Simultaneous Determination of Two Types of Active Components with Different Physicochemical Properties in Kushen by HPLC-UV

A simple, reliable and accurate high performance liquid chromatography(HPLC) coupled with a UV detector at varied wavelength was developed for the quantitation of two types of anti-carcinogenic compounds, namely, Kushen alkaloids(KS-As) and Kushen flavonoids(KS-Fs), in Kushen. Their remarkable difference in physicochemical properties was circumvented by integrated optimization of column and mobile phase. The separation was achieved on an alkaline-resisting C18 column via gradient elution with acetonitrile(ACN) and 0.025%(volume ratio) diethylamine(DEA) in water as mobile phase. The flow rate was 0.7 mL/min, and the column temperature was maintained at 35 °C. UV detection wavelength was set at 225 nm to monitor KS-As, and then changed to 335 nm for KS-Fs at 26th min, which was kept for 30 min before returning to the original wavelength. All the calibration curves show good linearity(r20.999) within test ranges. The intra- and inter-day precision values of these components were less than 3.82%, and the average recovery rates obtained were in a range of 97.24%―102.64% for all the samples with RSD below 3.94%. This assay was successfully applied to determining the major active components in commercial herbal samples of Kushen. Moreover, the possible relationship between sample and the geographical region was visualized based on the contents of the 6 compounds in the light of principal component analysis(PCA). The results suggest that the proposed method facilitates the quality control of Kushen.

Compound Kushen injection induces immediate hypersensitivity reaction through promoting the production of platelet-activating factor via de novo pathway

OBJECTIVE Compound Kushen injection(CKI)is a bis-herbal formulation extracted from Kushen(Radix Sophorae Flavescentis)and Baituling(Rhizoma Heterosmilacis Japonicae).Clinically,it is used as the adjuvant treatment of cancer.However,with the increased application,the cases of immediate hypersensitivity reactions(IHRs)also gradually rise.In this study,we investigated the underlying mechanism(s)and active constituent(s)for CKI-induced IHRs in experimental models.METHODS T helper 2(Th2)immunity-amplified mice were prepared by aluminum adjuvant.Anaphylactic shock was detected by measuring rectal thermometry in propranolol pretreated mice.For evaluating microvascular permeability,Evans blue extravasation assay was used.Platelet-activating factor(PAF),serum total IgE(tIgE)and mouse mast cell protease 1(MMCP1)were measured by ELISA.RESULTS The obtained results showed that CKI did not elevate serum tIgE and MMCP1 after consecutive immunization for five weeks,but could induce Evans blue extravasation(local)and cause obvious hypothermia(systemic)after a single injection.Further study showed that alkaloids in Kushen,especially matrine,were responsible for CKI-induced IHRs.Mechanism study showed that various PAF receptor antagonists could significantly counter CKI-induced IHRs locally or systemically.In cell system,CKI was able to promote PAF production in a non-cell-selective manner.In cell lysate,the effect of CKI on PAF production became stronger and could be abolished by blocking de novo pathway.CONCLUSION In conclusion,our study identifies,for the first time,that CKI is a PAF inducer.It causes non-immunologic IHRs,rather than IgE-dependent IHRs,by promoting PAF production through de novo pathway.Alkaloids in Kushen,especially matrine,are the prime culprits for IHRs.Our findings may provide a potential approach for preventing and treating CKI-induced IHRs.

Molecular mechanism prediction analysis of compound Kushen injection in the treatment of COVID-19 based on network pharmacology and molecular docking

