Application research of radiomics in colorectal cancer: A bibliometric study.

BACKGROUND: Radiomics has shown great potential in the clinical field of colorectal cancer (CRC). However, few bibliometric studies have systematically analyzed existing research in this field. The purpose of this study is to understand the current research status and future development directions of CRC. METHODS: Search the English documents on the application of radiomics in the field of CRC research included in the Web of Science Core Collection from its establishment to October 2023. VOSviewer and CiteSpace software were used to conduct bibliometric and visual analysis of online publications related to countries/regions, authors, journals, references, and keywords in this field. RESULTS: A total of 735 relevant documents published from Web of Science Core Collection to October 2023 were retrieved, and a total of 419 documents were obtained based on the screening criteria, including 376 articles and 43 reviews. The number of publications is increasing year by year. Among them, China publishes the most relevant documents (n = 238), which is much higher than Italy (n = 69) and the United States (n = 63). Tian Jie is the author with the most publications and citations (n = 17, citations = 2128), GE Healthcare is the most productive institution (n = 26), Frontiers in Oncology is the journal with the most publications (n = 60), and European Radiology is the most cited journal (n = 776). Hot spots for the application of radiomics in CRC include magnetic resonance, neoadjuvant chemoradiotherapy, survival, texture analysis, and machine learning. These directions are the current hot spots for the application of radiomics research in CRC and may be the direction of continued development in the future. CONCLUSION: Through bibliometric analysis, the application of radiomics in CRC has been increasing year by year. The application of radiomics improves the accuracy of preoperative diagnosis, prediction, and prognosis of CRC. The results of bibliometrics analysis provide a valuable reference for the research direction of radiomics. However, radiomics still faces many challenges in the future, such as the single nature of the data source which may affect the comprehensiveness of the results. Future studies can further expand the data sources and build a multicenter public database to more comprehensively reflect the research status and development trend of CRC radiomics.

Neuroprotective Iridoids and Lignans from Valeriana amurensis.

Valeriana amurensis (V. amurensis) is widely distributed in Northeast China. In addition to medicines, it has also been used to prepare food, wine, tobacco, cosmetics, perfume, and functional foods. Other studies have investigated the neuroprotective effects of V. amurensis extract. As the therapeutic basis, the active constituents should be further evaluated. In this paper, six new compounds (1-6) were isolated, including five iridoids (Xiecaoiridoidside A-E) and one bisepoxylignan (Xiecaolignanside A), as well as six known compounds (7-12). The neuroprotective effects of 1-12 were also investigated with amyloid ß protein 1-42 (Aß1-42)-induced injury to rat pheochromocytoma (PC12) cells. As a result, iridoids 1 and 2 and lignans 6, 8, and 9 could markedly maintain the cells' viability by 3-(4,5)-dimethylthiahiazo (-z-y1)-3,5-di-phenytetrazoliumromide (MTT) and lactate dehydrogenase (LDH) release assay.

The traditional herb Polygonum hydropiper from China: a comprehensive review on phytochemistry, pharmacological activities and applications.

CONTEXT: Polygonum hydropiper L. (Polygonaceae) (PH) is a traditional Chinese traditional medicine with a pungent flavor and mild drug properties. PH is mainly distributed in the channel tropism in the stomach and large intestine. PH has multiple uses and can be used to treat a variety of diseases for a long time. OBJECTIVE: This review summarizes the phytochemical and pharmacological activities, and applications of PH from 1980 to 2022. We also provide suggestions for promoting further research and developing additional applications of PH. METHODS: The data and information on PH from 1980 to 2022 reviewed in this article were obtained from scientific databases, including Science Direct, PubMed, Science Citation Index, SciFinder Scholar (SciFinder), Springer, American Chemical Society (ACS) Publications, and China National Knowledge Infrastructure (CNKI), etc. Some information was obtained from classic literature on traditional Chinese medicines. The search terms were Polygonum hydropiper, phytochemistry compositions of Polygonum hydropiper, pharmacological activities of Polygonum hydropiper, and applications of Polygonum hydropiper. RESULTS: The comprehensive analysis of the literature resulted in 324 compounds being isolated, identified, and reported from PH. Regarding traditional uses, the majority of phytochemical and pharmacological studies have indicated the diverse bioactivities of PH extracts, flavonoids, and volatile oil elements, including antibacterial, antifungal, insecticidal, antioxidant, and anti-inflammatory. CONCLUSIONS: PH has a long history of diversified medicinal uses, some of which have been verified in modern pharmacological studies. Further detailed studies are required to establish scientific and reasonable quality evaluation standards and action mechanisms of active constituents from PH.

