Screening for bioactive natural products from a 67-compound library of Glycyrrhiza inflata.

Licorice shows a variety of pharmacological activities. This work aims to discover bioactive natural products from one botanical source of licorice, Glycyrrhiza inflata. A total of 67 free phenolics were isolated to form a compound library. Based on the bioactivities of licorice, these compounds were screened using cell- or enzyme-based bioassay methods. A total of 11 compounds exhibited potent cytotoxic activities against three human cancer cell lines (HepG2, SW480 and MCF7), while showed little toxicity on human normal cell lines LO2 and HEK293T. A number of chalcones showed remarkable anti-inflammatory activities. Among them, 2 (licochalcone B, IC50 8.78µM), 10 (licoagrochalcone C, IC50 9.35µM) and 13 (licochalcone E, IC50 9.09µM) exhibited the most potent inhibitory activities on LPS-induced NO production, whereas 1, 8, 10, 12 and 13 (IC50 13.9, 7.27, 2.44, 6.67 and 3.83µM) showed potent inhibitory activities on NF-κB transcription. Nine prenylated phenolics were found to be PTP1B inhibitors. Particularly, licoagrochalcone A (4), kanzonol C (7), 2'-hydroxyisolupalbigenin (35), gancaonin Q (45), glisoflavanone (50) and glabrol (53) showed IC50 values of 0.31-0.97µM. Compounds 24 (semilicoisoflavone B, IC50 0.25µM), 26 (allolicoisoflavone B, IC50 0.80µM) and 64 (glabridin, IC50 0.10µM) showed noticeable tyrosinase inhibitory activities. Most of the above bioactive compounds were reported for the first time.

Polyacetylenic Oleanane-Type Triterpene Saponins from the Roots of Panax japonicus.

Three new polyacetylenic oleanane-type triterpenoids, baisanqisaponins A-C (1-3), and one new oleanane-type triterpenoid, chikusetsusaponin-V ethyl ester (4), together with 19 known compounds (5-23), were isolated from the roots of Panax japonicus. The structures were elucidated on the basis of spectroscopic analyses and chemical methods. Compounds 1-3 feature a rare panaxytriol group containing a polyacetylene on the saponin skeleton. Neuroprotective activity was evaluated for compounds 1-17, and angiotensin II-induced vascular smooth muscle cell proliferation inhibition was tested for compounds 5-7 and 10-12.

Lignanamides from the roots of Limonium gmelinii (Willd.) Kuntze and their anti-diabetic, cytotoxic and anti-inflammatory activities.

Nine undescribed lignanamides, limoniumins A-I, together with ten known lignanamides and two known phenolics were isolated from ethyl acetate extract of the roots of Limonium gmelinii (Plumbaginaceae). Their structures were determined by spectroscopic analysis including 1D and 2D NMR and HRESIMS experiments. Limoniumin A is the first hybrid lignanamide of phenylpropanoid and coumarin. All tested lignanamides showed significant inhibitory activity against α-glucosidase stronger than positive control and remarkable inhibitory effect to PTP1B with IC50 values less than 10 µM. In addition, some lignanamides exhibited moderate cytotoxic activity against HeLa and MCF-7 cells and anti-inflammatory activity against COX-2 in a dose-dependent way.

New phthalide glycosides from Helichrysum arenarium (L.) Moench.

Two new prenylated phthalide glycosides 1 and 2 were isolated from the whole plant of Helichrysum arenarium, and their structures were elucidated on the basis of spectral data.

[Simultaneous determination of contents of sophoridine, oxymatrine and oxysophocarpine in seed of Sophora alopecuroides by HPLC].

OBJECTIVE: To develop a HPLC method for simultaneous determination of the contents of sophoridine, oxymatrine and oxysophocarpine in seed of Sophora alopecuroides. METHOD: Chromatographic condition included a Phenomenex Gemini C18 (4.6 mm x 250 mm, 5 microm) column and thmobile phase consisting of a mixture of methanol-0.2% phosphatic acid (7:93). The detection wavelength was at 205 nm. The flow rate was 1.0 mL x min(-1) and column temperature was set at 30 degrees C. RESULT: All calibration curves showed good linearity (r > or = 0.9997) within test ranges. The mean recoveries were 100.0%, 97.0% and 97.0% respectively. CONCLUSION: This method is simple, rapid and accurate, and suitable for quality control of S. alopecuroides seed.

Rapid characterisation of flavonoids from Sophora alopecuroides L. by HPLC/DAD/ESI-MSn.

An HPLC/DAD/ESI-MSn method was established to characterise flavonoids in the seeds of Sophora alopecuroides L. All the flavonoids exhibited abundant [M-H]- ions, which triggered data-dependent multistage mass spectrometry fragmentations. Characteristic UV spectra were used to confirm flavonoid subtypes. In total, 22 flavonoids and two phenolic compounds were detected and identified. Five of them were identified by comparing with reference standards, and the others were characterised based on the retention behaviour, multistage fragmentation feature and UV absorption. A total of 19 compounds were reported from S. alopecuroides for the first time. This method accomplished rapid profiling of flavonoid constituents in S. alopecuroides L.