Hans Journal of Medicinal Chemistry

Journal Information
ISSN / EISSN : 2331-8287 / 2331-8295
Published by: Hans Publishers (10.12677)
Total articles ≅ 110
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Latest articles in this journal

黎 丹
Hans Journal of Medicinal Chemistry, Volume 10, pp 153-171; https://doi.org/10.12677/hjmce.2022.102015

Abstract:
Selaginella doederleininii is the whole grass of Selaginella doederleinii Hieron, which is pungent taste, neutral in nature, and Selaginella doederleininii has the effects of activating blood flow and dredging meridians, dispersing blood stasis. In order to deeply understand the material base of physicochemical action and its process, the article collects materials about antitumor, an-ti-inflammatory and anti-oxidation by consulting literature, and arranges some chemical composi-tions and working mechanisms. Moreover, this article might provide a reference for the research on Chinese medicine related to Selaginella doederleininii in the future.
李 彤
Hans Journal of Medicinal Chemistry, Volume 10, pp 190-197; https://doi.org/10.12677/hjmce.2022.102018

Abstract:
Rhodiola rosea is a kind of perennial herbaceous plant. It mainly grows in the area of high cold, dry, hypoxia, strong ultraviolet radiation and large temperature difference between day and night at the altitude of 1600~4000 meters. It has strong environmental adaptability and vitality. Salidroside is the main active ingredient and has many pharmacological effects. At present, salidroside has be-come the focus of domestic and foreign scholars. In this paper, the distribution, properties, struc-ture, extraction, determination and pharmacological effects of salidroside were reviewed, providing reference for further study of salidroside.
王 洋
Hans Journal of Medicinal Chemistry, Volume 10, pp 84-95; https://doi.org/10.12677/hjmce.2022.101009

Abstract:
Since the 20th century, antibiotic resistance has been regarded as one of the important factors af-fecting human health, and has posed a serious threat to global economic development. Therefore, the development and application of new antibiotics is urgent. Natural pyrrolomycinsare polyhalo-genated metabolites isolated from the fermentation broth of Actinomyces and Streptomyces. Be-cause of its significant antibacterial activity and novel chemical structure, it has great potential to become a new type of antibacterial agent, and has received extensive attention in the field of medi-cine and pesticides. The research progress on the isolation, biosynthesis, total synthesis and biolog-ical activity of natural pyrrolomycins was reviewed.
扬陈 锐
Hans Journal of Medicinal Chemistry, Volume 10, pp 53-69; https://doi.org/10.12677/hjmce.2022.101007

Abstract:
Objective: To explore the molecular mechanism of Belamcandae Rhizoma and Ephedrae Herba cou-plet medicines (BREHCM) on bronchitis based on molecular docking technology and network pharmacology. Methods: The active components were searched using the traditional Chinese Medi-cine Systems Pharmacology Database Analysis Platform (TCMSP). Gene Cards database was used to screen bronchitis disease targets. The STRING database and Cytoscape were applied to construct the couplet medicines with bronchitis action target network and protein interaction network (PPI). Molecular docking validation of the core components with key targets was performed using Auto-dock Vina. David (v6.8) was used to perform target Gene Ontology (GO) and KEGG pathway analysis. Results: The main active components of BREHCM are quercetin, luteolin, kaempferol, naringin and isorhamnetin. The key targets for bronchitis are TNF, IL-6, IL-1B, mapk1 and VEGFA. The results of molecular docking verification show that the core components can fully combine with the key tar-gets and play a role. Candidate targets mainly enrich TNF signaling pathway, HIF-1 signaling path-way, FoxO signaling pathway and nod like receptor signaling pathway. BREHCM can reduce the contents of immune proteins IgA, IgM, IgG and immune factors IL-1, IL-6 and TNF-a in the blood of rats with bronchopneumonia. Conclusion: The core active ingredients of BREHCM are quercetin, lu-teolin, kaempferol, naringenin, and isorhamnetin, which may regulate TNF signaling pathway, HIF-1 signaling pathway, FoxO signaling pathway, and NOD-like receptor signaling pathway to exert therapeutic effects on bronchitis.
柔江 雨
Hans Journal of Medicinal Chemistry, Volume 10, pp 1-8; https://doi.org/10.12677/hjmce.2022.101001

Abstract:
2-Nnitrobenzaldehyde is an important organic intermediate, which is widely used in organic syn-thesis and pharmaceutical fields. 2-Nitrobenzaldehyde was synthesized from N,N’-dimethylformamide dimethyl acetal (DMFDMA) by condensation oxidation. The isolated prod-uct was analyzed by 1H NMR, 13C NMR and FT-IR spectroscopic methods. The total yield was 88.03%, and the purity was as high as 99.07% (HPLC). The synthetic production process has the advantages of low economic cost, high yield and low environmental pollution, and has obvious advantages over the traditional process.
弘堵 桐
Hans Journal of Medicinal Chemistry, Volume 10, pp 211-223; https://doi.org/10.12677/hjmce.2022.102021