Electrosorption performance on graphene-based materials: a review.

Due to its unique advantages such as flexible planar structure, ultrahigh specific surface area, superior electrical conductivity and electrical double-layer capacitance in theory, graphene has unparalleled virtues compared with other carbon materials. This review summarizes the recent research progress of various graphene-based electrodes on ion electrosorption fields, especially for water desalination utilizing capacitive deionization (CDI) technology. We present the latest advances of graphene-based electrodes, such as 3D graphene, graphene/metal oxide (MO) composites, graphene/carbon composites, heteroatom-doped graphene and graphene/polymer composites. Furthermore, a brief outlook on the challenges and future possible developments in the electrosorption area are also addressed for researchers to design graphene-based electrodes towards practical application.

Differentiation of benign and malignant breast lesions using diffusion-weighted imaging with a fractional-order calculus model.

PURPOSE: To assess the feasibility of using three diffusion parameters (D, ß, and µ) derived from fractional-order calculus (FROC) diffusion model for improving the differentiation between benign and malignant breast lesions. METHOD: In this prospective study, 103 patients with breast lesions were enrolled. All subjects underwent diffusion-weighted imaging (DWI) with 12b values. Inter-observer agreement with respect to quantification of parameters by two radiologists was assessed using intraclass coefficient. Conventional apparent diffusion coefficient (ADC) and three FROC model parameters D, ß, and µ were compared between the benign lesion and malignant lesion groups using the Mann-Whitney U test. Then, a comprehensive prediction model was created by using binary logistic regression. Receiver operating characteristic (ROC) curve analysis was performed to evaluate the diagnostic performance of the parameters using histopathological diagnosis as the reference standard. RESULTS: The FROC parameters and ADC all exhibited significant differences between benign lesions and malignant lesions (P＜0.001). Among the individual parameters, the sensitivity of µ was higher than ADC (95.92% for µ vs 91.84% for ADC), and the specificity of ß was higher than ADC (72.22% for ß vs 70.37% for ADC). The combination of ADC and FROC parameters (D and ß) generated the largest area under the ROC curve (0.841) when compared with individual parameters, indicating an improved performance for differentiating benign lesions from malignant lesions. CONCLUSIONS: This study demonstrated the feasibility of using the FROC diffusion model to improve the accuracy of identifying malignant breast lesions.

Two new triterpene glycosides with antiproliferative activities on HepG2 from Phytolacca acinosa fruit fermentation broth.

Two new oleanane-type triterpene glycosides, phytolasides A (1) and B (2), and six known ones (3-8), were isolated from Phytolacca acinosa fruit fermentation broth. Their structures were elucidated by HR-ESI-MS and 1 D- and 2 D-NMR spectroscopic methods. Antiproliferation of compounds 1 and 2 against HepG2 cells was examined by using CCK8 assays.

An Effective Chromatography Process for Simultaneous Purification and Separation of Total Lignans and Flavonoids from Valeriana amurensis.

An effective chromatography process was developed and validated for simultaneous purification and separation of total lignans and flavonoids from Valeriana amurensis. The total lignans and flavonoids in Valeriana amurensis extract were prepurified with macroporous resin column chromatography, and the conditions were optimized as follows: 40 mg/mL Valeriana amurensis extract (2.0 g) solution was loaded onto an AB-8 resin column with a diameter-to-height ratio of 1:7, followed by adsorption for 6 h; then, the column was eluted successively with 5 BV water and 10% and 50% ethanol at a flow rate 2 BV/h. The obtained 50% ethanol fraction was further repurified and separated by polyamide resin column chromatography to obtain the total lignans and flavonoids, respectively. The chromatography conditions were optimized as follows: a 50% ethanol fraction (1.0 g) was mixed with 1.0 g polyamide resin and loaded onto a polyamide resin (60-100 mesh) column with a diameter-to-height ratio of 1:3; then, the column was eluted successively with 6 BV water and 40% and 80% ethanol at a flow rate of 4 BV/h. The total lignans and flavonoids were obtained from water and 80% ethanol fraction, respectively. The content and recovery of standard compounds in total lignans and flavonoids were analyzed with HPLC-PDA, and the feasibility of the process was confirmed.

