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Background: Baicalin, a flavonoid glycoside compound present in Scutellaria baicalensis, has shown a wide spectrum of biological activities, but its liposolubility, water-solubility and mucosal permeability are all very poor, which leads to the low concentration in brain and poor bioavailability by oral or intravenous injective administration., Objective: The primary objective of this study was to formulate the Scutellaria baicalensis extract (SBE) with phospholipid to yield Scutellaria baicalensis extract-phospholipid complex (SBEPC) , and to evaluate its pharmacodynamics in the middle cerebral artery occlusion (MCAO)., Methods: The optimal preparation technology of SBEPC was obtained through single-factor test and central composite design-response surface methodology (CCD-RSM), and was characterized with various analytical techniques including SEM, FT-IR and NMR. The storage conditions of SBEPC were established through stability study and the MCAO rat model was investigated through conducting pharmacodynamic studies to screen the appropriate administration and dose of SBEPC as well as to verify the neuroprotective effect of SBEPC on cerebral ischemia-reperfusion injury., Results: The optimized preparation conditions of SBEPC were summarized as follows: the ratio of phospholipids to drug was 2:1, the drug concentration was 3.5 mg/ml, the reaction temperature was 50 °C, and the entrapment efficiency was over 93.00%. Stability studies have demonstrated that SBEPC should be stored under 40 °C in a dry and ventilated place away from light and below 37% humidity. Furthermore, pharmacodynamic studies have found that, compared with SBE, SBEPC could introduce drugs into the brain and better exert the neuroprotective effect on MCAO rats, and the optimal administration and dose concentration of SBEPC were nasal administration and 40 mg/ml, respectively., Conclusion: These findings demonstrate that SBEPC is successfully prepared by CCD-RSM. SBEPC can enhance drugs' ability to enter the brain and improve the bioavailability of drugs in brain, and can effectively exert the neuroprotective effect on cerebral ischemia-reperfusion injury as compared with SBE., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Background: Qian-Yu decoction (QYD) is a traditional Chinese medicinal recipe composed of Radix astragali (Astragalus membranaceus (Fisch.) Bunge var. mongholicus (Bunge) P.K. Hsiao, Fabaceae ), Herba epimedii (Epimedium brevicornum Maxim., Berberidaceae), Herba leonuri (Leonurus japonicus Houtt., Lamiaceae), Cortex phellodendri (Phellodendron chinense Schneid., Rutaceae) and Radix achyranthis bidentatae (Achyranthes bidentata Bl., Amaranthaceae). This study aimed to evaluate the therapeutic activity of QYD against carrageenan-induced chronic prostatic/chronic pelvic pain syndrome (CP/CPPS) in rats and further elucidate its effective components., Methods: Three types of components, total polysaccharides, total flavonoids and total saponins were separately extracted from QYD. Carrageenan-induced CP/CPPS rats were intragastrically administered with lyophilized product of QYD, individual extracts and all the combined forms of extracts for three weeks. Prostatic index (PI) was determined and histopathological analysis was performed. The levels of tumor necrosis factor alpha (TNF-α), interleukin-1 beta (IL-1β), cyclooxygenase-2 (COX-2) and prostaglandin E2 (PEG2) in rat prostate tissues were measured using ELISA. The production of inducible nitric oxide synthase (iNOS) was evaluated by an enzymatic activity assay, and the release of nitric oxide (NO) was determined by a nitrate/nitrite assay., Results: Treatment with QYD significantly ameliorated the histological changes of CP/CPPS rats and reduced the PI by 44.3%, with a marked downregulation of TNF-α (42.8% reduction), IL-1β (45.3%), COX-2 (36.6%), PGE2 (44.2%), iNOS (54.1%) and NO (46.0%). Each of three extracts attenuated the symptom of CP/CPPS, but much more weakly than QYD. The combined administration of three extracts showed efficacy comparable to that of QYD while better than that of any combination of two extracts. A principal component analysis of the six inflammatory mediators as variables indicated that the effects of TS on CP/CPPS were rather different from those of TF and TP, which were similar., Conclusions: QYD can be beneficial in prevention and treatment of CP/CPPS. Polysaccharides, flavonoids and saponins, as the major effective components of QYD, exert a cooperative effect on CP/CPPS.

