable liposomes (UDLs), to expand the applications of the Chinese herbal medicine, imperatorin (IMP), and increase its transdermal delivery.Methods In this study, we prepared IMP-loaded UDLs using the thin-film hydration method and evaluated their encapsulation efficiency, vesicle deformability, skin permeation, and the amounts accumulated in different depths of the skin in vitro. The influence of different charged surfactants on the properties of the UDLs was also investigated.Results The results showed that the UDLs containing cationic surfactants had high entrapment efficiency (60.32%±2.82%), an acceptable particle size (82.4±0.65 nm), high elasticity, and prolonged drug release. The penetration rate of IMP in cationic-UDLs was 3.45-fold greater than that of IMP suspension, which was the highest value among the vesicular carriers. UDLs modified with cationic surfactant also showed higher fluorescence intensity in deeper regions of the epidermis.Conclusion The results of our study suggest that cationic surfactant-modified UDLs could increase the transdermal flux, prolong the release of the drug, and serve as an effective dermal delivery system for IMP.
研究领域:
药学
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药物递送系统
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中药
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DOI
PubMed
高影响因子
JOURNAL OF CHROMATOGRAPHY A
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2025
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IF 4
Qian Li,Yan-Qiong Luo,Han Zhang,Yu-Jiao Hou,Aleeza Jamil,Wen-jing Li,Bo Hong,Chun-Jie Zhao
Coumarin is an important natural compound in Angelica dahurica that has high value in food, cosmetics, and medicine. In this study, a multitemplate magnetic molecular-imprinted polymer (MMIP) was synthesized via surface imprinting using Fe 3 O 4 @SiO 2 -C=C nanoparticles as carriers and imperatorin, isoimperatorin and oxypeucedanin as templates. The products were characterized by FT-IR spectroscopy, BET adsorption, SEM, TGA, VSM, and XRD. The adsorption performance was evaluated by dynamic, static, and selective adsorption and repeated experiments. The results showed that the MMIP was superior to the magnetic non-imprinted polymer (MNIP) in terms of adsorption capacity and morphological characteristics and was highly reusable. This MMIP can be reused 6 times. Under optimal conditions, the three coumarins of Angelica dahurica were efficiently separated and purified, with an adsorption capacity of 98.18 mg/g and a spiked recovery rate of 96.97-98.69%, and the purity could reach 87-96%. The linear ranges of the methods for imperatorin, isoimperatorin, and oxypeucedanin are 0.0625-1.00 mg/mL, respectively, showing a good correlation (R 2 > 0.9984). Compared with traditional extraction methods, this method has excellent adsorption and extraction performance in the selective separation and purification of three coumarins and provides a new strategy for the efficient extraction of coumarins from Angelica dahurica even other matrix.
研究领域:
药学
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分析化学
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高分子科学
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天然产物提取
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材料科学
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DOI
PubMed
高影响因子
BIOCHEMICAL PHARMACOLOGY
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2020
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IF 4.96
Nan Wang,Jue Wang,Yongjing Zhang,Yingnan Zeng,Shiling Hu,Haoyun Bai,Yajing Hou,Cheng Wang,Huaizhen He,Langchong He
Background Allergic asthma is a common inflammatory lung disease associated with complex pathogenesis. Mast cell (MC) is one of the key drivers of allergic asthma, Mas-related G protein-coupled receptor X2 (MRGPRX2) on the MC could mediate MC activation and trigger a pseudo-allergic reaction. Imperatorin (IMP), the main active compound of Radix Angelicae Dahuricae , has been reported to exert various pharmacological effects. In this study, we focused on the therapeutical mechanism of IMP on MRGPRX2-induced pseudo-allergy and allergic asthma. Methods We examined the effect of IMP on MRGPRX2 related mast cell activation in mouse peritoneal MC (MPMC), Human Laboratory of Allergic Disease 2 MCs (LAD2 cells) and Mrgprx2 -expressing HEK293 cells. Molecular docking and Surface plasmon resonance (SPR) were taken to reveal the binding character between IMP and MRPGRX2. MRGPRX2 downstream proteins were also detected by western blotting . IgE-independent responses was evaluated by using passive cutaneous anaphylaxis (PCA) and active systemic anaphylaxis (ASA) models. The therapeutic effect of IMP on asthma was evaluated by a lung inflammation mouse model which was induced by ovalbumin (OVA). Results IMP was found to reduce substance P (SP) induced calcium flux and suppressed degranulation of MC. SP can promote the phosphorylation of ERK and CamKII, which regulates the synthesis of inflammatory factors such as MIP-2 and TNF-α in MC. In vivo assays revealed that IMP can mitigate SP-induced mouse PCA and ASA. IMP could also mitigate lung inflammation in an OVA induced mice model by inhibiting MC activation in the lung tissue. Furthermore, IMP binds well to MRGPRX2 protein. The binding constant ( K D ) is 4.48 ± 0.49 × 10 −7 M. The data suggeste that IMP is a novel inhibitor of MRGPRX2 to treat allergic asthma.
