Taraxacum mongolicum extract inhibited malignant phenotype of triple-negative breast cancer cells in tumor-associated macrophages microenvironment through suppressing IL-10 / STAT3 / PD-L1 signaling pathways.

ETHNOPHARMACOLOGICAL RELEVANCE: Triple-negative breast cancer (TNBC) is the most aggressive and the worst prognosis breast cancer with limited treatment options. Taraxacum mongolicum (also called dandelion) is a traditional Chinese medicine has been used to treat mastitis, breast abscess, and hyperplasia of mammary glands since ancient times. In modern pharmacological research, dandelion has been proven with anti-breast cancer activities. We previously reported that dandelion extract could induce apoptosis in TNBC cells. However, its anti-tumor effects and mechanisms in the tumor microenvironment have not yet been elucidated. AIM OF THE STUDY: Tumor-associated macrophages (TAMs) play an important role in regulating the interaction between tumor cells and the immune system. The present study aimed to investigate the effects and mechanisms of dandelion extract on TNBC cells under the microenvironment of TAMs, as well as its influence on the polarization of M2 macrophages. MATERIALS AND METHODS: M2 macrophages were induced by phorbol-12-myristate 13-acetate (PMA) and interleukin 4 (IL-4), and verified by flow cytometry, quantitative RT-PCR (qRT-PCR), Western blotting, and ELISA. MDA-MB-231 and MDA-MB-468 TNBC cells were co-cultured with the supernatant of M2 macrophage which providing the TAMs microenvironment. The antitumor activity of dandelion extract in TNBC cells was evaluated by MTT assay. The invasive and migratory capacity of TNBC cells was measured by transwell assays. The expression of protein and gene was assessed by Western blotting and qRT-PCR, respectively. RESULTS: TAMs microenvironment promoted the proliferation, migration, and invasion of TNBC cells. However, dandelion extract inhibited the malignant property of MDA-MB-231 and MDA-MB-468 cells induced by TAMs. Both of TAMs and IL-10 caused STAT3 activation and PD-L1 higher expression, the immunosuppressive molecules in TNBC cells, and this effect can be attenuated by IL-10 neutralizing antibody. Dandelion extract exerted inhibition on STAT3 and PD-L1 in TNBC cells under TAMs microenvironment. Furthermore, in M2 macrophages, dandelion extract remarkably promoted the expression of M1-like marker TNF-α, IL-8, and iNOS, but reduced M2-like marker IL-10, CD206, Arginase-1, and TGF-ß. CONCLUSION: Dandelion extract inhibited the proliferation, migration and invasion of TNBC cells in TAMs microenvironment through suppressing IL-10/STAT3/PD-L1 immunosuppressive signaling pathway. Furthermore, dandelion extract promoted the polarization of macrophages from M2 to M1 phenotype. Thus, our results indicated that dandelion may serve as a promising therapeutic strategy for TNBC by modulating tumor immune microenvironment.

Differentiating Westlake Longjing tea from the first- and second-grade producing regions using ultra high performance liquid chromatography with quadrupole time-of-flight mass spectrometry-based untargeted metabolomics in combination with chemometrics.

There are numerous articles published for geographical discrimination of tea. However, few research works focused on the authentication and traceability of Westlake Longjing green tea from the first- and second-grade producing regions because the tea trees are planted in a limited growing zone with identical cultivate condition. In this work, a comprehensive analytical strategy was proposed by ultrahigh performance liquid chromatography-quadrupole time-of-flight mass spectrometry-based untargeted metabolomics coupled with chemometrics. The automatic untargeted data analysis strategy was introduced to screen metabolites that expressed significantly among different regions. Chromatographic features of metabolites can be automatically and efficiently extracted and registered. Meanwhile, those that were valuable for geographical origin discrimination were screened based on statistical analysis and contents in samples. Metabolite identification was performed based on high-resolution mass values and tandem mass spectra of screened peaks. Twenty metabolites were identified, based on which the two-way encoding partial least squares discrimination analysis was built for geographical origin prediction. Monte Caro simulation results indicated that prediction accuracy was up to 99%. Our strategy can be applicable for practical applications in the quality control of Westlake Longjing green tea.

[Progress on treatment of rheumatoid arthritis with ethnodrugs].

