Biomed Research International
·
2021
·
IF 3.411
F. L. Wang,H. Wang,J. H. Wang,D. X. Wang,Y. Gao,B. Yang,H. J. Yang,Y. B. Ji,G. S. Xin
Sophora viciifolia Hance is an edible plant used in traditional Chinese medicine. Sophocarpine, a tetracyclic quinolizidine alkaloid, is one of the most abundant active ingredients in Sophora viciifolia Hance. Here, we study the analgesic and anti-inflammatory effects, as well as the acute toxicity of sophocarpine from Sophora viciifolia Hance in mice. Sophocarpine (20, 40, and 80 mg/kgbw) significantly prolonged the delay period before a hot plate reaction occurred (all ), and the delay before a tail-flick response was induced by a warm bath (; ). Sophocarpine (40, 80 mg/kg) resulted in dose-dependent inhibition of the writhing reaction induced by acetic acid in mice (; , respectively). Sophocarpine (80 mg/kg) reduced the total duration of a formalin-induced pain response (). Sophocarpine prolonged the foot-licking latency of mice after the hot plate reaction, and this effect was antagonized by calcium chloride and enhanced by verapamil. Sophocarpine (20, 40, and 80 mg/kg) significantly inhibited xylene-induced ear edema (; ; , respectively) and the penetration of acetic acid-induced dye into the peritoneal cavity (; ; , respectively). It also reduced the levels of proinflammatory cytokine interleukin (IL)-1β, IL-6, and prostaglandin E2 (, , ) and those of serum nitric oxide (). The results of this study suggest that sophocarpine possesses certain analgesic and anti-inflammatory activities, which may be related to calcium and inhibition of the secretion of inflammatory factors.
研究领域:
药理学
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中药学
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DOI
PubMed
高影响因子
JOURNAL OF NANOPARTICLE RESEARCH
·
2021
·Vol. 23
·期 6
·1-16
·
IF 2.253
Wang Qilong,Liu Jing,Liu Jian,Thant Yaminn,Weng Wen,Wei Chunmei,Bao Rui,Adu-Frimpong Michael,Yu Qingtong,Deng Wenwen,Cao Xia,Toreniyazov Elmurat,Ji Hao,Xu Ximing,Yu Jiangnan
Recently, bisdemethoxycurcumin (BDMC), a constituent of turmeric, has been studied widely in view of their various therapeutic effects, namely anti-oxidant, anti-cancer, anti-diabetic, and anti-inflammatory. Since ancient times, turmeric has been extensively used as a naturally occurring traditional Chinese medicine (TCM) and as a crucial home remedy for treatment of many health problems such as inflammation and pain. However, the action of anti-gouty arthritis and analgesic activity of its constituents, especially BDMC, have not been scientifically reported yet. Despite the various bioactivities of BDMC, its utilization in clinics has been restricted owing to poor solubility and bioavailability. This research aimed at enhancing oral bioavailability and pharmacokinetic of BDMC via liposome formulation which was modified with d -α-tocopherol polyethylene glycol 1000 succinate (TPGS or vitamin E TPGS) and was characterized using various parameters both in vitro and in vivo. Also, the analgesic and anti-gouty activities of BDMC-loaded TPGS-modified liposomes were investigated by assessing pain threshold and serum uric acid level in potassium oxonate–induced hyperuricemic rats. As the result, BDMC-loaded TPGS-modified liposomes were formulated successfully with optimal physiochemical properties such as 75.98 ± 5.46 nm (particle size), 0.246 ± 0.011 (polydispersity index), − 38.21 ± 0.29 mV (zeta potential), 96.98 ± 0.17 (encapsulation efficiency (EE%)), and 4.84 ± 0.0089 (drug loading capacity (DL%)). Moreover, the oral bioavailability of liposomized BDMC was approximately 10-fold greater than free BDMC in vivo and in vitro cumulative release rates in pH 1.2 (78%) and pH 7 (68%) respectively. This significantly improved the sustaining drug effect of BDMC compared with free form. In addition, BDMC-TPGS liposome acted as a xanthine oxidase inhibitor to evidently reduce uric acid level in potassium oxonate–induced hyperuricemic rats and remarkably increase pain threshold capacity and reaction time in hot plate test at a dose-dependent manner. Altogether, BDMC-conjugated TPGS liposome could act as favorable nanocarriers against gouty arthritis and intense pain with prospect of overcoming the limitation of BDMC application.