研究领域:
药理学
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免疫学
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过敏
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呼吸系统疾病
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DOI
PubMed
高影响因子
Journal of Oleo Science
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2022
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IF 1.628
Chunlian Li,Qiuyang Cai,Xianyi Wu,Zekai Tan,Lewen Yao,Shiyuan Huang,Weicheng Zhang,Zhengyi Hong,Zhuoyu Chen,Lanyue Zhang
Umbelliferae plants, which are widely used as traditional Chinese medicine because of their characteristics of relieving rheumatism, alleviating fever, circulating blood and easing pain. This experimental study was based on ear edema model caused by 12-O-tetracycline-propylphenol-13-acetic acid (TPA) in mice and compared with the Ibuprofen (Ib) group. Gas chromatography-mass spectrometry (GC-MS) was used to analyse the composition of the essential oils from the four studied Umbelliferae plants (Angelica sinensis (Oliv.) Diels, A. dahurica (Hoffm.) Benth. & Hook.f. ex Franch. & Sav., A. pubescens Maxim and Foeniculum vulgare Mill.). Biologically active components in volatile oils from the four studied Umbelliferae plants were evaluated. The expression levels of inflammatory cytokines Tumor Necrosis Factor-α (TNF-α), Cyclooxygenase-2 (COX-2), Interleukin-6 (IL-6) and RelA (p65) in mouse skin were determined by immunohistochemical method. The refractive index of the four essential oils was calculated. A total of 239 compounds were identified by GC-MS from the four studied plants, and the main constituents were osthole (44.61%, APEOs), obepin (0.59%, APEOs & 86.58%, FVEOs), undecanol (8.58%, ADEOs), α-muurolene (7.95%, ADEOs) and cis-anethol (9.11%, ADEOs). E-ligustilide (0.14%, APEOs & 81.14%, ASEOs), (-)-spathulenol (0.08%, FVEOs & 1.21%, ASEOs), (-)-terpinen-4-ol (4.91%, FVEOs), 2-butylthiolane (5.76%, APEOs) and α-bisabolol (3.80%, APEOs). This study showed that all the essential oils from the four studied Umbelliferae plants contained various lactones, including ligustrongolactone, trans-anisol and imperatorin. According to the results of the TPA induction test in the mouse ear edema model, the essential oils of four Umbelliferae plants reduced the levels of inflammatory cytokines TNF-α, COX-2, IL-6 and p65. All of them showed extraordinary biological activity in anti-inflammatory, so they have potential application value for biomedical products, pharmaceutical preparations, natural functional nutrients and cosmetic additives.