Background:As one of the eight effective traditional Chinese medicines for the treatment of atypical pneumonia,compound Kushen injection(CKI)played an important role in combating pneumonia caused by severe acute respiratory syndrome coronavirus 2 virus in China in 2003.CKI is known to inhibit inflammation,and its main chemical components,namely matrine and oxymatrine,can promote Th cells to recognize and eliminate viruses.In this study,network pharmacology and molecular docking were used to explore the mechanisms of CKI for treating coronavirus disease 2019.Methods:The Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform and other related literature were used to screen CKI’s active ingredients in the blood.Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform,Swiss Target Prediction and STITCH were used to search for potential targets of the active ingredients.The“ingredient-target”network was constructed using the Cytoscape software.The STRING online database was used to construct a target protein-protein interaction network that can be visualized and analyzed using the Cytoscape software to obtain key targets.Results:Sophocarpine,sophoridine,matrine,(+)-allomatrine,AIDS211310,and sophranol were the six active ingredients.After docking the active ingredients with severe acute respiratory syndrome coronavirus 23CL hydrolase and angiotensin-converting enzyme 2(ACE2),they displayed suitable affinity,which could block viral replication and its binding to ACE2.The key targets mainly involved inflammatory factors,such as interleukin-6(IL-6)and tumor necrosis factor(TNF).Gene Ontology enrichment analysis mainly indicated the IL-6 cytokine-mediated signaling pathway and cytokine-mediated signaling pathway.The Kyoto Encyclopedia of Genes and Genome pathway enrichment analysis mainly indicated steroid hormone biosynthesis and the TNF signaling pathway.Conclusion:The alkaloids in CKI can block viral replication and its binding to severe acute respiratory syndrome coronavirus 2 and ACE2 receptors.They regulate the IL-6-mediated signaling pathway,TNF signaling pathway,and steroid hormone biosynthesis,thereby initiating therapeutic responses against coronavirus disease 2019.

Association rules analysis of Fufang Kushen injection in combination with traditional Chinese medicine or modern medications in treating Cervical cancer: real-world retrospective study

Objective: The present study aimed to analyze the association rules of Fufang Kushen injection in combination with other traditional Chinese medicine ( TCM) or modern medications in treating cervical cancer (CC) based on the electrical medical records extracted from real-world hospital information system. Methods: The clinicians’ prescriptions regarding to the combination of with TCM or modern medications were from hospital information system electronic medical data integration warehouse established by the Institute of Basic Medical Research of Chinese Medicine, China Academy of Chinese Medical Sciences, which integrated the hospital information system data of 22 hospitals. The association rules of the drug characteristics were analyzed through Apriori algorithm. Results: A total of 839 patients with CC were included. We found that is often combined with prescriptions which could clear heat, remove toxicity, supplement Qi. also combined with chemotherapeutic drugs, immunomodulatory drugs, 5-HT receptor blockers, and glucocorticoids. The combination presents a specific law. Conclusion: Fufang Kushen injection combined with hepatoprotective drugs, immunomodulators and glucocorticoids is often used to treat cervical cancer.

Compound Kushen injection combined with chemotherapy in the treatment of gastric cancer: a meta-analysis of randomized controlled trials

Objective: This study aims to systematically evaluate the efficacy and safety of compound kushen injection (CKI) in combination with chemotherapy in patients with gastric cancer (GC). Methods: A comprehensive electronic search was conducted by searching PubMed, EMBASE, Cochrane Library, Chinese Biological Medical disc, China National Knowledge Infrastructure and Wanfang databases (the last update January 20, 2018). All randomized controlled trials (RCTs) of CKI plus chemotherapy versus chemotherapy alone in GC patients were identified. The quality of each study was evaluated using the Jadad’s scale, and the meta-analysis was performed using Review Manager 5.3 and STATA 14 software. Results: A total of nine studies on 688 cases were included in this study. The results showed that CKI combined with chemotherapy had a better effect on improving patients’ overall response rate (ORR) and life quality. The consequences of Egger’s and Begg’s tests showed there was no significant publication bias. Conclusion: The current evidence showed that CKI may enhance the clinical efficacy of chemotherapy, improve the quality of life and increase the safety in patients with gastric cancer.

Research Progress on the Antitumor Mechanism of Compound Kushen Injection

Compound Kushen Injection(CKI),as a clinical traditional Chinese medicine preparation,has prominent antitumor effect but with several side effects.A large number of studies have shown that CKI plays an antitumor role by regulating tumor cell proliferation,inducing tumor cell differentiation and apoptosis,inhibitrng tumor cell invasion and metastasis,reducing tumor angiogenesis,regulating the immunity,and so on.Clinically,CKI is widely used to treat various tumors,where it is often combined with surgery,chemotherapy,radiotherapy,targeted therapy,and other antitumor treatments.This article reviews the antitumor mechanism of CKI and the progress of its clinical application in order to provide a theoretical basis for further clinical application.

