Frontiers in Chemistry
·
2022
·
IF 5.545
Jiang Zhehui,Wang Tianhao,Zhang Kaixue,Zhang Meiqi,Ma Ling,Ren Weichao,Bao Yihong,Ma Wei
Light quality consists of a spectrum of different bands, which not only affects plant, development, and primary metabolism but also affects the secondary metabolism of plants. It is an important factor affecting the content of active components of medicinal plants. The A. paniculata seedlings planted in the laboratory, as materials, were tested with red light, far red light, blue light, and ultraviolet light separately. The study assays the content of six main chemical components separately by LC-MS, observes the changes in the content, and analyzes the relationship between the light quality and the active ingredient of A. paniculata. Using the ointment yield and pH value, the fingerprint analysis method of A. paniculata standard decoction was established, and we discussed the selection of index components of A. paniculata standard decoction. It was suggested to select andrographolide as the index component. It will provide a theoretical basis for the large area cultivation of A. paniculata and optimize the quality of medicinal materials to ensure the quality of standard decoction.
研究领域:
生药学
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植物生理学
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药物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
MOLECULAR NEUROBIOLOGY
·
2024
·
IF 4.6
Zhou Xuebin,Li Jinhua,Quan Shengli,Zhang Xinyue,Gu Lili,Hu Min,Huang Wenhai,Li Qin
The pathological and physiological studies of Alzheimer’s disease (AD) have been in-depth, and apolipoprotein E4 (ApoE4) has been proven to be highly correlated with AD, and clinical and experimental data show that ApoE4 can cause blood–brain barrier (BBB) injury, and the change of BBB permeability is an important factor affecting the development of AD. Andrographolide (Andro), as the active component of the natural plant Andrographis paniculata , has been proven to have anti-inflammatory and antioxidant effects, which have potential neuroprotective effects. To verify the protective effect of Andro on BBB in a short term, our research group used atorvastatin (Atorva)-mediated zebrafish brain injury model and the ApoE4-mediated cell co-culture model of BBB injury to explore the protective effects and mechanisms of Andro on BBB injury. Studies have shown that Andro can inhibit the activation of CypA/NF-κB/MMP-9 signaling pathway and has achieved the effect of antagonizing the inhibition of ApoE4 on intercellular tight junction proteins (occludin, claudin-5, and ZO-1). At the same time, Andro can inhibit the secretion of cell adhesion molecules (VCAM-1 and ICAM-1) in cells, thereby delaying the occurrence and progression of neuroinflammation and playing a protective role in BBB. In conclusion, Andro is a potent natural product which can protect the blood–brain barrier.
研究领域:
神经科学
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药理学
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分子生物学
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神经退行性疾病
✓ 已验证
DOI
PubMed
高影响因子
PeerJ
·
2024
·
IF 2.3
Zhaohong Wang,Hui Chen,Xufan Cai,Heqi Bu,Shengzhang Lin
Background Andrographolide (Andro), an extract of Andrographis paniculate (Burm.f.) Wall. ex Nees (Acanthaceae), possesses diverse biologically active properties. However, the precise mechanisms and effects of Andro on pancreatic cancer (PC) remain unclear. Methods The cytotoxic potential of Andro and underlying mechanism towards PC cells was investigated through in vitro experiments and a xenograft mouse model. PC cells were first subjected to varying concentrations of Andro. The reactive oxygen species (ROS) was assessed using flow cytometry and DCFH-DA staining. The apoptosis rate was detected by flow cytometry. Additionally, western blot was applied to evaluate the expression levels of cleaved-caspase-3, DJ-1, LC3-I, LC3-II, and p62. To further elucidate the involvement of ROS accumulation and autophagy, we employed N-acetylcysteine as a scavenger of ROS and 3-Methyladenine as an inhibitor of autophagy. Results Andro demonstrated potent anti-proliferative effects on PC cells and induced apoptosis, both in vitro and in vivo . The cytotoxicity of Andro on PC cells was counteracted by DJ-1 overexpression. The reduction in DJ-1 expression caused by Andro led to ROS accumulation, subsequently inhibiting the growth of PC cells. Furthermore, Andro stimulated cytoprotective autophagy, thus weakening the antitumor effect. Pharmacological blockade of autophagy further enhanced the antitumor efficacy of Andro. Conclusion Our study indicated that ROS accumulation induced by the DJ-1 reduction played a key role in Andro-mediated PC cell inhibition. Furthermore, the protective autophagy induced by the Andro in PC cells is a mechanism that needs to be addressed in future studies.
