• Motilità gastro-intestinale 

  
  • Coliti e Ulcere 
  • Crohn
  • Proprietà Anti-infiammatorie dei Fitosteroli

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Omega 3 e motilità gastro-intestinale 

L'assunzione di 1-3 cucchiai di Blusterol in un'unica volta porta ad un aumento della motilità gastro-intestinale ed è utilizzato per favorire il transito nelle persone che soffrono di Stipsi cronica.

 L'assunzione moderata e suddivisa nell'arco della giornata invece non incide significativamente sul transito.

Am J Clin Nutr 2002 Jul;76(1):232-8 

Acute ingestion of a meal rich in n-3 polyunsaturated fatty acids results in rapid gastric emptying in humans.

Robertson MD, Jackson KG, Fielding BA, Morgan LM, Williams CM, Frayn KN.

Oxford Centre for Diabetes, Endocrinology and Metabolism, Nuffield Department of Clinical Medicine, University of Oxford, Oxford, United Kingdom. denise.robertson@oxlip.ox.ac.uk

BACKGROUND: n-3 Polyunsaturated fatty acids (PUFAs) have proven benefits for both the development of atherosclerosis and inflammatory conditions. The effects on atherosclerosis may be partly mediated by the observed reduction in fasting and postprandial triacylglycerol concentrations after both acute and chronic n-3 PUFA ingestion. 

OBJECTIVE: The aim of this study was to assess gastric emptying and gastrointestinal hormone release after the consumption of mixed meals rich in n-3 PUFAs or other classes of fatty acids. 

DESIGN: Ten healthy women (aged 50-62 y) completed 4 separate study visits in a single-blind, randomized design. On each occasion, subjects consumed 40 g oil rich in either saturated fatty acids, monounsaturated fatty acids, n-6 PUFAs, or n-3 PUFAs as part of a mixed meal. [1-(13)C]Octanoic acid (100 mg) was added to each oil. Gastric emptying was assessed by a labeled octanoic acid breath test, and concentrations of gastrointestinal hormones and plasma lipids were measured. RESULTS: Recovery of (13)C in breath was enhanced after n-3 PUFA ingestion (P < 0.005). The cholecystokinin response after the n-3 PUFA meal was significantly delayed (P < 0.001), and the glucagon-like peptide 1 response was significantly reduced (P < 0.05).

  CONCLUSION: The inclusion of n-3 PUFAs in a meal alters the gastric emptying rate, potentially as the result of changes in the pattern of cholecystokinin and glucagon-like peptide 1 release.


J Nutr 2002 Sep;132(9):2506-13 

Dietary fish oil increases acetylcholine- and eicosanoid-induced contractility of isolated rat ileum.

Patten GS, Abeywardena MY, McMurchie EJ, Jahangiri A.

CSIRO Health Sciences & Nutrition, Adelaide, South Australia, Australia. glen.patten@csiro.au

The long-chain (n-3) polyunsaturated fatty acids (PUFA) have been reported to exhibit health benefits and healing properties for the gastrointestinal tract.

The aim of this study was to investigate the effects of dietary fish oil supplementation on the in vitro contractility of gut tissue.

 Rats (9 wk old) were fed synthetic diets supplemented with 170 g/kg Sunola oil (SO; 850 g/kg as oleic acid [18:1(n-9)]) or with 100 g/kg of the SO replaced by saturated animal fat (SF) or fish oil (FO) for 4 wk. In the colon, there was no difference in the sensitivity (50% effective concentration) or the maximal contraction among the three dietary groups induced by acetylcholine or 8-iso-prostaglandin (PG)E(2) with the rat colon being relatively insensitive to the thromboxane mimetic U-46619. However, in the ileum, the FO group had greater maximal contractions induced by acetylcholine and 8-iso-PGE(2) compared with the SO and SF groups (P < 0.05), and greater maximal contractions induced by PGE(2), PGF(2alpha) and U-46619 compared with the SF group (P < 0.05). FO feeding increased the incorporation of (n-3) PUFA (eicosapentaenoic [20:5(n-3)], docosapentaenoic [22:5(n-3)] and docosahexaenoic acids [22:6(n-3) primarily at the expense of (n-6) PUFA (linoleic [18:2(n-6)] and arachidonic acids [20:4(n-6)]) in the ileum and colon phospholipid fatty acids (P < 0.05). The FO group had a lower cecal digesta pH (P < 0.001) and a greater butyrate concentration than the SF group (P < 0.05). 