研究领域:
药理学
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药物化学
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中医药学
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免疫学
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DOI
PubMed
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
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2020
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IF 3.69
Jingyi Hu,Hai Huang,Yuan Che,Chujie Ding,Lu Zhang,Yun Wang,Haiping Hao,Hong Shen,Lijuan Cao
Ethnopharmacological relevance Inflammatory bowel disease (IBD) is a chronic and relapsing inflammatory disease of the gastrointestinal tract, consisting of ulcerative colitis (UC) and Crohn's disease (CD). Gut microbiota and their metabolites may play a role in the pathogen of IBD, especially of the UC. Qingchang Huashi Formula (QHF), a traditional Chinese medicine formula, has shown therapeutic effect on treating UC based on the clinical practice without clear pharmacological mechanism. Aim of the study The aim of this study was to clearly define the effect of QHF and its components, Baitouweng (PBR) and Baizhi (ADR) on treating UC. Materials and Methods Pharmacodynamic effects of QHF and single herb were evaluated in dextran sulfate sodium (DSS) induced acute or chronic colitis mice. Body weight loss, disease activity index (DAI) and colon length were estimated. Histological changes were observed by H&E staining. The number and abundance of gut microbiota were measured with 16S rRNA sequencing. LC-MS and GC-MS were used to detect the concentration of metabolites (e.g., bile acids (BAs) and short chain fatty acids (SCFAs)). The goblet cell was observed by Alcian blue/periodic acid-Schiff (AB/PAS) straining and the crypt stem cell was estimated by immunohistochemical analyses. The colorectal tissues were used to detect levels of IL-1β, IL-6 and TNF-α by ELISA or qRT-PCR. The expression of NLRP3, Caspase 1 and IL-1β were examined by western blotting . Results QHF significantly inhibited colitis, protected mice from the loss of body weight and colon shorten. Comparatively, ADR and PBR showed strong efficacy in inhibiting DSS-induced colitis. We verified that while ADR was responsible for QHF's effect on maintaining gut microbiota homeostasis and metabolism, PBR was more prominent in keeping crypt stem cells proliferation and colonic goblet cells function. Moreover, we demonstrated that the alleviation of colitis by QHF was associated with the restoration of gut microbiota-metabolism homeostasis, protection of intestinal epithelial barrier and regulation of NLRP3/IL-1β pathway. Conclusions The finding of the present study suggested that QHF is curative in DSS-induced colitis by restoring gut microbiota-metabolism homeostasis and goblet cells function. An optimized QHF was constituted by ADR and PBR, which showed comparable efficacy on colitis to that of QHF. Our work probed out the active constitutes as well as the relevant pharmacological mechanisms of QHF, shedding light on potential new drug combination for the treatment of IBD.
研究领域:
药理学
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免疫学
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胃肠病学
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微生物学
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中医
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DOI
PubMed
高影响因子
ACS Applied Nano Materials
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2024
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IF 5.3
Qiuxiang Li,Guowei Zhao,Fengling Wu,Xilan Tang,Zhenggen Liao,Xinli Liang,Wei Dong
Imperatorin (IMP) has demonstrated potential in reversing drug resistance in various tumor cells; however, its limited clinical application and development are attributed to its poor water solubility and low bioavailability. The current work is intended to enhance the oral bioavailability of IMP and its efficacy in overcoming tamoxifen (TAM) resistance in breast cancer cells. We employed mPEG–PLLA and Cremophor RH60 (RH60) to prepare imperatorin nanomicelles (IMP-RH60/mPEG–PLLA). The freeze-dried powder of IMP-RH60/mPEG–PLLA demonstrated a porous structure, and upon reconstitution, the resulting solution exhibited clarity and transparency. The particle size was measured to be 25.48 ± 0.92 nm, with a zeta potential of −5.50 ± 1.06 mV. The encapsulation efficiency was determined to be 85.78 ± 0.84%, while the drug loading was found to be 2.66 ± 0.03%. In comparison to the active pharmaceutical ingredients (APIs) of IMP, IMP-RH60/mPEG–PLLA exhibited a significant increase in in vitro release, improved bioavailability in rats, and enhanced uptake by MCF-7/TAM cells. The coadministration of IMP-RH60/mPEG–PLLA and TAM effectively inhibited the proliferation, colony formation, migration, and invasion of MCF-7/TAM cells. This outcome could potentially be attributed to the downregulation of GST-π and MDR1 drug resistance genes, consequently augmenting the susceptibility of MCF-7/TAM cells to TAM. An experimental model of BALB/c nude xenograft, consisting of human breast cancer cells resistant to tamoxifen (TAM), was established in order to assess the potential in vivo reversal of TAM resistance through the use of IMP-RH60/mPEG–PLLA. The growth of xenografts was inhibited by IMP-RH60/mPEG–PLLA, and it induced apoptosis in tumor tissues through the downregulation of Ki-67, GST-π, and MDR1 gene expression. The findings indicated that the utilization of IMP-RH60/mPEG–PLLA micelles resulted in an enhancement of IMP’s bioavailability and its efficacy in overcoming TAM resistance.