研究领域:
肿瘤学
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药理学
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细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2023
·
IF 5.8
Sicheng Yao,Naiying Chen,Xinxing Sun,Qiuyue Wang,Mingming Li,Yang Chen
Particle size is a key parameter to determine the capacity of nanoparticles to overcome the skin barrier; however, such effect and the possible mechanism remain only partially understood for nanosuspensions. In this work, we examined the skin delivery performance of andrographolide nanosuspensions (AG-NS) ranging in diameter from 250 nm to 1000 nm and analyzed the role of particle size in influencing their ability of skin penetration. The AG-NS with particle sizes of about 250 nm (AG-NS250), 450 nm (AG-NS450), and 1000 nm (AG-NS1000) were successfully prepared by ultrasonic dispersion method and characterized by transmission electron microscopy . The drug release and penetration via the intact and barrier-removed skin were compared by the Franz cell method, and the related mechanisms were probed using laser scanning confocal microscopy (LSCM) via visualization of penetration routes and histopathological study via observation of structural change of the skin. Our finding revealed that drug retention in the skin or its sub-layers was increased with the reduction of particle size, and the drug permeability through the skin also exhibited an obvious dependence on the particle size from 250 nm to 1000 nm. The linear relationship between the in vitro drug release and ex vivo permeation through the intact skin was well established among different preparations and in each preparation, indicating the skin permeation of the drug was mainly determined by the release process. The LSCM indicated that all these nanosuspensions could deliver the drug into the intercellular lipid space, as well as block the hair follicle in the skin, where a similar size dependence was also observed. The histopathological investigation showed that the formulations could make the stratum corneum of the skin loose and swelling without severe irritation. In conclusion, the reduction of particle size of nanosuspension would facilitate topical drug retention mainly via the modulation of drug release.
研究领域:
药剂学
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皮肤科学
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纳米技术
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Chinese Journal of Natural Medicines
·
2018
·
IF 1.991
Qi-Qing LI,Jian ZHANG,Ji-Hua LIU,Bo-Yang YU
Andrographis paniculata (Burm. f.) Nees (AP) is commonly used for the treatment of many infectious diseases and has been cultivated widely in Asian countries, and has been included in United States Pharmacopoeia as a dietary supplement, but the cultivars of A. paniculata are not abundant due to its self-pollinated. With the aims to enrich AP resources and provide materials for after breeding we explored the polyploidy induction. Different explants, colchicine concentration, and treatment time were tested. After identification by flow cytometry, eleven polyploid plants with different morphologic traits were obtained. The agronomic traits and andrographolide concentration of the polyploids were improved greatly. One of the polyploids (serial 3–7) was chosen for further study. The traits of the second and third generation polyploids (serial 3–7) were stable. Compared with the normal plants, the seeds (2nd generation) weight increased by 31%, and the andrographolide concentration of the leaves increased by 14% (2nd) and 28% (3rd). In conclusion, AP autopolyploids with different morphologic traits were established successfully for the first time, and the polyploids induction might be effective for crop improvement of AP.