辣椒新品种‘宁椒12号’的选育

‘宁椒12号’是由宁夏农林科学院园艺研究所选育的自主知识产权的杂一代中早熟鲜食螺丝椒品种。露地条件下生育期190~195 d,保护地条件下生育期210~250 d。株型直立,第一雌花节位7~8节。平均果长26.7 cm,果实横径3.8 cm,果肉厚度0.22 cm,平均单果质量78 g,最大单果质量90 g;果面皱褶大浅,集中于果实上部,果顺直,青熟果深绿色,老熟果鲜红色,单株结果数28~32个。果实商品性好,味香辣,维生素C含量0.179 g·kg^(-1),干物质含量13%,总辣椒素含量0.179 g·kg^(-1)。中抗疫病,抗白粉病。667 m2产量3 700~4 500 kg。适宜宁夏及环境条件相近区域露地及保护地种植。

复方苦参注射液联合DCF化疗方案对胃癌术后患者并发症及Th17/Treg平衡的影响

目的:探讨复方苦参注射液联合DCF化疗方案对胃癌术后患者并发症及Th17/Treg平衡的影响。方法:选取2022年10月至2023年8月于该院进行手术治疗的胃癌患者96例,根据治疗方案的不同分为复方苦参注射液组和对照组,每组48例。两组患者均接受根治性手术治疗,对照组患者采用DCF化疗方案(多西他赛+顺铂+5-氟尿嘧啶)治疗,复方苦参注射液组患者在对照组的基础上加用复方苦参注射液治疗。比较两组患者并发症发生率,Th17、Treg和Th17/Treg指标变化情况。结果:复方苦参注射液组患者的并发症发生率为10.42%(5/48),低于对照组的35.42%(17/48),差异有统计学意义(P<0.05)。治疗后,两组患者Th17、Th17/Treg指标高于治疗前,且复方苦参注射液组患者明显高于对照组,差异均有统计学意义(P<0.05);治疗后,两组患者Treg指标低于治疗前,且复方苦参注射液组患者明显低于对照组,差异均有统计学意义(P<0.05)。结论:复方苦参注射液能够调节胃癌术后患者体内T细胞亚群失衡,改善机体免疫功能,减轻术后并发症发生率,更有利于患者预后。

复方苦参注射液辅助胃癌术后化疗的作用及对机体功能的影响

目的 探讨复方苦参注射液辅助胃癌术后化疗的作用及对机体功能的影响。方法 将92例胃癌患者通过随机抽签分为研究组、对照组,各46例。术后对照组患者采用奥沙利铂+卡培他滨(XELOX)方案化疗,研究组患者在对照组基础上使用复方苦参注射液静脉滴注,观察2个化疗周期。比较治疗前后两组患者中医症候积分、健康状况[卡氏功能状态(KPS)评分]、肿瘤标志物[糖类抗原724(CA724)、癌胚抗原(CEA)、糖类抗原199(CA199)]水平、免疫功能(CD3^(+)、CD4^(+)、CD8^(+)水平及CD4^(+)/CD8^(+)比值)、临床疗效、毒副反应。结果 治疗后,研究组患者总有效率、KPS评分、CD3^(+)、CD4^(+)水平及CD4^(+)/CD8^(+)比值均高于对照组,中医证候积分、CA724、CEA、CA199、CD8^(+)水平均低于对照组(P<0.05或0.01)。研究组患者血液毒性、肝肾功能异常及胃肠道反应发生率均低于对照组(P<0.05)。结论 在化疗基础上,对胃癌术后患者加用复方苦参注射液治疗,能改善患者临床症状,有效调节免疫功能,改善健康状况,减少毒副反应的发生,临床疗效显著,优于单纯化疗。