研究领域:
药学
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肿瘤学
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纳米技术
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药理学
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DOI
高影响因子
Journal of Natural Medicines
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2024
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IF 2.5
Gao Chong,Hu Zhong-He,Cui Zhen-Yu,Jiang Yu-Chen,Dou Jia-Yi,Li Zhao-Xu,Lian Li-Hua,Nan Ji-Xing,Wu Yan-Ling
Angelica dahurica (A. dahurica) has a wide range of pharmacological effects, including analgesic, anti-inflammatory and hepatoprotective effects. In this study, we investigated the effect of A. dahurica extract (AD) and its effective component bergapten (BG) on hepatic fibrosis and potential mechanisms. Hepatic fibrosis was induced by intraperitoneal injection with carbon tetrachloride (CCl 4 ) for 1 week, and mice were administrated with AD or BG by gavage for 1 week before CCl 4 injection. Hepatic stellate cells (HSCs) were stimulated by transforming growth factor-β (TGF-β) and cultured with AD, BG, GW4064 (FXR agonist) or Guggulsterone (FXR inhibitor). In CCl 4 -induced mice, AD significantly decreased serum aminotransferase, reduced excess accumulation of extracellular matrix (ECM), inhibited caspase-1 and IL-1β, and increased FXR expressions. In activated HSCs, AD suppressed the expressions of α-SMA, collagen I, and TIMP-1/MMP-13 ratio and inflammatory factors, functioning as FXR agonist. In CCl 4 -induced mice, BG significantly improved serum transaminase and histopathological changes, reduced ECM excessive deposition, inflammatory response, and activated FXR expression. BG increased FXR expression and inhibited α-SMA and IL-1β expressions in activated HSCs, functioning as GW4064. FXR deficiency significantly attenuated the decreasing effect of BG on α-SMA and IL-1β expressions in LX-2 cells. In conclusion, AD could regulate hepatic fibrosis by regulating ECM excessive deposition and inflammation. Activating FXR signaling by BG might be the potential mechanism of AD against hepatic fibrosis.
研究领域:
药理学
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肝病学
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分子生物学
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DOI
PubMed
高影响因子
ANALYTICA CHIMICA ACTA
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2022
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IF 6.911
Hui Ouyang,Hongwei Yuan,Junyi Huang,Jiaxin Xian,Wenwen Wang,Zhifeng Fu
In view of the optimal catalytic efficiency (∼100%), single-atom site catalysts are being widely exploited in a range of areas including organic synthesis, energy conversion, environmental remediation, biotherapy, etc. However, low loading ratio of the unitary active sites on single-atom site catalysts dramatically hinders the remarkable improvement of their catalytic activity . Hereby, a facile low-temperature reduction protocol was adopted for synthesizing CoN 4 -supported Co 2 N metal clusters on graphitic carbon nitride , which show the remarkably superior chemiluminescent (CL) catalytic capacity than some reported pure single-atom site catalysts. Nitrogen-encapsulated Co 2 N clusters coupled with isolated Co–N 4 moieties (Co 2 [email protected] –N 4 ) endowed the synergetic catalysts with high Co content of 53.2 wt%. Through X-ray absorption spectroscopy, the synergetic active sites (Co 2 [email protected] –N 4 ) afforded the CoN 4 -supported Co 2 N clusters with the remarkable catalytic activity for accelerating the decomposition of H 2 O 2 to produce extensive superoxide radical anion rather than singlet oxygen or hydroxyl radical . Therefore, the CoN 4 -supported Co 2 N clusters possessed the superb enhancement effect on luminol-H 2 O 2 CL reaction by ∼22829 times. The CoN 4 -supported Co 2 N clusters were utilized as signal probes to establish a CL immunochromatographic assay (ICA) platform for quantitating mycotoxins . Herein, aflatoxin B1 was employed as a mode analyte and the limit of detection was as low as 0.33 pg mL −1 (3σ). As a proof-of-principle work, the developed ICA protocol was successfully employed on the detection of aflatoxin B1 spiked in Angelica dahurica and Ganoderma lucidum with acceptable recoveries of 84.0–107.0%. The ideal practicability of the work elucidates that CoN 4 -supported Co 2 N clusters showed a new perspective for developing the sensitive CL biosensing.
研究领域:
分析化学
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材料科学
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生物化学
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食品安全
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产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）