研究领域:
植物学
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药用植物研究
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遗传学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CARBOHYDRATE POLYMERS
·
2025
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IF 12.5
Xiaoyi Zhang,Peixia Luo,Jiaming Wang,Lei Yang,Zipei Pang,Shufeng Chen,Yi Zhou,Linghao Qin
Cellulose derivatives play important roles in the development of pharmaceutical oral solid formulations. Owing to their high molecular weight and functional groups, these polymers can interact with water-insoluble drug crystals, influencing not only the drug's physicochemical properties but also its absorption efficiency. In this study, an anticrystallization experiment was designed to compare the inhibitory effects of cellulose derivatives (methylcellulose (MC), hydroxypropyl cellulose (HPC) and hydroxypropyl methyl cellulose (HPMC)) with those of polyvinylpyrrolidone (PVP) and poloxamer (F68) on the crystallization of model drugs (andrographolide, AG). Both in vitro characterization experiments and in vivo pharmacokinetic studies were conducted to evaluate the interaction patterns between andrographolide crystals and polymers. The results indicated that cellulose derivatives exhibited stronger anticrystallization effects, with HPMC showing the most pronounced interaction with drug crystals among all the tested polymers. HPMC significantly prolonged the crystallization time and increased the degree of supersaturation. By adsorbing onto specific crystal surfaces, HPMC was able to modulate the crystal growth orientation, reduce the contact angle, and improve the wettability of drug crystals. Furthermore, andrographolide crystals adsorbed by HPMC exhibited rapid in vitro drug release behavior and upgraded in vivo absorption efficiency, demonstrating its potential to improve the utilization of water-insoluble drugs.
研究领域:
药剂学
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药物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Asian Journal of Pharmaceutical Sciences
·
2021
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IF 6.598
Haoshi Gao,Yan Su,Wei Wang,Wei Xiong,Xiyang Sun,Yuanhui Ji,Hua Yu,Haifeng Li,Defang Ouyang
Current formulation development strongly relies on trial-and-error experiments in the laboratory by pharmaceutical scientists, which is time-consuming, high cost and waste materials. This research aims to integrate various computational tools, including machine learning, molecular dynamic simulation and physiologically based absorption modeling (PBAM), to enhance andrographolide (AG) /cyclodextrins (CDs) formulation design. The lightGBM prediction model we built before was utilized to predict AG/CDs inclusion's binding free energy. AG/γ-CD inclusion complexes showed the strongest binding affinity, which was experimentally validated by the phase solubility study. The molecular dynamic simulation was used to investigate the inclusion mechanism between AG and γ-CD, which was experimentally characterized by DSC, FTIR and NMR techniques. PBAM was applied to simulate the in vivo behavior of the formulations, which were validated by cell and animal experiments. Cell experiments revealed that the presence of D-α-Tocopherol polyethylene glycol succinate (TPGS) significantly increased the intracellular uptake of AG in MDCK-MDR1 cells and the absorptive transport of AG in MDCK-MDR1 monolayers. The relative bioavailability of the AG-CD-TPGS ternary system in rats was increased to 2.6-fold and 1.59-fold compared with crude AG and commercial dropping pills, respectively. In conclusion, this is the first time to integrate various computational tools to develop a new AG-CD-TPGS ternary formulation with significant improvement of aqueous solubility, dissolution rate and bioavailability. The integrated computational tool is a novel and robust methodology to facilitate pharmaceutical formulation design.
研究领域:
药剂学
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计算生物学
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药物化学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Pharmacological Reports
·
2020
·Vol. 72
·期 2
·400-417
·
IF 2.754
Li Yingxue,Jiang Bo,Wang Ruiyin,Wang Jingyun,Li Yachen,Bao Yongming
Background Tanshinone IIA (Tan IIA) and andrographolide (Andro) are natural compounds that are reported to exhibit anticancer activities against various types of cancers. The aim of this study is to evaluate the synergistic anticancer effects of the combination of Tan IIA and Andro, and to investigate the mechanisms of pharmacological effect and their potential applications as an anticancer therapy in clinics.
