Ophiopogonis Radix (OR) is a traditional Chinese medicine. In recent years, in order to achieve the purpose of drying, bleaching, sterilizing and being antiseptic, improving appearance, and easy storage, people often use sulfur fumigation for its processing. However, changes in the chemical composition of medicinal herbs caused by sulfur fumigation can lead to the transformation and loss of potent substances. Therefore, the development of methods to rapidly reveal the chemical transformation of medicinal herbs induced by sulfur fumigation can guarantee the safe clinical use of medicines. In this study, a combined full scan-parent ions list-dynamic exclusion acquisition-diagnostic product ions analysis strategy based on UHPLC-LTQ-Orbitrap MS was proposed for the analysis of steroidal saponins and their transformed components in sulfur-fumigated Ophiopogonis Radix (SF-OR). Based on precise mass measurements, chromatographic behavior, neutral loss ions, and diagnostic product ions, 286 constituents were screened and identified from SF-OR, including 191 steroidal saponins and 95 sulfur-containing derivatives (sulfates or sulfites). The results indicated that the established strategy was a valuable and effective analytical tool for comprehensively characterizing the material basis of SF-OR, and also provided a basis for potential chemical changes in other sulfur-fumigated herbs.

Ophiopogonis Radix is a well-known Traditional Chinese Medicine and functional food that is rich in polysaccharides and has fructan as a characteristic component. In this study, an inulin neoseries-type fructan designated as OJP-W2 was obtained and characterized from Ophiopogonis Radix, and its potential therapeutic effect on liver fibrosis in vivo were investigated. Structural studies revealed that OJP-W2 had a molecular weight of 5.76 kDa and was composed of glucose and fructose with a molar ratio of 1.00:30.87. Further analysis revealed OJP-W2 has a predominantly lineal (1-2)-linked β-D-fructosyl units linked to the glucose moiety of the sucrose molecule with (2-6)-linked β-D-fructosyl side chains. Pharmacological studies revealed that OJP-W2 exerted a marked hepatoprotective effect against liver fibrosis, the mechanism of action was involved in regulating collagen deposition (α-SMA, COL1A1 and liver Hyp contents) and TGF-β/Smads signaling pathway, alleviating liver inflammation (IL-1β, IL-6, CCL5 and F4/80) and MAPK signaling pathway, and inhibiting hepatic apoptosis (Bax, Bcl-2, ATF4 and Caspase 3). These data provide evidence for expanding Ophiopogonis Radix-acquired fructan types and advancing our understanding of the specific role of inulin neoseries-type fructan in liver fibrosis therapy.

The purpose of this study was to ascertain the fresh processing technology of Cut Ophiopogonis Radix using a multi-index evaluation. This study comprehensively evaluated the fresh processing technology of sliced Cut Ophiopogonis Radix by investigating the cutting methods, cutting thickness, and drying conditions, and referring to The Chinese Pharmacopoeia 2020 edition. The appearance traits, internal quality (extract, total saponins, total flavonoids, total polysaccharides), and drying efficiency were used as evaluation indexes. The physical attributes of Cut Ophiopogonis Radix were found to vary based on the processing techniques employed. The shape, surface characteristics, texture, and color were observed to differ across the different methods. Notably, the apparent quality of Cut Ophiopogonis Radix was superior in samples processed using A1B1C1, A1B2C2, and A3B1C3 techniques. Drying time and energy consumption of Cut Ophiopogonis Radix produced by the A1B2C2 and A2B1C2 processes were less than those of other treatments, making them the optimal process for fresh processing Cut Ophiopogonis Radix. The impact of the cutting method and thickness on the extract was found to be statistically insignificant (P > 0.05). However, the drying method was observed to have a significant impact on the extract (P < 0.05). The cutting method, Cut thickness, and drying method did not affect the total saponin content (P > 0.05), but they had significant effects on the total polysaccharide and flavonoid contents (P < 0.01). Total polysaccharides were most affected by the cutting method, while total flavonoids were most affected by the drying condition. Based on the characteristics and internal quality, the fresh processing technology for Cut Ophiopogonis Radix was determined: fresh Ophiopogonis Radix was sliced to a thickness of 2-4 mm and dried at 55°C or a low temperature. The feasibility of Cut Ophiopogonis Radix is improved through its fresh processing. According to the evaluation indices, it is recommended to utilize the novel processing technique involving \"fresh Ophiopogonis Radix\" with fresh cuts, a cut thickness ranging from 2 to 4 mm, and drying at a temperature of 55℃ or through low-temperature drying. The Cut Ophiopogonis Radix exhibited favorable appearance and internal characteristics, thereby furnishing a scientific basis and innovative insights for the production of ophiopogon decoction slices.