Rheumatoid arthritis(RA) is a chronic autoimmune disease, belonging to the "Arthromyodynia (Bi Zheng)" category in traditional Chinese medicine. However, the ethnomedicine has a unique understanding of RA, with a long-term clinical experience accumulation and significant efficacy in the treatment of RA, and it has now become one of the important means in treatment of RA. On the basis of literature research, the understanding of RA and commonly used Tibetan medicine, Mongolian medicine, Hui medicine and other herbs and preparations were reviewed in this paper, with the aim of providing a reference for its clinical treatment of RA and research and development of innovative drugs.

[Advances on chemical constituents and bioactivities of genus Stellera].

Advance on chemical constituents and pharmacological activities of Stellera plants have been conducted. The chemical constituents include terpenes, coumarins, flavonoids, lignans, volatile oils, and other compounds. Pharmacological studies showed that diterpenoids and biflavones showed strong activities, such as antitumor, anti-HIV, and immune regulations. This review hopes to provide a scientific basis for further research and explorations of the medicinal values of the genus.

Component analysis and free radical-scavenging potential of Panax notoginseng and Carthamus tinctorius extracts.

Panax notoginseng and Carthamus tinctorius are known as traditional medicinal plants, and they also have edible values. To better understand their pharmacological mechanism, the present study assessed the in vitro antioxidant activities of extracts of P. notoginseng (EPN) and C. tinctorius (ECT). In addition, the main components of EPN and ECT were determined by HPLC. The results show that EPN mainly contained saponins, which were effective in scavenging (.)OH and O(.)(2-), while showing a low activity in the DPPH(.) assay. Flavonoids were the main components of ECT and were active in scavenging all three radicals in a dose-dependent manner. In brief, the antioxidant properties of EPN and ECT are distinct and might be complementary, their combined use tending to be more effective in scavenging (.)OH (P<0.05 vs. EPN or ECT).

Three new acylated glycosides from the stems of Casearia velutina and their protective effect against H2O2-induced impairment in PC12 cells.

Chemical investigation of the stems of Casearia velutina led to the isolation and structural elucidation of three new acylated glycosides, casearicosides A-C (1-3), together with 13 known compounds. The structures of the new compounds were established by spectroscopic and chemical methods. These isolates were evaluated for protective effects against H(2)O(2)-induced impairment in PC12 cells and inhibitory activity against snake venom phosphodiesterase I. A brief chemotaxonomy of the genus Casearia is also discussed.

A new seco-friedelolactone acid from the bark and twigs of Itoa orientalis.

A new seco-friedelolactone, named itoaic acid, together with 5 known compounds was isolated from the bark and twigs of Itoa orientalis. The structure was elucidated by means of MS, 1D and 2D NMR techniques. Anti-inflammatory activity against COX-2 was evaluated for several compounds from I. orientalis and another Flacourtiaceae plant Xylosma controversum.

Investigation of two Flacourtiaceae plants: Bennettiodendron leprosipes and Flacourtia ramontchi.

Investigations of two Flacourtiaceae plants, Bennettiodendron leprosipes and Flacourtia ramontchi, resulted in the isolation and structural elucidation of six new constituents including two phenolic glycosides ( 1 and 2), one lignan ( 3), two lignan glycosides ( 4 and 5), and a monoterpene glycoside ( 6), together with 22 known compounds ( 7- 28). The structures of the new compounds were elucidated by spectroscopic analysis and chemical methods. The selected isolates 1, 2, 8- 10, 22- 26, and some phenolic glycosides 29- 42 previously isolated from another Flacourtiaceae plant, Itoa orientalis, were tested against snake venom phosphodiesterase I (PDE I) activity. The result indicated that 22, 30, 32, 34, and 40 exhibited moderate inhibitory activities against PDE I with the values ranging from 13.15 to 20.86 %, and 1, 8, 10, 25, 31, 33, 35, 38, 39, and 41 showed weak inhibitory activity.

Itosides J-N from Itoa orientalis and structure - anti-COX-2 activity relationship of phenolic glycosides.

Two new phenolic glycosides, itosides J (1) and K (2), two new cylcohexenoyl glycosides, itosides L (3) and M (4), a new flavone glycoside, itoside N (5), and echitin (6) were isolated from the extract of the bark, twigs, and leaves of Itoa orientalis, together with 22 known compounds. The structures were elucidated by means of UV, IR, MS, and NMR techniques, and the relative configuration of compound 3 was confirmed by X-ray crystallography. NMR data for 6 are reported for the first time. Compounds 1, 3, 5, and phenolic glycosides 7- 22 were also assayed for anti-inflammatory activity against COX-2. Compounds 8, 10, 12- 14, 16, 19, 24, 26, and 27 showed significant inhibitory effects, with inhibitory rates of 49.7-85.3% at 10 microM.