Methods The anticancer effects of the combination of Tan IIA and Andro on MCF7, SMMC7721, and BGC823 cells were explored. The apoptosis of the cancer cells was determined by MTT and AV-PI dual stain assays. The intracellular GSH level was measured by DTNB assay, and the intracellular levels of reactive oxygen species (ROS) were examined by flow cytometry. The expression of the proteins in the apoptosis pathway was determined by immunobloting. Results The combination of Tan IIA and Andro exhibited significant synergistic anticancer effects against cancer cells, especially at low concentrations. Andro reacted with the thiol group of intracellular GSH, thus disrupting the GSH redox cycle and eventually increasing the level of intracellular ROS. Tan IIA triggered p53 responses and apoptosis by binding to the DNA of cancer cells. The crosstalk between ROS and p53 exhibited a synergistic effect on the apoptosis of cancer cells. Conclusion The combination of Tan IIA and Andro showed significant synergistic effects on cancer cell apoptosis by promoting crosstalk between ROS and p53, providing a novel and effective combination that has the potential to be applied in clinical anticancer therapy. Graphic abstract
研究领域:
肿瘤学
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药理学
·
细胞生物学
✓ 已验证
DOI
PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2023
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IF 5
Yupeng Feng,Peifu Xiao,Zixu Liu,Mei Li,Qingqing Wang,Tian Yin,Yu Zhang,Haibing He,Jingxin Gou,Yanjiao Wang,Xing Tang
Andrographolide (AND) and 14-deoxy-11, 12-dide-Hydroandrographolide (dehydroandrographolide, 14-DDA) are widely utilized traditional Chinese medicines for the treatment of inflammation. However, allergic reactions continue to be a concern. This research aimed to reduce allergic reactions and enhance the anti-inflammatory properties of 14-DDA by means of a liposome delivery system. To overcome the low encapsulation efficiency of conventional 14-DDA liposomes, a new 14-DDA derivative, dehydroandrographolide-divaline ester hydrochloride (DADH), was created by introducing valine groups at the C-3 and C-19 positions. DADH liposomes (DADH-lip) achieved high encapsulation efficiency (over 90%) via an ethanol injection method - pH gradient method. The lowest IC 50 value (16.34 μg/mL) of DADH-lip against P815 cells indicated that DADH-lip significantly reduced allergic reactions. In addition, DADH solution (DADH-sol) and DADH liposome decreased the amount of histamine released at both the high (1 mg/mL) and low (20 μg/mL) concentration dosages compared to the commercially available preparation. DADH-lip and DADH-sol also had significant effects in the LPS-induced RAW 264.7 macrophage model. In vivo anti-inflammatory results demonstrated that, compared to commercially available preparations, DADH-lip has a superior therapeutic effect and significantly reduces rat paw swelling. Collectively, DADH-lip with high encapsulation efficiency reduced allergic reactions significantly and enhanced therapeutic effect, suggesting that it may be a promising platform for inflammatory therapy.
研究领域:
药理学
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中药学
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纳米医学
✓ 已验证
产品关联
DOI
高影响因子
FISH & SHELLFISH IMMUNOLOGY
·
2025
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IF 3.9
Jingya Li,Mingyang Xue,Chen Xu,Nan Jiang,Yiqun Li,Yuding Fan,Yong Zhou,Yan Meng
It is well-established that Largemouth bass ranavirus (LMBRaV) induces viral ulcerative syndrome, a highly transmissible and lethal viral disease afflicting largemouth bass aquaculture. Given the urgent need for available prevention and control methods, this study evaluated the antiviral activities of fifteen naturally occurring compounds derived from herbal medicines against LMBRaV using an in vitro cell model. Andrographolide (Andro) was one of the substances that was evaluated and showed highly effective anti-LMBRaV activity of a 99.2 % maximal inhibition rate of at 20 mg/L dosage. Mechanistic investigation revealed Andro prevented viral entry and directly inactivated the virus. Ultrastructural observations and fluorescence staining further supported Andro's protective effects on EPC cells from LMBRaV invasion. In vivo experiments demonstrated Andro's efficacy in reducing mortality rates in LMBRaV-infected largemouth bass by 61.54 % and significantly lowering the viral load. Additionally, Andro upregulated antiviral genes such as ifn-γ , irf-3 , and mx , indicating its immunomodulatory properties. Histopathological analysis revealed that Andro alleviated tissue damage of liver, spleen, and kidney in the infected fish. Andro also changed the microbiotic composition of gut by increasing the amounts of good bacteria and reducing amounts of bad bacteria. These findings collectively highlight Andro's substantial antiviral and immunomodulatory potential, suggesting its promising application as a natural compound for combating LMBRaV infections in largemouth bass aquaculture and potentially other aquatic animal diseases.
