Anti-inflammatory and immunomodulating properties of a sterol fraction from Sideritis foetens Clem

A sterol fraction composed of campesterol (7.6%), stigmasterol (28.4%) and beta-sitosterol (61.1%) was obtained by activity-guided fractionation of the acetone extract of Sideritis foetens Clem. This sterol fraction showed anti-inflammatory activity in in vivo murine models of inflammation. It decreased carrageenan paw oedema in mice after oral administration of 30 and 60 mg/kg and inhibited mouse ear oedema induced by 12-O-tetradecanoylphorbol acetate (TPA) after topical application. Quantitation of the neutrophil specific marker myeloperoxidase (MPO) demonstrated that its topical anti-inflammatory activity was associated with reduction in neutrophil infiltration into inflamed tissues. Non-cytotoxic concentrations of the sterol fraction inhibited leukocyte granular enzyme release (beta-glucuronidase) and superoxide generation. However, it did not shown any significant inhibitory effect on histamine release from mast cells. In vitro modulatory activity towards the classical pathway of the complement system shown by this fraction would correlate with the anti-inflammatory profile shown in vivo.     

Polyphenolic Compounds of Sideritis lycia and Their Anti-Inflammatory Activity

Four phenylpropanoid glycosides lavandulifolioside 1, martynoside 2, verbascoside (=acteoside) 3 and leucosceptoside A 4, were isolated from aerial parts of Sideritis lycia Boiss. et Heldr. (Lamiaceae). Their structures were determined by chromatographic and spectroscopic methods (UV, IR, 1 H-NMR, 13 C-NMR, FAB-MS). These compounds and flavonoid glycosides isolated from the same plant in our previously study were screened for their anti-inflammatory activity using the carrageenan-induced mouse paw edema test. The active compounds were then investigated for their effect on gastric ulceration. Although flavonoid glycosides showed higher activity than the phenylpropanoid glycosides, the gastric ulceration effect of phenylpropanoid glycosides was less than flavonoid glycosides.     

Standardization and stability studies of neuroprotective lipid soluble fraction obtained from Curcuma longa

The lipid soluble fraction of curcuma longa, i.e. herbal medicament (HM) was isolated from rhizome of curcuma longa by solvent extraction method. The identification of chemical constituent present in HM was done with GC, GC–MS. The standardization of HM was done using HPLC method on the basis of three-marker compound isolated, i.e. ar-turmerone, turmerone and curlone. The effect of temperature, pH and light on stability of marker compounds of HM was studied. The composition of marker compound in HM was found to be 50–60%. The content of curcumnoids, another bioactive constituent present in HM was found to be 0.32–0.55%. The HM was found to be stable at different temperature and pH but light sensitive.     

Anti-inflammatory activity of a lipid fraction (lyprinol) from the NZ green-lipped mussel

A lipid-rich extract, preparared by supercritical fluid extraction of fresh stabilized mussel powder (Lyprinol), showed significant anti-inflammatory (AI) activity given therapeutically and prophylactically po to Wistar and Dark Agouti rats developing either (a) adjuvant-induced polyarthritis or (b) collagen(II)-induced autoallergic arthritis, with ED₅₀≤15 mg/kg; c.f. naproxen≥25 mg/kg or various therapeutic oils (flaxseed, evening primrose, fish)≥1800 mg/kg given orally. Lyprinol showed little or no activity in acute irritation assays (carrageenan, kaolin, histamine) indicating it is not mimicking rapid-acting NSAIDs. Incorporating Lyprinol into arthritigenic adjuvants composed of heat-killed Mycobacterium. tuberculosis suspended in olive oil or squalane, effectively prevented arthritis development at a dose of 5 mg/rat. By contrast, ‘dummy adjuvants’ prepared with Mycobacterium tuberculosis and flaxseed, evening primrose or fish oils were still arthritigenic in Dark Agouti rats (doses of oil=90 mg/rat). Lyprinol subfractions inhibited leukotriene-B₄ biosynthesis by stimulated human polymorphonuclear leukocytes in vitro, and prostaglandin-E₂ production by activated human macrophages in vitro. Much of this AI activity was associated with polyunsaturated fatty acids and natural antoxidants (carotenoids, etc.). In contrast to NSAIDs, Lyprinol is non-gastrotoxic in disease-stressed rats at 300 mg/kg po and does not seem to affect platelet aggregation (human, rat). These data show Lyprinol to be a reproducible, relatively stable, source of bioactive lipids with much greater potency than plant/marine oils currently used as nutritional supplements to ameliorate signs of inflammation.     