研究领域:
药剂学
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生物医学
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中药学
✓ 已验证
DOI
高影响因子
INTERNATIONAL IMMUNOPHARMACOLOGY
·
2024
·
IF 4.8
Li Guo,Sai Zhang,Cong Zhang,Shuang Ren,Zihan Zhou,Fengyuan Wang,Yuexuan Wang,Qiqi Chen,Yubing Wang,Wen-Hui Lee,Kui Zhu,Di Qin,Yuanyuan Gao,Tongyi Sun
Inflammatory pain is a chronic pain caused by peripheral tissue inflammation, seriously impacting the patient’s life quality. Cinobufacini injection, as a traditional Chinese medicine injection preparation, shows excellent efficacy in anti-inflammatory and analgesic treatment in patients with advanced tumors. In this study, a novel analgesic peptide CI5 with anti-inflammatory and analgesic bio-functions that naturally presents in Cinobufacini injection and its regulatory mechanism are reported. Our results showed that the administration of CI5 significantly relieved the pain of mice in the acetic acid twisting analgesic model and formalin inflammatory pain model. Furthermore, CI5 effectively reduced the inflammatory cytokines (IL-6, TNF-α and IL-1β) and inflammatory mediator (PGE2) expressions, and prevented the carrageenan-induced paw edema in mice. Further LC-MS/MS results showed the anti-inflammatory and analgesic bio-functions of CI5 depended on its interaction with the Rac-2 protein upstream of ERK1/2 and the inflammatory signaling pathway (ERK1/2/COX-2 axis). In summary, CI5, as a novel natural candidate identified from Cinobufacini injection, showed substantial clinical promise for inflammatory pain treatments.
研究领域:
药理学
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疼痛管理
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传统中药
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分子生物学
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产品关联
DOI
PubMed
高影响因子
BRAIN RESEARCH
·
2023
·
IF 2.9
Yong-Juan Gu,He-Ya Qian,Fang Zhou,Ling Zhang,Long Chen,Yu Song,Ya-Nan Chen,Hai-Long Zhang
Background Bone cancer pain (BCP) remains a clinical challenge due to the limited and side effects of therapeutic methods. Folic acid has been known as an FDA approved dietary supplement and proved to have an analgesic effect in neuropathic pain. Here we investigate the role and mechanism of folic acid in bone cancer pain of a rat model. Methods Walker 256 tumor cells were inoculated into the left tibia of rats to induce bone cancer pain model. Pain reflex were assessed by paw withdrawal threshold (PWT) response to Von Frey filaments and paw withdrawal latency (PWL) response to thermal stimulation. Folic acid was injected intraperitoneally to evaluate its analgesic effect in rats with bone cancer pain. Western blotting and qPCR were used to determine P2X2/3 receptor protein and mRNA levels in ipsilateral L4-6 dorsal root ganglion (DRG) and spinal dorsal horn (SDH). Results The PWT and PWL of rats with bone cancer pain were obviously decreased compared to the naïve and sham rats. Interestingly, continuous folic acid treatment significantly increased the PWT and PWL of rats with bone cancer pain. P2X2 and P2X3 receptors were clearly upregulated at both mRNA and protein expression in L4-6 DRG and SDH of rats with bone cancer pain. P2X2 and P2X3 receptors were mainly localized with CGRP (calcitonin gene-related peptide) or IB4 (isolectin B4) positive neurons in L4-6 DRG of rats with bone cancer pain. Notably, continuous folic acid treatment significantly reduced the expression of P2X2 and P2X3 receptors in L4-6 DRG and SDH of rats with bone cancer pain. Finally, intrathecal injection of A317491 (a selective antagonist of P2X2/3 receptors) markedly elevated the PWT and PWL of rats with bone cancer pain. Conclusion These results suggest that folic acid has an effective antinociceptive effect on bone cancer pain, which is mediated by downregulating P2X2/3 receptors in L4-6 DRG and SDH of rats with bone cancer pain. Folic acid may be a novel therapeutic strategy in cancer patients for pain relief.