The potential of Valeriana as a traditional Chinese medicine: traditional clinical applications, bioactivities, and phytochemistry.

Valeriana plants are members of the Caprifoliaceae family, which include more than 200 species worldwide. We summarized previous reports on traditional clinical applications, bioactivities, and phytochemistry of Valeriana by searching electronic databases of Science Direct, Web of Science, PubMed, and some books. Some Valeriana species have been used as traditional medicines, demonstrating calming fright and tranquilizing mind, promoting Qi and blood, activating blood circulation and regulating menstruation, dispelling wind and eliminating dampness, regulating Qi-flowing to relieve pain, and promoting digestion and checking diarrhea, and treating diseases of the nervous, cardiovascular, and digestive systems, inflammation, gynecology, and others. Pharmacology studies revealed the effects of Valeriana, including sedative, hypnotic, antispasmodic, analgesic, antidepressant, anxiolytic, anticonvulsant, antiepileptic, neuroprotective, antibacterial, antiviral, cytotoxic, and antitumor effects as well as cardiovascular and cerebrovascular system improvements. More than 800 compounds have been isolated or identified from Valeriana, including iridoids, lignans, flavonoids, sesquiterpenoids, alkaloids, and essential oils. Constituents with neuroprotective, anti-inflammatory, cytotoxic, and sedative activities were also identified. However, at present, the developed drugs from Valeriana are far from sufficient. We further discussed the pharmacological effects, effective constituents, and mechanisms directly related to the traditional clinical applications of Valeriana, revealing that only several species and their essential oils were well developed to treat insomnia. To effectively promote the utilization of resources, more Valeriana species as well as their different medicinal parts should be the focus of future related studies. Clinical studies should be performed based on the traditional efficacies of Valeriana to facilitate their use in treating diseases of nervous, cardiovascular, and digestive systems, inflammation, and gynecology. Future studies should also focus on developing effective fractions or active compounds of Valeriana into new drugs to treat diseases associated with neurodegeneration, cardiovascular, and cerebrovascular, inflammation and tumors. Our review will promote the development and utilization of potential drugs in Valeriana and avoid wasting their medicinal resources.

Synergistic removal of U(VI) from aqueous solution by TAC material: Adsorption behavior and mechanism.

The adsorption and recovery of uranium from wastewater is of positive significance to the development of nuclear industry and environmental remediation. The ternary polymer (PZS-co-TA) was prepared from hexachlorocyclotriphosphazene (HCCP), 4,4-sulfonyldiphenol (BPS) and tannic acid (TA) under ultrasonic. TAC was then obtained after carbonization under high temperature from PZS-co-TA. The structure and performance of TAC were analyzed using SEM, EDS, FT-IR, XRD, Raman, BET and TG. The adsorption capacity of TAC for uranium under different static adsorption conditions was investigated. The adsorption process was more consistent with pseudo-second-order model. The maximum adsorption capacity calculated by non-linear Langmuir model was 492.5 mg/g at pH 5.5. The thermodynamic values suggested that the adsorption process was spontaneous and endothermic. Moreover, after five cycles of adsorption-desorption tests, TAC remained effective at adsorbing uranium, implying the introducing of TA to the precursor (PZS-co-TA) could enhance the adsorption capacity for uranium.

Release behavior and mechanism of uranium and thorium from Ta-Nb tailings under simulated rainfall in Jiangxi Province, China.