Abstract:
Protein tyrosine phosphatase plays an important role in maintaining protein tyrosine phosphoryla-tion homeostasis. SHP2 is the first confirmed carcinogenic protein tyrosine phosphatase, whose dysregulation is closely related to the occurrence and development of a variety of malignant tu-mors. As the intersection of multiple signaling pathways, SHP2 not only affects the proliferation, metastasis and invasion of tumor cells, but also participates in PD-1/PD-L1-mediated tumor im-mune escape, promoting the occurrence and development of tumors in many aspects. Therefore, SHP2 has been considered as an ideal target for cancer intervention. However, over the years, ef-forts to develop anti-tumor drugs targeting SHP2 have had little success. Hence, SHP2 was once con-sidered as an “undruggable” target. It is only recently that the clinical development of allosteric SHP2 inhibitors, represented by TNO155, has brought hope for tackling this challenging target. So far, there have been 13 candidates in clinical trials. This review briefly introduces the structure and functions of SHP2 and its correlation with tumors, and focuses on the development process and clinical trial progress of allosteric SHP2 inhibitors in recent years.
娟李 玉
Hans Journal of Medicinal Chemistry, Volume 10, pp 204-210; https://doi.org/10.12677/hjmce.2022.102020

Abstract:
Aging has been regarded as an irreversible process, but the course of aging can be delayed with the help of prevention efforts. The effect of extract of caviar on aging in C. elegans was studied. The re-sults showed that relative to the control, the extract of caviar treatment caused a significant in-crease in mean lifespan, and maximum lifespan.
丽周 芳
Hans Journal of Medicinal Chemistry, Volume 10, pp 198-203; https://doi.org/10.12677/hjmce.2022.102019

Abstract:
Objective: To establish an HPLC method for the content of indirubin in Baphicacanthis Cusiae Rhi-zoma et Radix from different habitats. Methods: Agilent ZORBAX SB-C18 column (5 μm, 4.6 × 150 mm) was used. Gradient elution was performed with methanol-0.1% phosphoric acid as mobile phase. The flow rate was 0.8 mL·min−1. The column temperature was 35˚C. The detection wave-length was 290 nm. The injection volume was 10 μL. Results: The sample amount of indirubin showed a good linear relationship with the peak area in the range of 0.63~12.6 μg (r = 0.9999). The average recovery rate was 101.18% (RSD 2.74%). The content of indirubin was determined in the range of 0.040~0.151 mg·g−1. Conclusion: The established method for the determination of Baphic-acanthis Cusiae Rhizoma et Radix is simple, reproducible and reliable. It has certain guiding signif-icance for quality control and integrity evaluation of Baphicacanthis Cusiae Rhizoma et Radix.
唐 思
Hans Journal of Medicinal Chemistry, Volume 10, pp 108-121; https://doi.org/10.12677/hjmce.2022.102011

Abstract:
Objective: To explore the potential mechanism and pharmacodynamic substances of Huangqin-Tang decoction in the treatment of bacterial infection. Methods: A target gene set and ac-tive compounds of Huangqin-Tang decoction against bacterial infection were obtained using the Traditional Chinese Medicine Systems Pharmacology database (TCMSP) and GeneCards databases. STRING database was utilized for Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analysis. The compounds-targets network, compounds-targets-pathways net-work (C-T-P) and proteins-proteins interaction (PPI) network were constructed using Cytoscape 3.8.3 software. Molecular docking was performed to visualize the patterns of interactions between the core compounds and key target. Bacteriostatic experiment in vitro was performed to verify the antibacterial activity of core compounds screened. Result: 43 potential targets and 11 active com-pounds of Huangqin-Tang decoction in treatment of bacterial infection were screened. Network analysis indicated that quercetin, kaempferol, wogonin, and beta-carotene may act on 4 core tar-gets, which were TNF, JUN, IL6 and CASP3, and Toll-like Receptor, NOD-like receptor, NF-kappa B, and RIG-I-like receptor signaling pathway and other pathways played a role in anti-bacterial infec-tion. The molecular docking result showed that the key targets had high binding affinity with four core compounds of Huangqin-Tang decoction. In vitro bacteriostatic experimental verified that quercetin, kaempferol had good anti-inflammatory effect. Conclusion: The network pharmacological strategy integrates molecular docking and bacteriostatic experiment in vitro to reveal the thera-peutic effect and potential mechanism of Huangqin-Tang decoction on bacterial infection, which could provide the way to develop new combination medicines for bacterial infection.
曾 倩
Hans Journal of Medicinal Chemistry, Volume 10, pp 97-107; https://doi.org/10.12677/hjmce.2022.102010

Abstract:
Objective: To compare the content of lupanone and stigmasterol in the root, stem and leaf of Plan-tain plantain, and to provide a strong basis for the resource development and utilization of plantain. Methods: HPLC was used. Diamonsil-C18 (4.6 mm × 250 mm, 5 µm) column; Mobile phase: metha-nol-acetonitrile (50:50 by volume), isometric elution; Detection wavelength: 206 nm; Flow rate: 0.8 ml/min; Column temperature: 30˚C; Injection volume: 10 μL. SPSS 26.0 and SIMCA 11.5 were used to analyze the contents of lupanone and stigmasterol in plantain roots, stems and leaves by statisti-cal analysis, cluster analysis and principal component analysis. Results: The concentrations of lu-panone and stigmasterol had a good linear relationship with the peak areas in the range of 6.26~150.30 µg/ml and 11.26~270.20 µg/ml, respectively. The average recoveries were 95%~105%. The contents of lupanone in the roots and stems of 14 batches of Plantains were 94.46~917.23 µg/g and 180.82~1667.86 µg/g, and the contents of stigmasterol were 117.27~315.08 µg/g and 271.26~1186.74 µg/g. The results of statistical analysis showed that there were significant differences in the contents of lupanone and stigmasterol in different parts of M. japonica from the same plant (P < 0.05), but no significant differences were detected in M. japon-ica leaves. The results of principal component analysis and cluster analysis were consistent with those of statistical analysis. Conclusion: The results showed that the content of banana stem was higher than that of banana root. In order to make better use of drug resources, banana stem could be used as the source of lupanone and stigmasterol.
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