Study of antidepressant-like activity of an enriched phloroglucinol fraction obtained from Hypericum caprifoliatum

Context: Hypericum caprifoliatum Cham &; Schlecht (Guttiferae) extracts have a potential antidepressant-like effect in rodents. However, the molecular mechanisms by which these extracts exert this effect remain unclear.

Objective: This study evaluated the effect of HC1, a fraction obtained from H. caprifoliatum enriched in phloroglucinol derivatives, on the Na⁺, K⁺ ATPase activity in mouse brain and verified the influence of veratrine on the effect of HC1 in the forced swimming test (FST).

Materials and methods: Veratrine (0.06?mg/kg) and HC1 (360?mg/kg) were given alone or combined i.p. 60 and p.o. 30?min, respectively, before FST. The effect of single and repeated administration (once a day for 3 consecutive days) of HC1 (360?mg/kg) on Na⁺, K⁺ ATPase activity was evaluated ex vivo in the cerebral cortex and hippocampus of mice subjected or not to FST.

Results: HC1 reduced the immobility time (103.15?±?18.67?s), when compared to the control group (183.6?±?9.51?s). This effect was prevented by veratrine (151.75?±?22.19?s). Mice repeatedly treated with HC1 presented a significant increase in Na⁺, K⁺ ATPase activity, both in cerebral cortex (46?±?2.41?nmol Pi/min?mg protein) and hippocampus (49.83?±?2.31?nmol Pi/min?mg protein), in relation to the respective controls (30?±?2.66 and 29.83?±?2.31?nmol Pi/min?mg protein respectively).

Discussion and conclusion: The HC1 antidepressant-like effect on FST might be related to its capacity to inhibit Na⁺?influx. HC1 increases hippocampal and cortical Na⁺, K⁺ ATPase activities possibly through long-term regulatory mechanisms.     

Anti-inflammatory activity of 5-O-demethylnobiletin, a polymethoxyflavone isolated from Sideritis tragoriganum

We have studied the effect of 5- O-demethylnobiletin ( 1) on both the inflammation of mouse ears induced by repeated application of 12- O-tetradecanoylphorbol 13-acetate (TPA) and the acute mouse paw oedemas induced by carrageenan and phospholipase A (2) (PLA (2)), and determined its activity on 5-lipoxygenase (5-LOX) and elastase release/activity. Compound 1 reduced the oedema formation, cell infiltration, and tissue damage in the inflammation induced by TPA in mouse ears, along with the acute oedema induced by carrageenan in mouse paws and the acute PLA (2)-induced oedema in mouse paws. The flavone inhibited leukotriene B (4) formation in rat neutrophils and elastase release in human neutrophils, but did not reduce the expression of cyclooxygenase-2 (COX-2) in murine RAW 264.7 macrophages. These experimental results suggest that 1 may act through a direct inhibition of 5-LOX, without affecting the expression of COX-2.     

Some physico-chemical properties of phallolysin obtained from Amanita phalloides

Summary The molecular weight of phallolysin, the toxic haemolysin from Amanita phalloides, was established by gel chromatography to be 30000 daltons. The isoelectric point (I.P.) was found in Ampholine pH 7–10 at 8.34. In Ampholine pH 7–9 the gel chromatographically homogeneous phallolysin was separated into phallolysin A (I.P. 8.06) and phallolysin B (I.P. 7.49). Sodium dodecylsulphatepolyacrylamide gel electrophoresis indicated a molecular weight of 33000 daltons for phallolysin A.Phallolysin was thermo- and acid-labile. It was relatively stable in alkaline solutions. 8 M urea as well as 0.1% sodium dodecylsulphate caused irreversible denaturation. On the other hand, phallolysin showed resistance to diverse proteases (pepsin, trypsin, -chymotrypsin, subtilisin, pronase E, bromelin, proteinase K) and also -amylase and pancreatin. Treatment with proteinase K did not change the molceular weight and the isoelectric points of phallolysin. Resistance to proteases was not due to inhibition of proteases by phallolysin.with the technical assistance of Melitta HauptSupported by a grant of the Deutsche Forschungsgemeinschaft.     

决明子降血脂有效部位的化学成分

目的 研究决明子降血脂有效部位的化学成分.方法 用色谱法分离有效部位,据理化性质和光谱数据鉴定化合物的结构.结果 从决明子降血脂的有效部位分得6个单体化合物,分别鉴定为钝叶素(Ⅰ)、橙黄决明素(Ⅱ)、钝叶决明素苷(Ⅲ)、钝叶素苷(Ⅳ)、大豆苷(Ⅴ)和cassitoroside(Ⅵ).结论 化合物素Ⅳ、Ⅴ、Ⅵ为首次从决明Cassia obtusifolia L.中分得.