复方苦参注射液配合同期放化疗治疗鼻咽癌的临床观察

目的:探讨复方苦参注射液配合同期放化疗治疗鼻咽癌的临床治疗效果及对放射性口腔黏膜炎、放射性皮炎和其他放化疗不良反应的影响。方法:采用回顾性分析,选取2021—2022年该院肿瘤科收治的100例鼻咽癌患者,依据治疗方法分为观察组(n=48)和对照组(n=52)。对照组患者的治疗方案为同步放化疗,调强适形放疗,期间使用顺铂治疗;观察组患者在对照组的基础上联合复方苦参注射液静脉滴注,1日1次,连续应用14 d,停用7 d;两组患者的治疗周期均为6周。比较两组患者的近期疗效,治疗期间放射性口腔黏膜炎、放射性皮炎及其他放化疗不良反应的发生率。结果:治疗后,观察组患者客观缓解率为91.7%(44/48),高于对照组的88.5%(46/52),但差异无统计学意义(P>0.05)。治疗期间,观察组患者放射性口腔黏膜炎、放射性皮炎发生率低于对照组,差异均有统计学意义(P<0.05);两组患者骨髓抑制发生率的差异无统计学意义(P>0.05)。观察组患者消化道不良反应发生率低于对照组,差异有统计学意义(P<0.05)。结论:复方苦参注射液配合同步放化疗用于鼻咽癌患者,可减少放疗所致的放射性口腔黏膜炎、放射性皮炎,降低消化道不良反应发生率,提高同步放化疗的安全性。

复方苦参注射液辅助程序性死亡受体1抑制剂联合多西他赛+顺铂方案化疗治疗非小细胞肺癌的疗效观察

目的:探讨复方苦参注射液辅助程序性死亡受体1(PD-1)抑制剂联合多西他赛+顺铂方案化疗治疗非小细胞肺癌的临床疗效。方法:回顾性选取2020年10月~2023年5月某院收治的84例非小细胞肺癌患者为研究对象,根据不同的治疗方案分为对照组和观察组,每组42例。对照组给予PD-1抑制剂联合多西他赛+顺铂方案,观察组在对照组基础上加用复方苦参注射液。评估两组患者临床疗效;应用流式细胞仪测定治疗前后患者血清肿瘤标记物[癌胚抗原(CEA)、异常糖链糖蛋白(TAP)]水平;评估两组患者治疗后的生活能力[卡诺夫斯凯计分(KPS)];比较治疗期间两组患者的不良反应发生情况以评估药物安全性。结果:治疗后,观察组的客观缓解率和疾病控制率分别为69.05%和95.23%,高于对照组的47.62%和76.19%,组间存在统计学差异(P<0.05)。治疗前,患者的血清CEA和TAP水平组间比较无统计学差异(P>0.05);治疗后,观察组CEA和TAP水平均低于对照组(P<0.05);治疗后,观察组患者的KPS评分高于对照组(P<0.05)。此外,在不良反应发生情况方面,观察组的骨髓抑制率(30.95%)低于对照组(80.95%,P<0.05),且观察组总不良反应发生率(33.33%)也低于对照组(92.86%,P<0.05)。结论:与PD-1抑制剂联合多西他赛+顺铂方案相比,采用复方苦参注射液辅助PD-1抑制剂联合多西他赛+顺铂方案化疗治疗非小细胞肺癌的临床疗效较佳,患者生活质量提升更明显,安全性更高,推荐临床广泛应用。

苦蛇治霉滴耳剂的制备及其临床疗效观察

目的探讨苦蛇治霉滴耳剂的制备工艺与质量控制程序,观察该制剂治疗真菌性外耳道炎的临床疗效。方法采用常规制备工艺将该组方制备为滴耳剂,同时建立质量控制规范操作流程。收集在本院门诊就诊的真菌性外耳道炎患者300例,随机分为观察组160例和对照组140例。所有患者均彻底清洁外耳道,然后各组分别接受不同治疗。对照组患者以4%硼酸酒精滴耳液耳浴,治疗组患者则以苦蛇治霉滴耳剂耳浴,均为每日2次,7d为1疗程,共治疗2疗程。疗程结束后评定两组患者的治疗效果。结果该制剂生产工艺可行,质量控制良好。观察组有效率95.43%,明显优于对照组的有效率80.74%(P<0.01)。结论苦蛇治霉滴耳剂组方合理,质量标准稳定可控,治疗真菌性外耳道炎疗效确切,无明显毒副作用。

