Bingyou Yang

Lignan constituents from Chloranthus japonicus Sieb.

A new coumarinolignan glucoside named yinxiancaoside C, along with five known benzofuran lignans, have been isolated from the whole plant of Chloranthus japonicus Sieb. The structures of compounds 1–6 were elucidated by chemical and spectroscopic methods including 1D-NMR, 2D-NMR, ESI-MS and HR-ESI-MS. Five known benzofuran lignans were firstly discovered in the Chloranthaceae. In addition, the cytotoxic activity of the isolated compounds against human hepatoma (Hepg-2), ovarian carcinoma (OV420), and breast cancer (MCF-7) cells was investigated by MTT method.

Tangeretin exerts anti-neuroinflammatory effects via NF-κB modulation in lipopolysaccharide-stimulated microglial cells.

Increasing evidence suggests that tangeretin, a flavonoid from citrus fruit peels, exhibits anti-inflammatory properties and neuroprotective effects in animal disease models. However, the underlying molecular mechanisms are not clearly understood. In this study, we investigated whether tangeretin suppresses excessive microglial activation implicated in the resulting neurotoxicity following stimulation with lipopolysaccharide (LPS) in primary rat microglia and BV-2 microglial cell culture models. The results showed that tangeretin decreased the production of nitric oxide (NO), prostaglandin E₂ (PGE₂), tumor necrosis factor alpha (TNF-α), interleukin-1 beta (IL-1β), and interleukin-6 (IL-6), in a dose-dependent manner. Additionally, it inhibited the LPS-induced expression of nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) (examined at the protein level) as well as TNF-α, IL-1β, and IL-6 (examined at the mRNA level) in microglial cells. To explore the possible mechanisms underlying these inhibitions by tangeretin, we examined the mitogen-activated protein kinase (MAPK) protein levels and the NF-κB protein signaling pathway. Tangeretin clearly inhibited LPS-induced phosphorylation of ERK, N-terminal Kinase (JNK), and p38. In addition, tangeretin markedly reduced LPS-stimulated phosphorylation of IκB-α and IKK-β, as well as the nuclear translocation of the p65 subunit of pro-inflammatory transcription factor NF-κB. Taken together, these results support further exploration of the therapeutic potential and molecular mechanism of tangeretin in relation to neuroinflammation and neurodegenerative diseases accompanied by microglial activation.

New anti-inflammatory withanolides from the leaves of Datura metel L.

Nine new withanolides, named daturafolisides A-I (1-9), along with six known compounds (22R)-27-hydroxy-7α-methoxy-1-oxowitha-3,5,24-trienolide-27-O-β-d-glucopyranoside, daturataturin A, daturametelin J, daturataurin B, baimantuoluoside B, 12-deoxywithastramonolide (10-15), were isolated from the leaves of Datura metel L. The structures and absolute stereochemistry of these compounds were elucidated by means of spectroscopic methods including 1D and 2D NMR techniques, mass spectrometry and circular dichroism (CD) analyses. All isolates were evaluated for in vitro anti-inflammatory potential using LPS-stimulated RAW 264.7 murine macrophages. Among them, compounds 1, 2, 14, and 15 exhibited significant inhibition of nitrite production with values of IC50 at 20.9, 17.7, 17.8, and 18.4μM. Compounds 3, 4, 6, and 13 presented moderate inhibitory activities with values of IC50 at 59.0, 52.8, 71.2, and 53.1μM, while the rest compounds displayed weak suppressive effect.

Dammarane-type saponins from Panax quinquefolium and their inhibition activity on human breast cancer MCF-7 cells

A new compound, named quinquefoloside-L(c) (1), together with nine known compounds, was isolated from leaves of Panax quinquefolium, and its structure was elucidated as 3beta,12beta, 20S-trihydroxy-25-methoxydammar-23-ene 3-O-beta-D-glucopyranosyl (1-->2)beta-D-glucopyranosyl-20-O-beta-D-xylopyanosyl (1-->6) beta-D-glucopyranoside (1), on the basis of MS, 1D-and 2D-NMR experiments as well as by chemical degradation. The cytotoxicity of these compounds against human breast cancer MCF-7 cell line was also tested by MTT method.

Purification, characterization and immunomodulatory effects of Plantago depressa polysaccharides

Four purified polysaccharide fractions from seeds of Plantago depressa (PDSP-1, PDSP-2, PDSP-3 and PDSP-4) were obtained by isolation and purification using DEAE-52 cellulose and Sephacryl S-400 HR chromatography. Basic physicochemical properties including molecular weight, chemical composition, FT-IR and glycosidic linkage of these fractions were investigated. They seemed to be homogeneous acidic protein-bound heteropolysaccharides with high molecular weight of over 1000 kDa and contained a lot more β-type glycosidic linkages than α-type. PDSP-3 mainly contained mannose, arabinose and fucose, and the others were rich in arabinose, fucose and galacturonic acid. The immunomodulatory effects of them were assessed by splenocyte proliferation index and production of NO and TNF-α from macrophages. They all showed significant immunomodulatory activities, and PDSP-3 presented the strongest effect. Their observed differences in biological activities were probably due to their structure differences. And monosaccharide compositions, linkage types and molecular weight may affect their immunomodulatory activities.

