古代经典名方,是指至今仍广泛应用、疗效确切、具有明显特色与优势的古代中医典籍所记载的方剂.近年来,我国出台一系列法律法规,积极鼓励开发经典名方.2018年,第一批古代经典名方目录公布,为深入挖掘中医药宝库中的精华开启方便之门.小承气汤出自张仲景《伤寒论》,方由大黄、枳实、厚朴三味药组成,适用于治疗阳明腑实轻证.查阅文献发现,关于小承气汤历史沿革的考证,化学成分、药理研究都已有文献记载,而有关小承气汤临床应用的文献都十分零散.其临床应用所涉及的疾病广泛,但至今未有较为详细的总结.作者将小承气汤的古今文记载、药理作用及其近代临床应用的相关文献进行了整理,并进行归纳.据统计有关"小承气汤临床应用"的文献共有304篇,主要涉及消化系统疾病、术后治疗、呼吸系统疾病及其他.其中治疗消化系统疾病的文献最多,共有151篇,涉及胃部和肠部的共128篇,占总数的42.11％.温故而知新,通过对小承气汤临床应用等信息的统计,以期为其进一步的开发应用提供依据.

对《中华人民共和国药典》2020版一部所收载的处方中含冰片、薄荷或其加工品的成方制剂进行了统计,共305种,占一部成方制剂总量的18.98％.针对成方制剂中冰片、薄荷质量控制情况,分别对鉴别方法、含量测定方法进行了总结,发现两者的质量控制均以薄层色谱法鉴别、气相色谱法含测为主,方法较为成熟但也存在制剂中未对两药进行质量控制的情况.对含冰片、薄荷的中药成方制剂收载品种情况、入药方式、鉴别检查、含量测定及注意事项等内容进行分类统计,总结冰片、薄荷质量控制的现状、规律和不足,以期为含冰片、薄荷的中药成方制剂质量全面控制提供参考和借鉴.

In recent years, small interfering RNA (siRNA) has been widely used in the treatment of human diseases, especially tumors, and has shown great appeal. However, the clinical application of siRNA faces several challenges. Insufficient efficacy, poor bioavailability, poor stability, and lack of responsiveness to a single therapy are the main problems affecting tumor therapy. Here, we designed a cell-penetrating peptide (CPP)-modified metal organic framework nanoplatform (named PEG-CPP33@ORI@survivin siRNA@ZIF-90, PEG-CPP33@NPs) for targeted co-delivery of oridonin (ORI), a natural anti-tumor active ingredient) and survivin siRNA in vivo. This can improve the stability and bioavailability of siRNA and the efficacy of siRNA monotherapy. The high drug-loading capacity and pH-sensitive properties of zeolite imidazolides endowed the PEG-CPP33@NPs with lysosomal escape abilities. The Polyethylene glycol (PEG)-conjugated CPP (PEG-CPP33) coating significantly improved the uptake in the PEG-CPP33@NPs in vitro and in vivo. The results showed that the co-delivery of ORI and survivin siRNA greatly enhanced the anti-tumor effect of PEG-CPP33@NPs, demonstrating the synergistic effect between ORI and survivin siRNA. In summary, the novel targeted nanobiological platform loaded with ORI and survivin siRNA presented herein showed great advantages in cancer therapy, and provides an attractive strategy for the synergistic application of chemotherapy and gene therapy.

目的 建立景参浓缩丸高效液相色谱(HPLC)指纹图谱,并对丹酚酸B、柚皮苷、新橙皮苷进行含量测定.方法 采用Agilent Eclipse Plus C18色谱柱(4.6 mm × 250 mm,5 μm);流动相为甲醇-0.1％磷酸水,梯度洗脱;检测波长278 nm;流速1.0 mL·min-1;柱温35℃;进样量10μL,根据11批样品的色谱图数据建立景参浓缩丸的指纹图谱并确立共有峰;通过HPLC法测定基准样品中丹酚酸B、柚皮苷、新橙皮苷的含量.结果 11批景参浓缩丸的HPLC图谱中有23个共有峰,相似度＞0.99,指认了其中红景天苷、特女贞苷、丹酚酸B、柳穿鱼叶苷、柚皮苷、新橙皮苷、丹参酮Ⅰ、隐丹参酮、丹参酮ⅡA 9个色谱峰成分;所建立的3种指标成分含量测定方法稳定性、重复性、线性关系、加样回收率良好,符合要求.结论 所建立的景参浓缩丸HPLC指纹图谱和指标成分的含量测定方法具有良好的稳定性和重复性,可为景参浓缩丸质量控制提供参考.