The effects of drying temperature and air velocity on the drying characteristics, color, bioactive compounds, rehydration ratio, and microstructure of Ophiopogonis Radix during hot air impingement drying (HAID) were explored in the current study. The experimental results showed that the drying temperature and air velocity had a significant impact on the drying characteristics and quality attributes of dried products except for the rehydration ratio. The drying time decreased from 720 to 240 min with the increase of drying temperature from 50 to 70 °C. Increasing the air velocity from 6 to 12 m/s enhanced the drying process of Ophiopogonis Radix, while the extension of air velocity to 15 m/s lowered the drying rate. The samples that were dried at a lower drying temperature obtained lower color difference. Properly increasing the drying temperature or air velocity could increase the total polysaccharide and flavonoid contents of dried products. Additionally, a back-propagation neural network (BPNN) model was developed to predict the moisture ratio of Ophiopogonis Radix during the drying process. The optimal BPNN with 3-11-1 topology were obtained to predict the moisture ratio of Ophiopogonis Radix during HAID and performed with an acceptable performance.

Ophiopogonis Radix, also known as \"Maidong\" (MD) in China, is frequently sulfur-fumigated (SF) in the pretreatment process of MD to improve the appearance and facilitate preservation. However, the process leads to changes in chemical composition, so it is essential to develop an approach to identify the chemical characteristics between nonfumigated and sulfur-fumigated products. This paper provided a practical method based on UPLC-QTOF-MS combined Global Natural Products Social Molecular Networking (GNPS) with multivariate statistical analysis for the characterization and discrimination of MD with different levels of sulfur fumigation, high concentration sulfur fumigation (HS), low concentration sulfur fumigation (LS) and without sulfur fumigation (WS). First, a number of 98 compounds were identified in those MD samples. Additionally, the results of Principal component analysis (PCA) and Orthogonal partial least-squares-discriminant analysis (OPLS-DA) demonstrated that there were significant chemical differences in the chemical composition of MD with different degrees of SF. Finally, fourteen and sixteen chemical markers were identified upon the comparison between HS and WS, LS and WS, respectively. Overall, these results can be able to discriminate MD with different levels of SF as well as establish a solid foundation for further quality control and pharmacological research.

Ophiopogonis Radix, also known as Maidong in Chinese, is largely produced in the Sichuan and Zhejiang provinces: \"Chuan-maidong (CMD)\" and \"Zhe-maidong (ZMD),\" respectively. This study aimed to distinguish and evaluate the quality of CMD and ZMD. In this study, the tubers of CMD and ZMD were investigated using UPLC-Q/TOF-MS, GC-MS, and LC-MS methods, respectively. Overall, steroidal saponins, homoisoflavonoids, amino acids, and nucleosides were quickly identified. Furthermore, multivariate statistical analysis revealed that CMD and ZMD could be separated. Moreover, CMD showed higher levels of 4-aminobutanoic acid, glycine, l-proline, monoethanolamine, and serine than ZMD. Besides, the levels of chlorogenic acid, traumatic acid, cytidine, cadaverine, pyridoxine 5-phosphate, glutinone, and pelargonidin 3-O-(6-O-malonyl-β-d-glucoside) were remarkably higher in ZMD than in CMD. Furthermore, these different constituents were mainly associated with galactose metabolism; starch and sucrose metabolism; cysteine and methionine metabolism; valine, leucine, and isoleucine biosynthesis; and glycerophospholipid metabolism. In general, these results showed many differences between the bioactive chemical constituents of Ophiopogon japonicus from different production areas, where ZMD performed better in the quality assessment than CMD, and that UPLC-Q/TOF-MS, GC-MS, and LC-MS are effective methods to discriminate medicinal herbs from different production areas.