Tantalum-niobium ore belongs to associated radioactive ore, which is accompanied by a certain amount of radioactive uranium and thorium. The remaining slag is enriched with a large number of radionuclides; after weathering, natural rainfall, and surface water scouring, radioactive elements such as uranium, thorium, and some heavy metal elements are exposed or washed into the soil, which poses a threat to the ecological environment and human health. In this study, for characterization analysis during, before, and after leaching, dynamic simulation experiment was carried out on a Ta-Nb slag sample in Jiangxi, China. From SEM analysis, the soluble substances adsorbed on the slag surface dissolve into the solution after leaching in simulated rainfall, and the remained slag becomes smooth with different particle sizes. The XRD diffraction analysis of the sample showed that after leaching in simulated rainfall, the existing forms of elements are different. pH of the leachate of Ta-Nb slag is 1.79; Ta-Nb slag contains many rare metal elements, nonmetal elements, radioactive elements, and some salt compounds; and the content of thorium is higher than that of uranium by EDS analysis. The release of uranium and thorium is obviously affected by the amount of leachate and pH. Under the lower pH of leaching solution, the release of uranium and thorium is more effective. The results of Fick diffusion theory and Elovich equation show that the release and migration mode of uranium and thorium in Ta-Nb slag are mainly surface elution; under acidic conditions, the release and migration of uranium and thorium are faster. This study provides basic data and scientific information for solving the key problems of pollution control of associated radioactive waste in environmental protection.

[Study on mechanism of Phytolaccae Radix and its split components based on network pharmacology].

This paper aimed to explore the mechanism of the split components of Phytolaccae Radix by means of network pharmaco-logy. Based on the theoretical hypothesis of the nature and taste of traditional Chinese medicine, the chemical components of the separated components of Phytolaccae Radix were selected by using Traditional Chinese Medicine Systems Pharmacology Database(TCMSP) and Traditional Chinese Medicines IntegratedDatabase(TCMID) databases in combination with related literatures. Relevant target analysis was carried out based on PubChem and SwissTargetPrediction databases. Targets corresponding to disease were excavated based on GeneCards for each split component, corresponding potential targets were obtained through mapping the target set of target compounds to disease targets. GO biological process analysis and KEGG pathway enrichment analysis were performed on the mapped targets with the help of DAVID database. Based on Cytoscape software and the corresponding efficacy, the network diagram of "medicinal material-split components-compound-target-pathway" was constructed to explore the mechanism of different efficacy of the separated components of Cytoscape. And the target purgation and diuretic mapping was used as the target of the traditional efficacy of smoothening secretion for the first time. The study explored esculentoside component, fatty oil component and phenolic acid component, a total of 30 target compounds and 301 corresponding targets, involving 44 potential targets for "anti-inflammatory", 50 potential targets for "immunoregulation", 52 potential targets for "smoothening secretion", 28 potential targets for "antibacterial activity", 28 potential targets for "antiviral effect", and 29 potential targets for "antitumor effect". Topological analysis revealed 14 key gene targets such as MAPK8, MAPK14, EGFR and PTGS2. A total of 684 GO entries and 235 KEGG pathways were obtained through bioinformatics enrichment analysis, mainly involving TNF signaling pathway, NF-kappaB signaling pathway and MAPK signaling pathway. This study revealed the multi-component, multi-target, and multi-channel action mechanism of the split components of Phytolaccae Radix, which provided certain basis for the next step to clarify the split components of Phytolaccae Radix through the method of system biology, and injected new content and significance into the study of properties and flavors theory.

Assembly of three-dimensional ultralight poly(amidoxime)/graphene oxide nanoribbons aerogel for efficient removal of uranium(VI) from water samples.

Assembling graphene oxide nanoribbons (GONRs) into three-dimensional (3D) materials with controllable and desired structure is an effective way to expand their structural features and enable their practical applications. In this work, an ultralight 3D porous amidoxime functionalized graphene oxide nanoribbons aerogel (PAO/GONRs-A) was prepared via solvothermal polymerization method using acrylonitrile as monomer and GONRs as solid matrices for selective separation of uranium(VI) from water samples. The PAO/GONRs-A possessed a high nitrogen content (13.5%), low density (8.5 mg cm-3), and large specific surface area (494.9 m2 g-1), and presented an excellent high adsorption capacity of uranium, with a maximum capacity of 2.475 mmol g-1 at a pH of 4.5, and maximum uranium-selectivity of 65.23% at a pH of 3.0. The results of adsorption experiments showed that U(VI) adsorption on PAO/GONRs-A was a pH-dependent, spontaneous and endothermic process, which was better fitted to the pseudo-second-order kinetic model and Langmuir isotherm model. Both X-ray photoelectron spectroscopy (XPS) and density functional theory (DFT) calculations revealed that U(VI) adsorption on PAO/GONRs-A mainly did rely on the amidoxime groups anchored on the aerogel while UO2(PAO)2(H2O)3 was dominant after interaction of uranyl with PAO/GONRs-A. Therefore, as a candidate adsorbent, PAO/GONRs-A has a high potential for the removal of uranium from aqueous solutions.