Polyphyllin I (PPI) is a naturally active steroidal saponin that has good therapeutic effects in various cancers, such as liver and lung cancers. However, owing to its non-selective distribution in various tissues, it is toxic and has side effects on normal human organs while taking effect. To solve this problem, a unique functionalized nanomaterial called metal-organic frameworks (MOFs) was prepared as a targeted nanoparticle for tumor therapy. MOFs are porous coordination polymers that can achieve precise structural and functional adjustability by regulating the organic ligands and metal ions. IRMOF-8 with a multidimensional network topology whose aperture matched the size of PPI was selected to load the PPI. In this study, PPI was loaded into IRMOF-8 via ex situ encapsulation. Drug-loaded nanoparticles (NPs) were coated with polyethylene glycol (PEG) coupled to cell-penetrating peptides (CPPs). The obtained nanoplatform denoted as PEG-CPP44/PPI@IRMOF-8 NPs had a spherical shape, a rough and uneven surface, an average particle size of 202.97 nm, excellent drug loading (33.37%), and showed release behavior. In addition, the NPs showed remarkable targeting selectivity for cellular uptake and in vivo imaging. More importantly, it exhibited good antitumor activity in vivo and in vitro. It not only increased the therapeutic efficiency of PPI for liver cancer but also reduced the damage caused by PPI to normal organs. The preparation of the functional nanoplatform (PEG-CPP44/PPI@IRMOF-8) shows the advantages and highlights of MOF-based drug delivery systems and can help in the follow-up precise treatment of tumors.& COPY; 2023 Vietnam National University, Hanoi. Published by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

中药的本草考证在经典名方的开发中发挥着重要作用.查阅文献发现,现代对旋覆花的研究多集中在化学成分及药理作用等方面,对其名称、基原、产地变迁、采收加工、炮制、药用部位及功效的本草考证仍缺乏报道.经查阅历代本草、医籍、方书,古今所用旋覆花均为菊科植物旋覆花Inula japonica Thunb.的干燥头状花序.在历代本草中旋覆花分布广泛,在明代明确道地产区为河南及湖南,近代在广西、广东等地也有出产.现代资源调查结果发现,旋覆花生于海拔150～2400 m的山坡路旁、湿润草地、河岸和田埂上.旋覆花极少以生品入药,多花开后晒干或采用其炮制品入药.根据考证结果,建议旋覆花选取菊科植物旋覆花Inula japonica Thunb.为基原,以其干燥头状花序入药,未注明特殊要求均可参考《中国药典》处理.

Photodynamic therapy (PDT) and photothermal therapy (PTT) have attracted research interest for their noninvasive nature and selective treatment of tumor tissues. They are effective through the generation of reactive oxygen species (ROS) or heat. Nevertheless, several problems, including low bioavailability and long-lasting cutaneous photosensitivity, have limited their clinical application. In this study, we reported an in situ self-assembly strategy that could improve various biological properties of the photosensitizer in vivo. A photosensitizer connected to a receptor-mediated smart peptide can self-assemble into nanoparticles (NPs) under the force of hydrophobic interaction and then transform into a nanofibrillar network after attaching to the tumor cell surface with the help of the β-sheet-forming peptide KLVFF. The supramolecular structural changes deeply affected the PDT and PTT properties of the photosensitizer on tumors. After being aggregated into the nanostructure, the water solubility and targeting ability of the photosensitizer was ameliorated. Moreover, the improvement of the photothermal conversion efficiency, ROS generation, and tumor retention followed the formation of nanofibrils (NFs). This self-assembly strategy showed the ability of supramolecular nanofibrils to improve the bioavailability of photosensitizers, which provides a new potential treatment avenue for various cancer therapies.