In this study, a high-performance thin layer chromatography (HPTLC) method by two step gradient elution with two mobile phases was developed for the simultaneous analysis of seven constituents in Ophiopogonis Radix. The chromatography was performed on silica gel 60 F254 plate with dichloromethane-methanol-ethyl acetate-water (70:25:12:3, v/v/v/v) and dichloromethane-methanol (300:1, v/v) as the mobile phase for two step gradient elution. Then, the HPTLC profiles were observed after derivatization with 10% sulfuric acid in ethanol solution. The obtained HPTLC images were further analyzed by chemometric approaches and the samples could be clustered based on regions and/or growth years, which were two important factors affecting the constituents in Ophiopogonis Radix. Furthermore, five compounds including ophiopogonin D, ophiopojaponin C, ophiopogonin D\', ophiopogonin C\' and methylophiopogonanone B were screened as potential lipase inhibitors from Ophiopogonis Radix by the HPTLC-bioautographic method. The binding modes and interactions between the five compounds and lipase were further explored by molecular docking analysis. The developed HPTLC method could be used for quality control of Ophiopogonis Radix and screening of the potential lipase inhibitors.

Ophiopogonis Radix is an important Yin-nourishing drug in traditional Chinese medicine(TCM), with the effects of nourishing Yin, promoting fluid production, clearing away heart-fire, and relieving restlessness. It is widely used in clinical practice due to its multiple chemical components and pharmacological effects. The technique "mapping knowledge domains" is an effective tool to quantitatively and objectively visualize the development frontiers and trends of certain disciplines. In this study, TCM research papers related to Ophiopogonis Radix were retrieved from Web of Science(WoS) and CNKI, and the research institutions, journals, and keywords involved were visualized and analyzed using the scientometric software CiteSpace. The co-occurrence network of related research on Ophiopogonis Radix was constructed, and the Ophiopogonis Radix-disease-target network was plotted using Cytoscape 3.8.2. The hot topics in Chinese and English papers were analyzed and the shortcomings in the research on Ophiopogonis Radix were summed up. Furthermore, the development trends were discussed. A total of 1 403 Chinese papers and 292 English papers were included in this study. The analysis of research institutions showed that Beijing University of Chinese Medicine and China Pharmaceutical University were the two research institutions with the largest numbers of papers published. The analysis of journals showed that Hebei Journal of Traditional Chinese Medicine and Journal of Asian Natural Products Research were the two journals with the highest numbers of papers concerning Ophiopogonis Radix. The keyword analysis showed that the research contents of Chinese papers focused on the analysis of medication regularity and clinical observation trials, while the English papers focused on component analysis and pharmacological investigation. Data mining and apoptosis-based pharmacological mechanism might be the research trends in the future.