These results suggest that dietary (n-3) PUFA may modulate the contractility of the small intestine.

 

OMEGA 3 nelle  Coliti e Ulcere 

L'assunzione moderata e suddivisa nell'arco della giornata degli Omega 3 esplica il massimo dell'attività antinfiammatoria.  L'associazione con beta-Sitosterolo e Vitamina E ne potenzia l'effetto a livello gastro-intestinale.

APPROFONDIMENTO: ACIDI GRASSI ESSENZIALI NELLA TERAPIA DI MANTENIMENTO DELLA MALATTIA DI CROHN

 

Paola Roggero

Dipartimento di Pediatria - Servizio di gastroenterologia e nutrizione clinica

Clinica De Marchi - Università degli Studi di Milano

 

Le malattie infiammatorie croniche sono condizioni la cui eziopatogenesi rimane ancora oggi  di origine sconosciuta.

I metaboliti dell’acido arachidonico, gli eicosanoidi, vengono ritenuti responsabili della cascata infiammatoria che automantiene la flogosi iniziale. Tali metaboliti vengono prodotti a partire dagli acidi grassi a 20 atomi di carbonio. 

Si possono distinguere due vie metaboliche: 

a - attraverso la via della ciclossigenasi, l’acido arachidonico viene trasformato in prostaglandine, prostacicline e trombossani 


b - attraverso la via della 5-lipossigenasi, attiva a livello dei granulociti eosinofili e dei monociti, deriva la produzione di leucotrieni. 

Il leucotriene B4 e l’acido 5-idrossieicosatetraenoico costituiscono i principali metaboliti flogogeni prodotti a livello dei granulociti 

 

E’ stato dimostrato che il leucotriene B4 è presente nella mucosa colica dei pazienti con malattia infiammatoria cronica intestinale in concentrazioni 50 volte superiori a quelle riscontrabili in condizioni di normalità. Inoltre agisce attraverso un secondo messaggero amplificando la risposta infiammatoria secondaria alla produzione di citochine ad azione flogogena. Infine, avendo elevate proprietà chemiotattiche, favorisce la migrazione di cellule direttamente responsabili dei processi di flogosi.

I farmaci attualmente più utilizzati nella terapia delle malattie infiammatorie croniche intestinali agiscono interferendo a vari livelli di tale cascata infiammatoria. I glucocorticoidi ( cortisonici ) prevengono la formazione di molecole libere di acido arachidonico, attraverso l’inibizione dell’attività delle fosfolipasi A2  e C sui fosfolipidi di membrana. La mesalazina agisce attraverso l’inibizione della 5-lipossigenasi nella mucosa colica.

 

Figura 1 - Via metabolica della Ciclossigenasi

Figura 2 - Via metabolica della 5-Lipossigenasi

 

Lee e coll. suggerirono possibili effetti degli acidi grassi contenuti nell’olio di pesce sui processi metabolici cellulari di tipo infiammatorio. 

L’acido eicosapentaenoico ( EPA ), acido grasso polinsaturo a 20 atomi di carbonio ( Figura 3 ), prodotto dal metabolismo dell’acido α-linolenico (ALA), si differenzia dall’acido arachidonico per la presenza di un doppio legame in più in posizione 17.  