Three new flavanes and eight known flavonoids were isolated from the fruits of Livistona chinensis. The structure of the new flavanes were established as 2S,3S-3,5,7,3',5'-pentahydroxyflavane (1), 2R,3R-3,5,6,7,8,4'-hexahydroxyflavane (2) and 2R,3R-3,5,6,7,8,3',5'-heptahydroxyflavane (3), respectively, on the basis of chemical and spectroscopic data. The antiproliferative activity against four human tumor cell lines (HL-60, Mata, HepG2 and CNE-1) was evaluated. 1 had significantly antiproliferative effects against HL-60 and CNE-1 with the IC(50) of 0.2 ± 0.01 and 1.0 ± 0.1 μM, respectively, overpowering the reference compound in the assay (cisplatin). Most compounds also exhibited potent antioxidant activity., (Copyright © 2011 Elsevier B.V. All rights reserved.)

A linear free-energy relationship (LFER) equation that is able to provide a valid prediction of the skin permeability coefficients (log Kp) of neutral molecules, ions and ionic species has recently been constructed and optimized. This study aimed to evaluate the feasibility of predicting the skin-permeating components (SPCs) of externally applied herbs using the LFER equation, with Evodiae fructus (EF) taken as a model herb. The log Kp values of the reported chemical components of EF at pH 4.0 were calculated using the LFER equation and their structural descriptors. The results showed that the essential oils, quinolone, acridone and indole alkaloids of EF are more permeable when compared to other main components, such as phenylpropanoids, furoquinoline alkaloids, limonoids and flavonoids. The SPCs of EF were further collected via ex vivo skin permeation experiments, and analyzed by liquid chromatography-high resolution tandem mass spectrometry. A total of 80 SPCs were detected, and part of them were tentatively identified based on their empirical molecular formulae and MS/MS spectra. The SPCs are made up of 58 alkaloids, including 23 or more quinolone alkaloids, 14 or more indole alkaloids and 1 acridone alkaloid, and 22 non-alkaloids, including 7 or more essential oils and 1 flavonoid, which is in good agreement with the prediction by the LFER equation. It is suggested that a log Kp of −7.0 may be considered as a borderline, above which are potential SPCs and below which are non-SPCs. Very interestingly, the primary SPCs give a good explanation to the antihypertensive action of externally applied EF. To sum up, the LFER equation can be used to predict the SPCs of externally applied herbs, and thus to narrow the range of their potential effective components and speed up the pharmacological study. [ABSTRACT FROM AUTHOR]

Highlights • JinYin Hua is the most common ingredient for formulations and indigenous beverages. • Four novel and eleven known bioactive flavonoids were isolated. • All isolated flavonoids showed anti-hepatoma activity in SMCC 7721 cell. • Novel flavonoid 12 also showed significant hepatoprotective activity in vitro. • The isolated flavonoids could serve as nuclei for hepatic related diseases. Abstract Lonicera japonica , a widely used traditional Chinese medicine, possessed antiviral, hepatoprotective, anti-tumor and other activities. Meanwhile, L. japonica could be used as healthy food, cosmetics, and so on. Herein, four novel flavonoids, japoflavone A–D (2 - 3 , 5 , 12), together with ten known flavonoids, were isolated and identified on the basis of spectroscopic evidence from L. japonica. In addition, all isolates were assayed for their anti-hepatoma and hepatoprotective activities in vitro. 5 and 8 showed significant anti-hepatoma activity in SMCC 7721 cell with IC 50 values of 13.01 ± 2.62 and 16.69 ± 0.35 μg/ml; Compound 12 showed significant hepatoprotective activity against H 2 O 2 -induced injury in SMCC 7721 and HepG 2 cells (p < 0.001). Drop in the levels of catalase and superoxide dismutase caused by H 2 O 2 were remarkably reversed in a dose-dependent manner after treatment with 12. This study provided a phytochemical evidence for further development and utilization of Lonicera japonica in health products. [ABSTRACT FROM AUTHOR]