Triptolide (TP) is the major bioactive compound extracted from Tripterygium wilfordii Hook F. It exerts anti-inflammatory, antirheumatic, antineoplastic, and neuroprotective effects. However, the severe hepatotoxicity induced by TP limits its clinical application. Ginsenoside Rb1 has been reported to possess potential hepatoprotective effects, but its mechanism has not been fully investigated. This study was aimed at investigating the effect of ginsenoside Rb1 against TP-induced cytotoxicity in HL-7702 cells, as well as the underlying mechanism. The results revealed that ginsenoside Rb1 effectively reversed TP-induced cytotoxicity in HL-7702 cells. Apoptosis induced by TP was suppressed by ginsenoside Rb1 via inhibition of death receptor-mediated apoptotic pathway and mitochondrial-dependent apoptotic pathway. Pretreatment with ginsenoside Rb1 significantly reduced Bax/Bcl-2 ratio and down-regulated the expression of Fas, cleaved poly ADP-ribose polymerase (PARP), cleaved caspase-3, and -9. Furthermore, ginsenoside Rb1 reversed TP-induced cell cycle arrest in HL-7702 cells at S and G2/M phase, via upregulation of the expressions of cyclin-dependent kinase 2 (CDK2), cyclin E, cyclin A, and downregulation of the expressions of p53, p21, and p-p53. Ginsenoside Rb1 increased glutathione (GSH) and superoxide dismutase (SOD) levels, but decreased the reactive oxygen species (ROS) and malondialdehyde (MDA) levels. Pretreatment with ginsenoside Rb1 enhanced the expression levels of nuclear factor-erythroid 2-related factor 2 (Nrf2), total Nrf2, NAD(P)H: quinone oxidoreductases-1 (NQO-1), heme oxygenase-1 (HO-1), and Kelch-like ECH-associated protein 1 (Keap1)/Nrf2 complex. Therefore, ginsenoside Rb1 effectively alleviates TP-induced cytotoxicity in HL-7702 cells through activation of the Keap1/Nrf2/ARE antioxidant pathway.

目的 优化五味子的提取纯化工艺参数,得到较高含量的五味子总木脂素;并经制剂处方工艺优化,制备得到载药量高、稳定性良好的微乳制剂.方法 采用回流提取、大孔树脂柱洗脱相结合的方法,对五味子木脂素成分进行富集;建立高效液相色谱法,以五味子醇甲等8种成分为指标,考察五味子提取物中总木脂素的含量,明确不同环节的成分转移率;采用超声乳化法制备五味子木脂素微乳,并通过单因素考察,对制剂处方和工艺进行研究.结果 建立的8种木脂素成分同时测定的方法专属性、准确性和精密度等方法学考察均符合要求;五味子提取物总木脂素含量为60.85％,其中五味子醇甲等8种木脂素成分总含量为44.57％;以大豆油为油相,吐温-80为表面活性剂制备微乳,微乳的平均粒径为248.3nm,平均载药量为2.44mg·mL-1,pH值为6.5.结论 建立的五味子提取物中8种成分同时测定方法准确可行,可用于其质量控制;提取纯化得到的总木脂素含量较高、重复性良好;制备的五味子微乳载药量较高、粒径均匀、稳定性良好,可为五味子总木脂素的进一步研究奠定基础.

The introduction of different pore diameters in metal organic frameworks (MOFs) could adjust their drug delivery performance. MOFs with customized structures have potential application value in targeted drug delivery. However, no research on this topic has been found so far. In this report, isoreticular metal organic frameworks (IRMOFs) have been taken as a typical case of tailor-made MOFs, the pore size of which is enlarged (average BJH pore sizes of about 2.43, 3.06, 5.47, and 6.50 nm were determined for IRMOF-1, IRMOF-8, IRMOF-10, and IRMOF-16, respectively), emphasizing the relationship between pore size and model drugs (Oridonin, ORI) and clarifying its potential working mechanism. IRMOF-1, whose pore size matches the size of ORI, has an outstanding drug loading capacity (57.93% by wt) and release profile (about 90% in 24 h at pH 7.4). IRMOF-1 was further coated with polyethylene glycol (PEG) modified with a cell penetrating peptide (CPP44) bound to M160 (CD163L1) protein for targeting of hepatic tumor lines. This nanoplatform (CPP44-PEG@ORI@IRMOF-1) exhibited acid-responsive drug release behavior (37.86% in 10 h at pH 7.4 and 66.66% in 10 h at pH 5.5) and significantly enhanced antitumor effects. The results of cell targeting and in vivo animal imaging indicated that CPP44-PEG@ORI@IRMOF-1 may serve as a tumor-selective drug delivery nanoplatform. Toxicity assessment confirmed that PEGylated IRMOF-1 did not cause organ or systemic toxicity. Furthermore, it is encouraging that the IRMOF-based targeted drug delivery system with pore size modulation showed rapid clearance (most administered NPs are metabolized from urine and feces within 1 week) and avoided accumulation in the body, indicating their promise for biomedical applications. This MOF-based aperture modulation combined with a targeted modification strategy might find broad applications in cancer theranostics. Thus, it is convenient to customize personalized MOFs according to the size of drug molecules in future research.