蛋黄油外敷联合苦参汤加减熏洗对混合痔术后创面愈合的影响

目的探讨蛋黄油外敷联合苦参汤加减熏洗对混合痔术后创面愈合的影响。方法选取河北省中医院2019年10月至2023年4月收治行混合痔手术的患者141例,按随机数字表法分为对照A组、对照B组和观察组,各47例。3组患者接受常规混合痔外剥内扎手术,术后予常规抗感染、补液,对照A组患者予温水熏洗后加用凡士林油纱条覆盖创面,对照B组患者予苦参汤加减熏洗后加用凡士林油纱条覆盖创面,观察组患者予苦参汤加减熏洗后加用蛋黄油纱条覆盖创面。结果观察组总有效率为100.00%,显著高于对照B组的93.62%和对照A组的87.23%(P<0.05)。术后第7,14天,观察组及对照B组患者血清P物质、5-羟色胺、肿瘤坏死因子-α、白细胞介素6水平,创面愈合时间及创面缩小率均显著优于对照A组(P<0.05),且观察组上述指标均显著优于对照B组(P<0.05)。3组患者均无明显不良反应发生。结论蛋黄油外敷联合苦参汤加减熏洗可促进混合痔术后创面愈合,减轻患者疼痛,降低炎性因子水平,缩短康复进程。

复方苦参注射液联合阿片类镇痛药对结直肠癌晚期患者疼痛、生活质量及凝血功能的改善效果观察

目的:探讨复方苦参注射液联合阿片类镇痛药对结直肠癌(CRC)晚期患者疼痛、生活质量及凝血功能的改善效果,并查阅文献初步探讨相关作用机制。方法:选取2019年1月至2024年3月该院收治的CRC晚期患者106例,根据随机数字表法分为单药组(n=53,给予盐酸曲马多或盐酸羟考酮治疗)、联合用药组(n=53,给予复方苦参注射液联合盐酸曲马多或盐酸羟考酮治疗)。比较两组患者治疗前后的视觉模拟评分(VAS)和疼痛缓解程度、生活质量[卡诺夫斯凯计分(KPS)]及凝血功能状况(D-二聚体和纤维蛋白原表达水平)。结果:治疗前,两组患者VAS评分、KPS评分、D-二聚体和纤维蛋白原表达水平的差异均无统计学意义(P>0.05)。治疗后,联合用药组患者的VAS评分为(1.28±1.08)分,明显低于单药组的(2.72±0.72)分;联合用药组患者的疼痛缓解程度显著优于单药组,差异均有统计学意义(P<0.05)。治疗后,联合用药组患者的KPS评分为(85.28±11.23)分,高于单药组的(78.87±12.81)分,差异有统计学意义(P<0.05)。治疗后,单药组患者凝血功能指标(D-二聚体和纤维蛋白原)表达水平较治疗前轻度升高,但差异无统计学意义(P>0.05);联合用药组患者凝血功能指标表达水平较治疗前显著降低,且低于同期对照组,差异均有统计学意义(P<0.05)。结论:复方苦参注射液联合盐酸阿片类镇痛药用于CRC晚期患者,在缓解疼痛、提升生活质量及改善凝血功能方面的治疗效果满意。