Clinical application and mechanism of traditional Chinese medicine in treatment of lung cancer.

ABSTRACT: Lung cancer is a malignant tumor characterized by a rapid proliferation rate, less survivability, high mortality, and metastatic potential. This review focuses on updated research about the clinical application of traditional Chinese medicine (TCM) as an adjuvant therapy to lung cancer treatment and the mechanisms of TCM effect on lung cancer in vitro and in vivo. We summarized the recent 5 years of different research progress on clinical applications and antitumor mechanisms of TCM in the treatment of lung cancer. As a potent adjuvant therapy, TCM could enhance conventional treatments (chemotherapy, radiation therapy, and epidermal growth factor receptors [EGFRs] tyrosine kinase inhibitors [TKIs]) effects as well as provide synergistic effects, enhance chemotherapy drugs chemosensitivity, reverse drug resistance, reduce adverse reactions and toxicity, relieve patients' pain and improve quality of life (QOL). After treating with TCM, lung cancer cells will induce apoptosis and/or autophagy, suppress metastasis, impact immune reaction, and therapeutic effect of EGFR-TKIs. Therefore, TCM is a promisingly potent adjuvant therapy in the treatment of lung cancer and its multiple mechanisms are worthy of an in-depth study.

Paeoniae radix alba polysaccharides obtained via optimized extraction treat experimental autoimmune hepatitis effectively.

The extraction process of Paeoniae radix alba polysaccharides (PRAP) was optimized as the liquid-solid ratio of 10.65 mL/g, the extraction time of 2.10 h, and the 2 extraction repetitions through a response surface methodology. The chemical profiles of the obtained PRAP were characterized by measuring the contents of total carbohydrates, total phenolics, uronic acid and protein, and by analyzing the FT-IR spectrum and monosaccharide composition. To determine the therapeutic effects of PRAP on experimental autoimmune hepatitis (EAH), we established an EAH mice model. After treated with PRAP, liver and spleen injuries were reduced, and hepatocyte regeneration and liver function were improved. Further study of the mechanism by which PRAP treats EAH showed that PRAP significantly inhibited oxidative stress in the livers of EAH model mice. More importantly, PRAP inhibited immune inflammatory reactions in EAH model mice, including the hepatic infiltration of inflammatory CD4+ and CD8+ T cells, as well as overexpression of inflammatory cytokines IL-2, IL-6 and IL-10, via inhibition of the NF-κB signaling pathway.

Coupled influence of precipitation regimes and seedling emergence time on the reproductive strategy in Chloris virgata.

Precipitation regime and seedling emergence time both influence plant growth and reproduction. However, little attention has been given to the effects of these combined factors on the reproductive strategy of Chloris virgata, which is a vital species in Songnen grassland. Here, we simulated the changes in the precipitation regime and seedling emergence time to evaluate tiller traits and seed production. The results showed that tiller number behaved similarly among three precipitation regimes when sowed on 15 May (T1), while it increased significantly with precipitation regimes when sowed on 15 June (T2) and 15 July (T3). Tiller number decreased significantly with the seedling emergence time under the same water supply treatment. The proportional allocation of reproductive tiller number to total tiller number was significantly higher at T3 than at T1 and T2. Seed number remained similar under different precipitation regimes at T2 and T3, whereas it was significantly lower under low precipitation than under other water levels at T1. Seed number reached the maximum values at T2 under the same level of precipitation treatment. Seed size was significantly lower under low precipitation compared to other water supply treatments and the lowest values in seed size, about 0.5 mg, occurred at T2 under all the precipitation regimes. The lowest values in spike number were under low precipitation at all seedling emergence times. Seed yield exhibited similar trends with seed size under different precipitation regimes, while the greatest gains in these values were at T1 under all the precipitation regimes. Our findings showed that simulated precipitation regimes and seedling emergence time affected the reproductive strategy of C. virgata. Typical and high precipitation, as well as early seedling emergence, will improve the seed yield and seed quality in this species.