Metal-organic frameworks (MOFs) are porous coordination polymers formed by metal ions and organic ligands through coordination bonds. In drug delivery applications, MOFs can impart sustained release, targeting, protection of easily degradable drugs, and improved drug solubility. Isoreticular metal-organic framework-8 (IRMOF-8) is a mesoporous MOF with a network topology bridged in the form of an octahedral cluster. Compared with other materials, it has the remarkable advantages of high porosity and a regular pore structure. Curcumin (CUR) is a diketone compound with potent antitumor effects. Due to its poor solubility and stability, its clinical application is limited. Therefore, we used IRMOF-8 as a carrier for the encapsulation of CUR to overcome the shortcomings of CUR itself and expand its clinical application. In this study, IRMOF-8 was synthesized through direct mixing of triethylamine (TEA). In vitro cell experiments demonstrated the biocompatibility of IRMOF-8. Using the solvent adsorption method, CUR was encapsulated by IRMOF-8 with a drug loading content of 58.86 +/- 0.98 wt%. In vitro drug release experiments performed at pH levels of 7.2 and 5.5 showed that the preparation had a sustained-release effect over 7 days. Through cytotoxicity experiments after drug loading, it was found that CUR@IRMOF-8 had a strong cytotoxic effect on HepG2 cells, promoted cell apoptosis and intracellular uptake, decreased mitochondrial membrane potential, and increased reactive oxygen species. Hence, CUR@IRMOF-8 is expected to become an excellent sustained-release preparation for potential applications in tumor treatment.

Metal-organic frameworks (MOFs) with tunable structures, high porosity, and abundant active sites are considered to be promising drug delivery systems (DDSs). In this study, novel MOFs-based nanoparticles (CUR@IRMOF-16) were successfully prepared using Zn-based IRMOF-16 as a carrier and curcumin (CUR) as the model drug. This nanocargo delivery platform has dual capabilities, enabling simultaneous drug delivery and fluorescence imaging. In vitro release experiments showed that nanoparticles were released more quickly under mildly acidic conditions, which proved their potential for tumor microenvironmentresponsive drug release. Through in vitro cell experiments, it was found that the nano-drug platform had high antitumor cytotoxicity, which may be related to the mechanism of increasing intracellular reactive oxygen species (ROS), reducing intracellular mitochondrial membrane potential (MMP), and inducing apoptosis. In addition, confocal laser microscopy showed that CUR@IRMOF-16 could localize to the nucleus to exert an antitumor effect. Meanwhile, CUR@IRMOF-16 exhibited superior antitumor activity compared with pure CUR in vitro experiments. The biocompatibility test of IRMOF-16 showed reasonable biosafety, and no evidence of obvious toxicity was observed in vitro. CUR@IRMOF-16 has unique advantages with regard to pH response, biocompatibility, and antitumor efficacy, indicating that the nanodrug platform is a promising drug delivery carrier with an antitumor effect. (c) 2022 Vietnam National University, Hanoi. Published by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

In this study, the critical quality attributes of Wuzhuyu Decoction reference sample were explored by using characteristic chromatogram, index component content and dry extract rate as indexes.The dissemination relationship of quantity value between medicinal materials-decoction pieces-reference sample was investigated to preliminarily formulate the quality standard of the reference sample.The characteristic chromatogram of 15 batches of Wuzhuyu Decoction was established by high performance liquid chromatography(HPLC) and the similarity analysis was conducted.Common peaks were demarcated and assigned to medicinal materials.Moreover, quantitative determination of limonin, evodiamine, rutaecarpine and ginsenoside Rb_1 of Wuzhuyu Decoction were performed.The dissemination of quantity value was explored combined with dry extract rate, similarity of characteristic chromatogram and transfer rate of index component content.A total of 18 common peaks were identified in the corresponding materials of Wuzhuyu Decoction reference sample, with the similarity of characteristic chromatogram greater than 0.9, and Fructus Evodiae, Radix Ginseng, Rhizoma Zingiberis Recens and Fructus Jujubae contributed 9, 5, 8 and 2 chromatographic peaks, respectively.The index component content of corresponding materials and the transfer rates of medicinal materials-decoction pieces and decoction pieces-reference sample of different batches of Wuzhuyu Decoction reference sample were as follows: the content of limonin was 0.16%-0.51%, and the transfer rates were 83.66%-115.60% and 38.54%-54.58%, respectively; the content of evodiamine was 0.01%-0.11%, the transfer rated were 80.80%-116.15% and 3.23%-12.93%, respectively; the content of rutaecarpine was 0.01%-0.05%, the transfer rates were 84.33%-134.53% and 5.72%-21.24%, respectively; the content of ginsenoside Rb_1 was 0.06%-0.11%, and the transfer rates were 90.00%-96.92% and 32.45%-67.24%, respectively.The dry extract rate of the whole prescription was 22.58%-29.89%.In this experiment, the dissemination of quantity value of Wuzhuyu Decoction reference sample was analyzed by the combination of characteristic chromatogram, index component content and dry extract rate.A scientific and stable quality evaluation method of the reference sample was preliminarily established, which provided basis for the subsequent development of Wuzhuyu Decoction and the quality control of related preparations.