复方苦参注射液联合双膦酸盐类药物治疗恶性肿瘤骨转移所致癌性疼痛患者的疗效和安全性Meta分析

目的:系统评价复方苦参注射液(CKI)联合双膦酸盐(BPs)类药物治疗恶性肿瘤骨转移所致癌性疼痛(以下简称癌痛)患者的有效性和安全性。方法:计算机检索中国知网(CNKI)、万方数据库(Wanfang)、维普中文科技期刊数据库(VIP)、PubMed、CochraneLibrary,检索时间均为建库至2024年1月22日,收集CKI联合BPs类药物治疗恶性肿瘤骨转移所致癌痛患者的随机对照试验(RCT)研究文献。通过Cochrane风险评估工具进行文献质量评价,并采用RevMan5.4软件进行Meta分析。结果:共检索出245篇文献,最终纳入27篇文献,共计2255例患者,其中对照组(单用BPs类药物)1108例,联合组(CKI联合BPs类药物)1147例。Meta分析结果显示,在疼痛缓解率、生活质量评分[卡诺夫斯凯计分(KPS)]、血清碱性磷酸酶(ALP)和不良反应发生率方面,CKI联合BPs类药物的治疗效果均优于单用BPs类药物(P<0.01)。结论:CKI联合BPs类药物治疗可有效提高恶性肿瘤骨转移所致癌痛患者的疼痛缓解率、KPS评分,改善血清ALP水平,降低不良事件的发生风险。

复方苦参注射液联合同步放化疗治疗宫颈鳞癌术后患者的临床研究

目的:探讨宫颈鳞癌患者经根治性子宫切除术后给予复方苦参注射液联合同步放化疗方案的治疗效果。方法:选取2018年12月~2023年10月期间某院收治的80例宫颈鳞癌患者作为研究对象,根据治疗方案不同分为对照组和观察组,每组40例。两组患者均进行根治性子宫切除术,术后对照组患者给予同步放化疗方案治疗,观察组患者在对照组治疗基础上加用复方苦参注射液,两组均治疗42天。比较两组患者肿瘤标记物[鳞状上皮细胞癌相关抗原(SCC-Ag)]、炎症因子[肿瘤坏死因子-α(TNF-α)和白介素-2(IL-2)]、免疫指标[自然杀伤(NK)细胞]及不良反应发生情况。结果:治疗后,观察组患者血清SCC-Ag、TNF-α和IL-2水平均低于对照组,NK细胞水平高于对照组(P<0.05)。治疗期间,观察组患者胃肠道反应发生率低于对照组(P<0.05)。结论:复方苦参注射液联合同步放化疗治疗可抑制宫颈鳞癌术后患者肿瘤生长,降低SCC-Ag、炎症因子水平,提高NK细胞水平,且减少胃肠道不良反应的发生。

基于血水同治法刍议当归贝母苦参丸之异病同治

目的 基于血水同治法刍议当归贝母苦参丸之异病同治。方法 以血水同治法为理论依据,结合当归贝母苦参丸之组方原理,探讨其异病同治之临床应用。结果 当归贝母苦参丸为血水同治法代表方剂,为治疗妇女妊娠并发小便难之名方。现代中医学者基于其血水同治的组方思路,扩展其临床应用,如盆腔炎、前列腺炎、慢性便秘、溃疡性结肠炎,以及肿瘤类疾病。结论 当归贝母苦参丸之异病同治皆为其血水同治之配伍功效与多种疾病之病机吻合,临证之时应灵活加减。

复方苦参注射液联合FOLFOX4化疗方案对胃癌患者免疫功能及基质金属蛋白酶水平的影响

目的 分析复方苦参注射液联合FOLFOX4化疗方案在胃癌患者中的应用效果。方法 选取2019年4月至2021年4月我院收治的86例胃癌患者为研究对象,根据随机数字表法将其分为对照组(FOLFOX4化疗方案)和研究组(FOLFOX4化疗方案+复方苦参注射液),各43例。比较两组的临床疗效、中医证候积分、血清指标及骨髓与免疫功能指标。结果 研究组的疾病控制总有效率显著高于对照组(P<0.05)。治疗后,两组的上腹疼痛、纳差、厌食、神疲积分均降低,且研究组显著低于对照组(P<0.05)。治疗后,两组的miR-4485-3p、miR-1469水平均升高,基质金属蛋白酶-2(MMP-2)、基质金属蛋白酶-9(MMP-9)及基质金属蛋白酶-14(MMP-14)水平均降低,且研究组优于对照组,差异具有统计学意义(P<0.05)。治疗后,研究组的血小板计数、白细胞计数、CD3^(+)、CD4^(+)、CD4^(+)/CD8^(+)高于对照组,CD8^(+)低于对照组,差异具有统计学意义(P<0.05)。结论 复方苦参注射液联合FOLFOX4化疗方案有助于改善胃癌患者的血清指标与免疫功能,有效保护骨髓造血功能,促进病情转归,临床可进一步推广运用。