研究领域:
水产养殖学
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病毒学
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免疫学
✓ 已验证
DOI
PubMed
高影响因子
Frontiers in Immunology
·
2024
·
IF 5.7
Yue Zhongqun,Zhu Yue,Chen Teng,Feng Tingting,Zhou Ying,Zhang Jiaojiao,Zhang Ning,Yang Jing,Luo Gang,Wang Zuhua
Background: Vitamin E, which is also known as tocopherol, is a compound with a polyphenol structure. Its esterified derivative, Vitamin E succinate (VES), exhibits unique anticancer and healthcare functions as well as immunomodulatory effects. Natural polysaccharides are proved to be a promising material for nano-drug delivery systems, which show excellent biodegradability and biocompatibility. In this study, we employed a novel bletilla striata polysaccharide-vitamin E succinate polymer (BSP-VES) micelles to enhance the tumor targeting and anti-colon cancer effect of andrographolide (AG).Methods: BSP-VES polymer was synthesized through esterification and its structure was confirmed using 1H NMR. AG@BSP-VES was prepared via the dialysis method and the drug loading, entrapment efficiency, stability, and safety were assessed. Furthermore, the tumor targeting ability of AG@BSP-VES was evaluated through targeted cell uptake and in vivo imaging. The antitumor activity of AG@BSP-VES was measured in vitro using MTT assay, Live&Dead cell staining, and cell scratch test.Results: In this study, we successfully loaded AG into BSP-VES micelles (AG@BSP-VES), which exhibited good stability, biosafety and sustained release effect. In addition, AG@BSP-VES also showed excellent internalization capability into CT26 cells compared with NCM460 cells in vitro. Meanwhile, the specific delivery of AG@BSP-VES micelles into subcutaneous and in-situ colon tumors was observed compared with normal colon tissues in vivo during the whole experiment process (1–24 h). What’s more, AG@BSP-VES micelles exhibited significant antitumor activities than BSP-VES micelles and free AG.Conclusion: The study provides a meaningful new idea and method for application in drug delivery system and targeted treatment of colon cancer based on natural polysaccharides.
研究领域:
药学
·
肿瘤学
·
生物材料学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PHARMAZIE
·
2018
·Vol. 73
·期 10
·594-597
·
IF 1.016
Wu Bo,Chen Xi,Zhou Ying,Hu Pingjun,Wu Dan,Zheng Guodong,Cai Yi
Background: Andrographolide (Andro) belongs to the main bioactive ingredients of Andrographis paniculata. Many studies have shown that andro has a variety of pharmacological activities such as anti-inflammatory, anti-bacterial, anti-virus, anti-oxidant, immune regulation
and liver protective effects. Moreover andro has been reported to have anticancer activity in multiple types of cancer, including gastric cancer, breast cancer, lung cancer and so on. However, there is no report about the effect of andro on the human NPC cell line C666-1 and the molecular
mechanisms of andro-mediated apoptosis in C666-1 cells remain to be clarified. Methods: Cell proliferation was measured by a CCK8 assay, cell apoptosis rate was evaluated by flow cytometric analysis, and the protein expression of LKB1/AMPK signaling pathways was detected by Western
blotting. Results: Treatment with andro inhibited cell proliferation and induced apoptosis of C666-1 cells. Moreover, andro could activate LKB1-AMPK signaling. We also demonstrated that Ca2+/calmodulin-dependent protein kinase kinaseβ (CaMKKβ) was not involved in
the regulation of andro on AMPK activation in C666-1 Cells. Conclusions: Andro suppressed proliferation and induced apoptosis of C666-1 cells through regulating the LKB1/AMPK/mTOR signal pathway.
研究领域:
肿瘤学
·
药理学
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细胞生物学
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分子生物学
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）