研究领域:
药理学
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肿瘤学
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神经科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Theranostics
·
2024
·
IF 12.4
Jing Liu,Weiwei Wu,Fei Peng,Deying Gong,Yi Kang,Yujun Zhang,Congyan Liu,Yuncheng Li,Guoyan Zhao,Feng Qiu,Wensheng Zhang
Rationale: To meet the need of long-acting analgesia in postoperative pain management, slow-releasing formulations of local anesthetics (LAs) have been extensively investigated. However, challenges still remain in obtaining such formulations in a facile and cost-effective way, and a mechanism for controlling the release rate to achieve an optimal duration is still missing. Methods: In this study, nanosheets formed by a self-assembling peptide were used to encapsulate ropivacaine in a soft-coating manner. By adjusting the ratio between the peptide and ropivacaine, ropivacaine particles with different size were prepared. Releasing profile of particles with different size were studied in vitro and in vivo . The influence of particle size and ropivacaine concentration on effective duration and toxicity were evaluated in rat models. Results: Our results showed that drug release rate became slower as the particle size increased, with particles of medium size (2.96 ± 0.04 μm) exhibiting a moderate release rate and generating an optimal anesthetic duration. Based on this size, formulations at different ropivacaine concentrations generated anesthetic effect with different durations in rat sciatic nerve block model, with the 6% formulation generated anesthetic duration of over 35 h. Long-acting analgesia up to 48 h of this formulation was also confirmed in a rat total knee arthroplasty model. Conclusion: This study provided a facile strategy to prepare LA particles of different size and revealed the relationship between particle size, release rate and anesthetic duration, which provided both technical and theoretical supports for developing long-acting LA formulations with promising clinical application.
研究领域:
药剂学
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生物医学工程
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疼痛管理
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产品关联
DOI
PubMed
高影响因子
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
·
2025
·
IF 4.9
Xinru Zhu,Yulin Chen,Yumeng Li,Wenwen Cui,Xiaoying Wang,Lele Mao,Yue Li,Letian Zhang,Ying Chen,Mei Dong,Qingsong Wang
This study aimed to employ eutectic technology to formulate a stable, organic solvent-free and high-concentration capsaicin cream. Herein, menthol was selected to form a eutectic with capsaicin from ten compounds. The eutectic mixtures (EMs) were characterized by polarized optical microscopy (POM), differential scanning calorimetry (DSC), Fourier Transform Infrared (FT-IR) spectroscopy, and X-ray diffraction (XRD). The stability of the EMs in the cream was prolonged for over 8 months due to the interactions among capsaicin, menthol, Span 40, and polyvinyl alcohol (PVA). The rheological properties were further enhanced by incorporating white petrolatum and anhydrous calcium hydrogen phosphate into the eutectic cream, which indicated improved physical stability and spreadability. Moreover, the retention of capsaicin in porcine skin was comparable between the eutectic cream group (4% w/w capsaicin) and the Qutenza® group (8% w/w capsaicin). Once applied the capsaicin eutectic cream (4% w/w) to chronic constriction injury (CCI) model in mice, mechanical and thermal pain were alleviated in a manner similar to Qutenza®. Overall, the capsaicin eutectic cream was successfully prepared by combining eutectic, with a specific mixture of surfactant and PVA. Also, the cream showed excellent permeability and storage stability for topical application, which provided a promising potential for the development of long-acting analgesic drugs.
研究领域:
药剂学
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疼痛管理
·
药物递送系统
✓ 已验证
产品关联
DOI
高影响因子
Drug Delivery and Translational Research
·
2025
·
IF 5.5
Zhao Erman,Tang Xiuling,Zhao Minggao,Yang Le
Wound healing for various diseases and wounds such as diabetes and burns remains a major biomedical challenge. Conventional monotherapy is ineffective, and the efficacy of drug delivery is limited by the depth of drug penetration. In this study, we develop a novel, multifunctional, dissolvable hyaluronic acid (HA) microneedle patch (MN-LTT). Microneedling is biocompatible and delivers the drug in a painless and non-invasive manner. Lidocaine and thrombin are mixed with HA hydrogel and loaded onto the needle tips of the MN-LTT, which facilitates wound repair by continuously delivering the drug deep into the dermis for rapid analgesia and hemostasis. In addition, the backing layer of the MN-LTT is composed of tetracycline hydrochloride and HA hydrogel, and its excellent antimicrobial properties further accelerate wound healing. In a mouse full-thickness skin wound model, MN-LTT accelerated cell proliferation and granulation tissue growth, reduced inflammatory-factor levels, and restored collagen deposition, resulting in complete wound healing within seven days. Thus, the proposed microneedle delivery system achieved rapid hemostatic, analgesic, and bactericidal effects, providing a safer and more effective strategy for wound healing. These features make the multifunctional HA microneedle patch potentially valuable for clinical applications. Graphical This self-assembled multifunctional microneedle (MN-LTT) can deliver drugs into the wound tissue in a painless and minimally invasive manner, quickly achieving the functions of hemostasis, analgesia, and antibacterial effects to jointly promote wound healing. In addition, the rapid degradation of MN-LTT can avoid secondary damage to the wound during dressing changes. This combined therapy is a potential strategy for achieving high-quality wound healing