基于网络药理学探讨苦参治疗结直肠癌活性成分、作用靶点及潜在作用机制

目的使用网络药理学方法分析抗肿瘤中药苦参活性成分及其治疗结直肠癌的潜在靶点与作用机制。方法通过中药系统药理学数据库与分析平台(TCMSP)数据库筛选中药苦参活性成分,并使用PubChem数据库验证所收集活性成分化合物结构,运用SwissTargetPrediction数据库反向分子对接预测苦参活性成分可能作用靶点。采用GeneCards、DisGeNET、TTD、MalaCards数据库预测结直肠癌疾病靶点,通过Cytoscape 3.8软件构建“药物-活性成分-靶点-疾病”关系网络图,利用STRING数据库分析苦参-结直肠癌共同靶蛋白PPI蛋白间相互作用网络,采用DAVID数据库对关键靶点进行基因本体论(GO)富集分析以及京都基因和基因组百科全书(KEGG)通路富集分析。结果共筛选获得中药苦参活性成分45个,通过调控结直肠癌相关作用靶点54个,参与体内信号传导、蛋白质磷酸化、凋亡等生物学过程,并通过调控癌症相关信号通路、PI3K-Akt信号通路、癌症蛋白聚糖信号通路等途径发挥治疗作用。结论中药苦参能够通过多途径、多靶点协同发挥抗结直肠癌作用。

复方苦参注射液通过调控巨噬细胞极化改善大鼠急性放射性口腔黏膜炎的机制研究

目的从巨噬细胞极化角度探讨复方苦参注射液(Compound Kushen Injection,CKI)对大鼠急性放射性口腔黏膜炎的防治效果及相关机制。方法将72只SPF级雌性SD大鼠按电脑随机抽样法平均分为对照组、模型组和CKI组各24只。将模型组和CKI组暴露于单次30 Gy照射下,对大鼠左侧颊黏膜建立急性放射性口腔黏膜炎模型。CKI组给予复方苦参注射液(1.8 mL/kg)静脉注射,其余各组给予等量0.9%氯化钠溶液。观察照射后各组大鼠一般情况,颊黏膜肉眼观及病理变化。ELISA检测大鼠颊黏膜组织中白细胞介素-6、转化生长因子-β、肿瘤坏死因子-α和白细胞介素-10的浓度水平。免疫荧光法检测大鼠颊黏膜组织中CD86和CD206阳性巨噬细胞数量。RT-PCR和Western Blotting法检测颊黏膜中诱导型一氧化氮合酶(inducible nitric oxide synthase,iNOS)、精氨酸酶1(arginase 1,Arg1)、共刺激分子CD86和CD206 mRNA表达和蛋白水平。结果与模型组比较,CKI组大鼠的一般情况得到改善,颊黏膜炎症明显减轻。与模型组比较,CKI组大鼠颊黏膜组织中CD86+巨噬细胞数量明显减少(P<0.05),M1型巨噬细胞标记物iNOS和CD86 mRNA表达和蛋白水平均显著下降(P<0.05),促炎因子白细胞介素-6和肿瘤坏死因子-α水平显著降低(P<0.05)。与模型组比较,CKI组大鼠颊黏膜CD206+巨噬细胞数量明显升高(P<0.05),M2型巨噬细胞标记物Arg1和CD206 mRNA表达和蛋白水平升高(P<0.05),转化生长因子-β和白细胞介素-10水平明显升高(P<0.05)。结论复方苦参注射液可通过抑制巨噬细胞M1极化,下调促炎因子白细胞介素-6和肿瘤坏死因子-α蛋白表达,同时促进巨噬细胞M2极化,上调抗炎因子转化生长因子-β和白细胞介素-10蛋白表达,从而改善大鼠一般情况,减轻口腔黏膜炎症反应。