对2020年版《中国药典》(一部)中收载的毒性中药品种与相关中成药的质量标准进行统计,对质量标准中限量检查、含量测定与注意等内容进行总结归纳,分析其质量标准的共性特点和存在的不足,为毒性中药与相关中成药的质量标准提高提供参考和借鉴.

Curcumin (CUR) has a bright future in the treatment of cancer as a natural active ingredient with great potential. However, curcumin has a low solubility, which limits its clinical application. In this study, IRMOF-10 was created by the direct addition of triethylamine, CUR was loaded into IRMOF-10 using the solvent adsorption method, and the two were characterized using a scanning electron microscope (SEM), X-ray diffraction (XRD), dynamic light scattering (DLS), Fourier transform infrared spectroscopy (FTIR), thermogravimetric analysis (TG) methods, and Brunauer–Emmett–Teller (BET) analysis. We also used the MTT method, 4′,6-diamidino-2-phenylindole (DAPI) staining, the annexin V/PI method, cellular uptake, reactive oxygen species (ROS), and the mitochondrial membrane potential (MMP) to perform a safety analysis and anticancer activity study of IRMOF-10 and CUR@IRMOF-10 on HepG2 cells. Our results showed that CUR@IRMOF-10 had a CUR load of 63.96%, with an obvious slow-release phenomenon. The CUR levels released under different conditions at 60 h were 33.58% (pH 7.4) and 31.86% (pH 5.5). Cell experiments proved that IRMOF-10 was biologically safe and could promote curcumin entering the nucleus, causing a series of reactions, such as an increase in reactive oxygen species and a decrease in the mitochondrial membrane potential, thereby leading to cell apoptosis. In summary, IRMOF-10 is an excellent drug carrier and CUR@IRMOF-10 is an effective anti-liver cancer sustained-release preparation.

金属有机骨架材料(metal organic frameworks,MOFs)是由金属离子中心与有机配体连接而成的杂化多孔晶体材料,具有比表面积大、孔径可调、活性位点丰富、生物相容性良好的优点,被广泛用于气体储存、吸附、提取、催化及药物递送等领域.近年来,MOFs在中药研究领域的应用也越来越广泛,主要用于中药有效成分的缓控释放、靶向递送、改善药物的溶解性、增加药物的稳定性、降低药物的毒副作用等.此外,MOFs在中药成分的提取分离及检测方面也有诸多应用.综述近年来MOFs在中药研究领域的应用进展,以期为MOFs在中药研究中的进一步应用提供参考,为中药成分的新型递药系统研究提供新思路.

本文对《中国药典》2020版一部“药材及饮片”部分和“中成药”部分收载的矿物药、含矿物药中成药的品种、性状、鉴别、检查、含量测定等方面的内容进行了总结与分析。根据矿物药中含有的阳离子种类（汞、钙、镁、钠、铁、砷、铝及其他8类）将含矿物药的中成药进行分类统计，包括对矿物药的入药方式、鉴别检查、含量测定以及毒性矿物药用法用量、注意事项等方面，分析了含矿物药的中成药的质量标准控制的现状和不足，整理了“药材及饮片”部分中未收载但中成药处方中含有的矿物药品种（9种），希望能够为进一步丰富《中国药典》中收载的矿物药品种提供参考。通过以上内容的分析，希望能够全面地了解《中国药典》2020版一部中矿物药、含矿物类中成药的质量控制现状，为矿物药的全面质量控制提供借鉴，为更加科学、完整地评价矿物药、含矿物药中成药提供参考。