BACKGROUND: Ophiopogonis Radix, the commonly used traditional Chinese medicine in clinic for treating cardiovascular diseases, is returned to the stomach, lung and heart meridian. It is reported to nourish yin, moisten lung and is used to treat heart yin deficiency syndromes and asthenia of heart and lung, which indicated that Ophiopogonis Radix may have a protective effect on heart disorders. Atherosclerosisis is an important process in the development of cardiovascular diseases and abnormal lipid deposition induced macrophage foam cells is its crucial foundation. Our previous study showed the extract of Ophiopogonis Radix (EOR) ameliorates atherosclerosis in vitro. However, it may protect against cardiovascular diseases through inhibiting macrophage foam cell formation and its potential effective components and mechanisms are still unclear.
OBJECTIVE: Our study aimed to investigate the effect of Ophiopogonis Radix on macrophage foam cell formation and its potential active constituents and mechanisms.
METHODS: Ox-LDL induced macrophage cells were employed to evaluate the effect of Ophiopogonis Radix on macrophage foam cell formation. Then the potential active constituents inhibited formation of macrophage foam cells were screened by biospecific cell extraction and its underlying mechanisms were also explored by Western blot.
RESULTS: The extract of Ophiopogonis Radix was found to significantly inhibit macrophage foam cell formation, evidenced by the decrease of TG and TC and Oil Red O staining analysis in macrophage cells, which indicated that EOR reduced the formation of macrophage foam cells. At the same time, EOR was showed to increase antioxidant capacity in macrophage cells. After treatment with EOR, two potential active components interacted with macrophage foam cells specifically were identified to inhibit macrophage foam cell formation including methylophiopogonanone A and methylophiopogonanone B. Methylophiopogonanone A was then proved to decrease the expression of CD36, Lox-1 and SREBP2, increase the expression of ABCA1 obviously, while the expression of ABCG1 and SREBP1 had no changes.
CONCLUSIONS: In our study, Ophiopogonis Radix was found to protect against atherosclerosis through suppressing ox-LDL induced macrophage foam cell formation and two potential compounds were identified by biospecific cell extraction including methylophiopogonanone A and methylophiopogonanone B. Moreover, methylophiopogonanone A was proved to inhibit foam cells through reducing uptake, synthesis and increasing efflux, which may provide guidance and reference for application of Ophiopogonis Radix and investigation of the effective components of TCMs.

Ophiopogonis Radix can be divided into Zhemaidong (ZMD) and Chuanmaidong (CMD). The main planting areas of ZMD are Cixi City and Sanmen county. The quality and price of Ophiopogonis Radix from different producing areas are different. In this study, the headspace-gas chromatography-ion mobility spectrometry (HS-GC-IMS) method is used to rapidly identify ZMD and CMD. The method is also used to identify ZMD from Cixi and Sanmen by analyzing volatile organic compounds (VOCs). A total of 58 VOCs was obtained from ZMD samples with more abundant signals of which 41 were identified. The peak intensities of all VOCs in ZMD and CMD, Cixi and Sanmen data were averaged and then those VOCs whose peak intensities were distributed outside of mean ± 2 standard deviation (μ ± 2σ) were selected as characteristic markers. We selected 14 characteristic markers to establish the characteristic fingerprint of ZMD and CMD, among the 14 VOCs, ZMD contained more eucalyptus oil compounds than CMD, CMD contained more volatile aldehydes than ZMD. We selected 12 characteristic markers for the establishment of the characteristic fingerprint of ZMD from Cixi and Sanmen. The principal component analysis (PCA) results indicated that both ZMD and CMD or ZMD from Cixi and Sanmen could be effectively divided. The ZMD and CMD as well as ZMD from Cixi and Sanmen were evaluated by partial least squares regression-discriminants analysis (PLS-DA) resulting to be excellent chemical descriptors for sample discrimination. One hundred percent classification rates for both PLS-DA calibration and prediction models were obtained. These results provided a reference for the traceability of species and origin and market standard of Ophiopogonis Radix. PRACTICAL APPLICATIONS: Ophiopogonis Radix can be divided into Zhejiang Ophiopogonis Radix (ZMD) and Sichuan Ophiopogonis Radix (CMD). As far as ZMD is concerned, its producing areas mainly include the traditional planting areas (Cixi City) and new growth areas (Sanmen county). In this paper, the HS-GC-IMS method was adopted to analyze VOCs in Ophiopogonis Radix from different producing areas and then we screen out the respective characteristic VOCs of ZMD and CMD as well as ZMD from Cixi and Sanmen. These characteristic VOCs can effectively identify ZMD and CMD as well as ZMD from Cixi City and Sanmen country to provide a scientific basis for the origin identification of Ophiopogonis Radix.