研究领域:
生物医学工程
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药剂学
·
组织修复与再生
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Food Science & Nutrition
·
2021
·Vol. 9
·期 4
·2191-2202
·
IF 2.863
Zefeng Chen,Shupeng Cheng,Huiqiong Lin,Wenjing Wu,Liyi Liang,Xicai Chen,Xi Zheng,Yan He,Kun Zhang
Acanthopanax trifoliatus (L.) Merr (AT) is a medicinal and edible plant with high nutritional value. The biological activity of A. trifoliatus (L.) Merr and its basis for injury treatment are explored in this paper. AT was ethanol-extracted then refined separately with petroleum ether, chloroform, ethyl acetate, and n-butanol. Active ingredients were analyzed, and anti-bacterial, anti-inflammatory, analgesic, and hemostatic effects were explored. Petroleum ether layer (PEL) extract produced the strongest antibacterial effect. Ethyl acetate layer (EAL) extract had the highest active substance content, with strong hemostatic and analgesic activities. Chloroform layer (CL) extract had the strongest anti-inflammatory effect and significantly reduced IL-1β protein expression. Active ingredients were analyzed using HPLC and UPLC-MS to determine saponin, polyphenol, flavonoid, and characteristic ingredient contents. EAL extract had the highest polyphenol and flavonoid levels, including rutin, chlorogenic acid, isochlorogenic acid A, and isochlorogenic acid C, which may contribute to its nutritional activities. The study provides a reliable theoretical and practical basis for the applications of AT nutraceutical products.
研究领域:
药理学
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植物学
·
营养科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Journal of Anesthesia
·
2024
·Vol. 38
·期 2
·232-243
·
IF 2.8
Zheng Ling-xi,Yu Qian,Li Qiang,Zheng Chuan-dong
Purpose Lidocaine microspheres can prolong the analgesic time to 24–48 h, which still cannot meet the need of postoperative analgesia lasting more than 3 days. Therefore, we added Fe 3 O 4 to the lidocaine microspheres and used an applied magnetic field to attract Fe 3 O 4 to fix the microspheres around the target nerves, reducing the diffusion of magnetic lidocaine microspheres to the surrounding tissues and prolonging the analgesic time. Methods Fe 3 O 4 –lidocaine–PLGA microspheres were prepared by the complex-emulsion volatilization method to characterize and study the release properties in vitro. The neural anchoring properties and in vivo morphology of the drug were obtained by magnetic resonance imaging. The nerve blocking effect and analgesic effect of magnetic lidocaine microspheres were evaluated by animal experiments. Results The mean diameter of magnetically responsive lidocaine microspheres: 9.04 ± 3.23 μm. The encapsulation and drug loading of the microspheres were 46.18 ± 3.26% and 6.02 ± 1.87%, respectively. Magnetic resonance imaging showed good imaging of Fe 3 O 4 –Lidocain–PLGA microspheres, a drug-carrying model that slowed down the diffusion of the microspheres in the presence of an applied magnetic field. Animal experiments demonstrated that this preparation had a significantly prolonged nerve block, analgesic effect, and a nerve anchoring function. Conclusion Magnetically responsive lidocaine microspheres can prolong analgesia by slowly releasing lidocaine, which can be immobilized around the nerve by a magnetic field on the body surface, avoiding premature diffusion of the microspheres to surrounding tissues and improving drug targeting.
研究领域:
药剂学
·
神经科学
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医学影像学
✓ 已验证
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2024
·
IF 7.7
Yan Wu,Yibin Lin,Ying Chen,Haiting Fan,Jieheng Zhang,Jiaxin Li,Wenjing Lin,Guobin Yi,Xia Feng
Considering the astonishing prevalence of localized pain affecting billions of patients worldwide, the development of advanced analgesic formulations or delivery systems to achieve clinical applicability is of great significance. In this study, an integrated PDA-based LiH@PDA@Ag@PAA@Gelatin system was designed for sustained delivery of lidocaine hydrochloride (LiH). By optimizing the preparation process and formulation of the hydrogel, the hydrogel exhibited superior mechanical properties, reversibility, adhesion strength , and self-healing attributes. Moreover, PDA@Ag nanoparticles were evenly dispersed within the hydrogel, and the optimized PDA@Ag@PAA@Gelatin showed a higher photothermal conversion efficiency than that of pure PDA. Importantly, LiH@PDA@Ag@PAA@Gelatin could effectively capture and eradicate bacteria through the synergistic interaction between near-infrared (NIR), PDA, Ag and LiH. In vitro and in vivo tests demonstrated that LiH@PDA@Ag@PAA@Gelatin exhibited higher drug delivery efficiency compared to commercial lidocaine patches. By evaluating the mechanical pain withdrawal threshold of the spared nerve injury (SNI) model in rats, it was proven that LiH@PDA@Ag@PAA@Gelatin enhanced and prolonged the analgesic effect of LiH. Furthermore, LiH@PDA@Ag@PAA@Gelatin induced by NIR possessed excellent on-demand photothermal analgesic ability. Therefore, this study develops a convenient method for preparing localized analgesic hydrogel patches, providing an important step towards advancing PDA-based on-demand pain relief applications.