Optimization of polysaccharides extraction from seeds of Pharbitis nil and its anti-oxidant activity

In the present study, polysaccharides were extracted from Pharbitis nil seeds (PNSs) by ultrasonic extraction method for the first time. Response surface methodology with Box-Behnken design was used to optimize the extraction process of PNS polysaccharides (PNSPs). Highest PNSPs yield 6.01 ± 0.15% that agreed closely with the predicted yield 5.99% were obtained under the optimal conditions as follows: ratio of water to raw material 6.5 mL/g, extraction temperature 49.0 °C, ultrasonic power 61.6 W, and extraction time 32.6 min. Preliminary characterization indicated that the sugar, uronic acid and protein contents of the product were 83.6 ± 1.61, 21.8 ± 1.25 and 16.4 ± 0.88% (w/w), respectively. FT-IR analysis revealed the general characteristic absorption peaks of polysaccharides. Besides, PNSPs showed a remarkable antioxidant activity in vitro in a dose-dependent manner. These may provide theoretical basis for further system research and rational development and utilization of PNS resources.

Compounds from the roots and rhizomes of Valeriana amurensis protect against neurotoxicity in PC12 cells.

Three new germacrane-type sesquiterpenoids, heishuixiecaoline A–C (compounds 1–3), were isolated along with ten known compounds 4–13 from fraction of Valeriana amurensis roots and rhizomes effective against Alzheimer’s disease (AD). The structures of 1–3 were elucidated on the basis of their spectroscopic data. We also investigated the protective effect of compounds 1–13 on the neurotoxicity of PC12 cells induced by amyloid-beta (Aβ25–25), respectively. As a result, germacrane-type sesquiterpenoids 1–4 and lignans 5–7 were seen to afford protection against Aβ-induced toxicity in PC 12 cells. This study will contribute to revealing the chemical basis for the therapeutic effect of V. amurensis against AD.

Two New Withanolide Lactones from Flos Daturae

Chemical investigation of the 50% ethanol eluate fraction from a macroporous resin of flowers of Datura metel L. collected in the Jiangsu Province of China resulted in the isolation of two new withanolides, baimantuoluoline G (1) and baimantuoluoside H (2). Their structures were elucidated as (12β,6β,22R)-1,10-seco-6,12,27-trihydroxy-26-oxo-witha-3,5,24-trienolide-1-oic acid-ε-lactone (1) and (5β,6α,12β,22R)-5,6,12,27-tetra-hydroxy-1,26-dioxo-witha-2,24-dienolide-27-O-β-glucopyranoside (2) on the basis of extensive spectroscopic analysis (1D, 2D-NMR and HRESIMS) and chemical studies.

The Progress of Metabolomics Study in Traditional Chinese Medicine Research

Traditional Chinese medicine (TCM) has played important roles in health protection and disease treatment for thousands of years in China and has gained the gradual acceptance of the international community. However, many intricate issues, which cannot be explained by traditional methods, still remain, thus, new ideas and technologies are needed. As an emerging system biology technology, the holistic view adopted by metabolomics is similar to that of TCM, which allows us to investigate TCM with complicated conditions and multiple factors in depth. In this paper, we tried to give a timely and comprehensive update about the methodology progression of metabolomics, as well as its applications, in different fields of TCM studies including quality control, processing, safety and efficacy evaluation. The herbs investigated by metabolomics were selected for detailed examination, including Anemarrhena asphodeloides Bunge, Atractylodes macrocephala Kidd, Pinellia ternate, etc.; furthermore, some valuable results have been obtained and summarized. In conclusion, although the study of metabolomics is at the early phase and requires further scrutiny and validation, it still provides bright prospects to dissect the synergistic action of multiple components from TCM. Overall, with the further development of analytical techniques, especially multi-analysis techniques, we expect that metabolomics will greatly promote TCM research and the establishment of international standards, which is beneficial to TCM modernization.

Triterpenoids from the Roots of Sanguisorba tenuifolia var. Alba

The ethyl acetate soluble fraction from the roots of Sanguisorba tenuifolia was found to have a hypoglucemic effect in alloxan-induced diabetic rats. Two new triterpenoids, identified as 2-oxo-3β,19α-dihydroxyolean-12-en-28-oic acid β-D-gluco-pyranosyl ester (1) and 2α,19α-dihydroxy-3-oxo-12-ursen-28-oic acid β-D-glucopyranosyl ester (4) were isolated from this fraction, along with thirteen known triterpenoids. Their structures were elucidated by chemical and spectroscopic methods. All these compounds demonstrated inhibitory activities against α-glucosidase with IC50 values in the 0.62-3.62 mM range.