The diagnostic value of multi-slice spiral computed tomography in patients with renal carcinoma.

OBJECTIVE: This study was aimed to investigate the characteristics of multi-slice spiral computed tomography (CT) image in kidney cancer patients and its clinical value in staging diagnosis of kidney cancer. MATERIALS AND METHODS: This study included 57 patients who were confirmed as kidney cancer through postoperative pathological examination; they were diagnosed within February 2014 and December 2016 in our hospital. The data obtained from multi-slice spiral CT plain scan and contrast-enhanced CT of these patients was retrospectively analyzed. Moreover, we determined the characteristics of multi-slice spiral CT image for kidney cancer and analyzed their consistency with pathological staging. RESULTS: CT plain scan showed that kidney lumps were mostly found in the prominent renal contour or renal parenchyma, and they were round-like or round in shape. Among the 57 included patients, the tumors of 43 cases showed regular edges, and 14 showed irregular edges. Among the 14 cases, 10 patients had tumors with lobulated edges and 5 with spinous tumor edge. Among all the 57 patients, CT plain scan showed there were 5 cases with slightly higher density, 24 cases with mixed density, 28 cases with equal density or slightly lower density. The range of tumor diameter was 2.1-12.6 cm; the tumor diameter was smaller than 3 cm in 11 cases, 3-7 cm in 34 cases, and larger than 7 cm in 12 cases. In terms of contrast enhancement, the arterial phase was obviously enhanced in 31 cases, moderately and irregularly enhanced in 18 cases, and slightly enhanced in 8 cases. Moreover, the renal parenchymal scan showed a rapid decline in the enhancement and a further decline in the enhancement of renal pelvic tumor; the three stages of enhancement could be expressed in terms of fast forwardness and fast backwardness. A total of 33, 4, 9, and 11 cases were classified as postoperative pathological Stage I, II, III, and IV, respectively; 35, 5, 7, and 10 cases were classified as CT scan Stage I, II, III, and IV, respectively; and 34, 5, 8, and 10 cases were classified as contrast-enhanced CT scan Stage I, II, III, and IV, respectively. No significant difference was observed in the frequency of CT scan, the enhanced stage and pathological stage (P > 0.05). CONCLUSION: CT image of kidney cancer revealed the morphological and enhanced features of this tumor. The consistency between CT stage and pathological stage was high; thus, this method can be applied as a forecasting method for pathological staging.

Value of magnetic resonance images in preoperative staging and resectability assessment of pancreatic cancer.

OBJECTIVE: The objective of this study is to evaluate the clinical value of magnetic resonance images (MRI) in preoperative staging and resectability evaluation of pancreatic cancer. MATERIALS AND METHODS: Thirty-one pancreatic cancer patients who received operation from January 2012 to May 2017 were included in this study. The upper abdominal MRI of 31 cases were analyzed retrospectively. The results of operation and pathology were compared to evaluate the correlation between MRI staging and postoperative pathological staging of pancreatic cancer. RESULTS: According to pathological staging, there were 12 cases of Stage I, 13 cases of Stage II, 4 cases of Stage III, and 2 case of Stage IV. However, for preoperative MRI stage, there were 13 cases of Stage I, 14 cases of Stage II, 4 cases of Stage III. In addition, there was no significant difference in the distribution frequency of pathological staging and MRI staging (P > 0.05). This finding indicated that the results of MRI staging were consistent with that of postoperative pathological staging. The pathology I/II or III/IV stage of pancreatic cancer patients could be predicted with preoperative abdominal MRI detection, with the sensitivity of 1.00 and the specificity of 0.67. CONCLUSION: MRI was clinically significant in preoperative staging and resectability assessment of pancreatic carcinoma.

Kudinoside-D, a triterpenoid saponin derived from Ilex kudingcha suppresses adipogenesis through modulation of the AMPK pathway in 3T3-L1 adipocytes.