研究领域:
药剂学
·
生物医学工程
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材料科学
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产品关联
DOI
PubMed
高影响因子
Korean Journal of Pain
·
2024
·
IF 3.4
Kaiwen Lin,Datian Fu,Zhongtao Wang,Xueer Zhang,Canyang Zhu
Background Galangin, commonly employed in traditional Chinese medicine for its diverse medicinal properties, exhibits potential in treating inflammatory pain. Nevertheless, its mechanism of action remains unclear. Methods Mice were randomly divided into 4 groups for 7 days a normal control group, a galangin-treated (25 and 50 mg/kg), and a positive control celecoxib (20 mg/kg). Analgesic and anti-inflammatory effects were evaluated using a hot plate test, acetic acid-induced writhing test, acetic acid-induced vascular permeability test, formalin-induced paw licking test, and carrageenan-induced paw swelling test. The interplay between galangin, transient receptor potential vanilloid 1 (TRPV1), NF-κB, COX-2, and TNF-α proteins was evaluated via molecular docking. COX-2, PGE2, IL-1β, IL-6, and TNF-α levels in serum were measured using ELISA after capsaicin administration (200 nmol/L). TRPV1 expression in the dorsal root ganglion was analyzed by Western blot. The quantities of substance P (SP) and calcitonin gene-related peptide (CGRP) were assessed using qPCR. Results Galangin reduced hot plate-induced licking latency, acetic acid-induced contortions, carrageenan-triggered foot inflammation, and capillary permeability in mice. It exhibited favorable affinity towards TRPV1, NF-κB, COX-2, and TNF-α, resulting in decreased levels of COX-2, PGE2, IL-1β, IL-6, and TNF-α in serum following capsaicin stimulation. Galangin effectively suppressed the upregulation of TRPV1 protein and associated receptor neuropeptides CGRP and SP mRNA, while concurrently inhibiting the expression of NF-κB, TNF-α, COX-2, and PGE2 mRNA. Conclusions Galangin exerts its anti-inflammatory pain effects by inhibiting TRPV1 activation and regulating COX-2, NF-κB/TNF-α expression, providing evidence for the use of galangin in the management of inflammatory pain.
研究领域:
药理学
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生物化学
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分子生物学
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炎症研究
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疼痛管理
✓ 已验证
DOI
PubMed
高影响因子
MOLECULES
·
2019
·Vol. 24
·期 9
·1692
·
IF 3.06
Jiajia Guo,Dan Zhang,Chao Yu,Ling Yao,Zhuo Chen,Yanduo Tao,Weiguo Cao
Incarvillea compactaMaxim is a traditional Tibetan plant widely used to treat rheumatic pain and bruises. We conducted qualitative analyses by liquid chromatography-mass spectrometry and quantitative analyses of the total phenols, flavonoids, and alkaloids content of different extracts ofI. compactaMaxim. Antioxidant and analgesic activity were analyzed. The results showed that the methanol extract had the highest content of the various ingredients. A total of 25 constituents were identified, of which compounds1–23were found for the first time in this plant. The water extract had the highest capacity to clear free radicals in the antioxidant test. The water extract had dose-dependent analgesic effects in the first and second phase in a formalin test. The latency of pain from a hot-plate test was augmented by the water extract when the dose was greater than or equal to 30 g/kg. The water extract significantly decreased the amount of writhing in a dose-dependent manner compared with the control group in the acetic acid-induced writhing test. These results showed thatI. compactaMaxim is a new antioxidant and analgesic agent, and this study provides information on its ingredients for further study.Keywords:LC-MS;anti-oxidation;analgesia;formalin test;Tibetan plant
研究领域:
植物化学
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药理学
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民族植物学
✓ 已验证
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）