Gastrodia elata Blume and its pure compounds protect BV-2 microglial-derived cell lines against β-amyloid: The involvement of GRP78 and CHOP

Objectives: Gastrodia elata (GE) Blume (Orchidaceae) has been previously known for its therapeutic benefits against neurodegenerative diseases. Microglial activation and death have been implicated in the pathogenesis of a variety of neurodegenerative diseases, including Alzheimer's disease. In this study, GE and its pure components, gastrodin and 4-hydroxybenzyl alcohol (4HBA), were applied to β-amyloid-induced BV2 mouse microglial cells. Materials and Methods Cell viability was assessed by the MTT assay and Western blotting was also performed. Results: β-amyloid-induced cell death was shown to be induced time- and dose-dependently. To examine the cell death mechanism, we confirmed the involvement of ER stress signaling. C/EBP homologous protein (CHOP), a pro-apoptotic ER stress protein, was expressed at high levels but glucose-regulated protein 78 (GRP78), an anti-apoptotic ER stress protein with chaperone activity, was only slightly affected by treatment with β-amyloid. However, pretreatment with GE and its components inhibited the expression of CHOP but increased that of GRP78 in β-amyloid-treated cells. This study also showed that a single treatment with GE extracts, gastrodin, or 4HBA induced the expression of GRP78, a marker for enhanced protein folding machinery, suggesting a protective mechanism for GE against β-amyloid. Conclusions: This study reveals the protective effects of GE against β-amyloid-induced cell death, possibly through the enhancement of protein folding machinery of a representative protein, GRP78, and the regulation of CHOP in BV2 mouse microglial cells.

Flavonoids of enhydra fluctuans exhibits analgesic and anti-inflammatory activity in different animal models

Enhydra fluctuans [Compositae], an edible semi aquatic herbaceous vegetable plant, widely used in traditional system of Indian medicine. Total flavonoids of E. fluctuans [TFEF] were screened for analgesic and anti-inflammatory activity. Analgesic activity was studied in acetic acid induced writhing response and by hot plate method in Swiss albino mice. Anti-inflammatory activity was estimated by carrageenan and histamine induced acute inflammation and Freund's complete adjuvant [FCA] induced chronic inflammation in rats. Two flavonoids, baicalein 7-O-glucoside and baicalein 7-O-diglucoside, were isolated from the ethyl acetate fraction. Oral administration of TFEF at the doses of 200 and 400 mg/kg provide 27.05 and 55.49% protection respectively in acetic acid induced writhing method. It also increased the pain threshold in mice evidenced by hot plate method. TFEF showed more potent anti-inflammatory activity. The results of this study may be attributed to high free radical scavenging and antioxidant potential of the flavonoids present in ethyl acetate fraction of Enhydra fluctuans

Flavonoids of retama raetam, and in vitro antitumor screening of two isoflavones

From the aerial parts of Retama raefam ten flavonoids were isolated and identified as saponarin, genistein 8-C-glucoside, genistein 5-O- methylether, genistein 5,4'-di-O-methylether, alpuminoisoflavone, ephedroidin, luteolin, apigenin and two new flavones, luteolin 4'-O- neohesperidoside and 5,4'-dihydroxy- [3",4''- dihydro- [3",4"-dihdroxy] -2",2"dimethylpyrano [5",6":7,8]-flavone[1]. In vitro antitumor screening of genistein-5-O-methylether and genistein-8-C-glucoside were carried out on sixty human tumor cell lines

N-Glucosides: new phase II metabolites of two barbiturates

The new phase-II N-glucoside metabolites of butobarbitone and pentobarbitone are identified and quantified in human urine after single doses of these drugs. The identification and quantification of these metabolites were carried out by mass spectroscopy technique [accurate mass measurement and high voltage scanning]. It was found that the butobarbitone N-glucoside comprised 26% of the dose with tl/2= 44h, while the pentobarbitone N-glucoside was 43% with t1/2= 40h

Phytochemical study of two plantago species: part II: iridoid glucosides

The isolation of aucubin, plantarenaloside, ixoroside, asperuloside and melampyroside from Plantago major L. and aucubin, plantrenaloside and asperuloside from Plantago lagopus L. [plantagenaceae] is reported. The identification of the isolated iridoid glucosides was carried out by spectroscopic analysis and comparison with authentic materials