The leaves of Ilex Kudingcha, locally named "Kudingcha" in China, has been traditionally applied for treating obesity. Studies have demonstrated that the ethanol extract of Ilex kudingcha have anti-adipogenic effects. However, the constituent which was responsible for its anti-obesity and its underlying molecular mechanism has not yet been elucidated. This research explored the anti-obesity effect of kudinoside-D which was a main natural component of triterpenoid saponin from the ethanol extract of Ilex kudingcha, on lipid accumulation and the potential mechanism of action of adipogenesis in 3T3-L1 adipocytes. The adipocytes were treated with various concentrations of kudinoside D (0 to 40µM) during differentiation. The image-based Oil Red O staining analyses revealed that KD-D, dose dependently reduced cytoplasmic lipid droplet in 3T3-L1 adipocytes with the IC50 is 59.49µM. Meanwhile, major adipogenic transcription factor peroxisome proliferator-activated receptor γ (PPARγ), CCAAT/enhancer binding protein-α (C/EBPα) and sterol regulatory element-binding protein 1c (SREBP-1c) were significantly repressed as well as their target genes. The phosphorylation of AMP-activated protein kinase (AMPK) and its downstream target phosphorylated-acetyl CoA carboxylase (ACC) expression were also increased. In addition, the inhibitory effects of KD-D on the expressions of PPARγ and C/EBPα were weakened when cells were cotreated with AMPK inhibitor Compound C. These results indicated KD-D exerts anti-adipogenic effects through modulation of adipogenic transcription factors via AMPK signaling pathway. And the current findings demonstrated that KD-D was a potential therapeutic candidate for alleviating obesity and hyperlipidemia.

Iridoids and sfingolipids from Hedyotis diffusa.

Seven new compounds were isolated from the aerial part of Hedyotis diffusa, including three iridoid glycosides, hedyoiridoidside A - C (1-3), two cerebrosides, hedyocerenoside F (4) and G (5), and two new ceramides, hedyoceramide A (6) and B (7). And six known iridoid glycosides (8-13) were also obtained. Their structures were established by their physico-chemical constants and spectroscopic analysis. The cytotoxicity of all compounds against tumor cell lines of human cervical cancer HeLa, human leukemia HL-60, human lung cancer A459, human hepatoma HepG2, human gastric gland carcinoma BCG-823, human nasopharyngeal cancer CNE-2, human colon cancer HCT15, and human prostate cancer PC-3 were also evaluated in vitro. As a result, new compound 1 exhibited evident cytotoxicity to all tumor cell lines, and the IC50 values are from 9.5µM to 28.2µM, while new compound 2 exhibited evident cytotoxicity to Hela, HL-60, A459, HepG2, BGC-823, CNE-2, and HCT15, and the IC50 values are from 15.8µM to 26.2µM. Known compound 11 also exhibited evident cytotoxicity to HL-60, A459, HepG2, BGC-823, CNE-2, and HCT15, and the IC50 values are from 16.5µM to 40.4µM. New compounds 4-7 and known compounds 12 and 13 showed moderate cytotoxicity to some tumor cell lines.

The Antitumor Constituents from Hedyotis Diffusa Willd.

As a TCM, Hedyotis diffusa Willd. has been using to treat malignant tumors, and many studies also showed that the extracts from Hedyotis diffusa Willd. possessed evident antitumor activities. Therefore, we carried out chemical study on Hedyotis diffusa Willd. and investigated the cytotoxicity of the obtained compounds on a panel of eight tumor cell lines. As a result, four new compounds were isolated from Hedyotis diffusa Willd., including three iridoid glycosides of Shecaoiridoidside A-C (1-3) and a cerebroside of shecaocerenoside A (4). Also, six known iridoid compounds (5-10) were also obtained. The cytotoxicity of all compounds against human tumor cell lines of HL-60, HeLa, HCT15, A459, HepG2, PC-3, CNE-2, and BCG-823 were also evaluated in vitro. New compound 3 exhibited evident cytotoxicity to all tumor cell lines except the Hela, and the IC50 values are from 9.6 µM to 62.2 µM, while new compound 4 showed moderate cytotoxicity to all the cell lines, and the IC50 values are from 33.6 µM to 89.3 µM. By contrast, new compound 1 and known compound 9 showed moderate cytotoxicity to HCT15, A459, and HepG2 selectively. Known compound 7 also exhibited moderate cytotoxicity to HCT15 and A459 selectively.