Esso rappresenta un buon substrato per la 5-lipossigenasi e compete con l’acido arachidonico per l’utilizzazione di tale enzima insieme al suo omologo acido docosaesaenoico ( DHA ). L’incorporazione di acido eicosapentaenoico e di docosaesaenoico nelle membrane dei granulociti neutrofili è il presupposto fondamentale per il realizzarsi del meccanismo d’azione competitivo nei confronti  dell’acido arachidonico. Tale effetto comporta una ridotta sintesi di leucotriene B4 e la sintesi di un nuovo leucotriene B5 il quale non possiede alcun effetto flogogeno.

Gli effetti antinfiammatori dell’olio di pesce sono stati verificati su modelli animali, su coliti indotte nel ratto da acido trinitrobenzensulfonico. Accanto agli effetti sulla cascata dell’acido arachidonico, gli acidi grassi omega 3 contenuti nell’olio di pesce, riducono i livelli circolanti e tissutali delle principali citochine flogogene (IL-1,TNFα ) e limitano la sintesi del “platelet activating factor”, fosfolipide con potente azione flogogena.

 

NOTA "VitalOil": in uno studio con pazienti anziani, (pertanto a ridotta attività enzimatica),  l'arrichimento della dieta con 3 gr di ALA - Omega 3 + 3 gr di LA - Omega 6  hanno dimostrato di  elevare i livelli plasmatici di tutti gli acidi grassi Omega 3: - ALA (+100%),    - EPA (+44%) e DHA (+20%)(1) (i  suoi  metaboliti). L'uso di Blusterol-Forte consente di assumere elevate dosi di Omega 3 e di Beta-Sitosterolo ad elevata attività antinfiammatoria .

(per leggere l'abstract dell'articolo clicca sull'icona )

1.   Lee TH, Austen KF. Arachidonic acid metabolism by the 5-lipoxygenase pathway, and the effects of alternative dietary fatty acids. Adv. Immunol. 1986; 39 : 145-75.  

2.   Lee TH, Hoover RL, Williams JD, Sperling RI, Ravalese J, Spur BW, Robinson DR, Corey EJ, Lewis RA, Austen KF. Effect of dietary enrichment with eicosapentaenoic and docosahexaenoic acids on in vitro neutrophil and monocyte leukotriene generation and neutrophil function. N. Engl. J. Med.1985;312 (19):1217-24.

3.   Stenson WF, Cort D, Rodgers J, Burakoff R. Dietary supplementation with fish oil in Ulcerative colitis. 

      Ann. Intern. Med.  1992; 116 (8) : 609-14.

4.   Hawthorne AB, Daneshmend TK, Hawkey CJ, Belluzzi A, Everitt SJ, Holmes GK, Malkinson C, Shaheen MZ, Willars JE. Treatment of Ulcerative colitis with fish oil supplementation : a prospective 12 month randomised controlled trial. Gut 1992; 33 (7) : 922-8.  

5.   Belluzzi A, Brignola C, Campieri M, Pera A, Boschi S, Miglioli M .Effect of an enteric coated fish oil preparation on relapses in Crohn's disease. N Engl J Med 1996 ;334 (24):1557-60.

6.   Romano C, Cucchiara S, Barabino A, Roggero P, Sferlazzas C, Annese V. Omega-3 fatty acids supplementation in pediatric Crohn's disease : Italian multicentric study. Dig. Liv. Dis. 2002; 34 ( Suppl 1 ) : A82.

7.   Almallah YZ, Ewen SW, El-Tahir A, Mowat NA, Brunt PW, Sinclair TS, Heys SD, Eremin O. Distal proctocolitis and n-3 polyunsaturated fatty acids : the mucosal effects in situ. J. Clin Immunol. 2000; 20 (1) : 68-76.

8.   Nieto N,Torres MI, Rios A, Gil A. Dietary polyunsaturated fatty acids improve histological and biochemical alterations in rats with experimental ulcerative colitis. J. Nutr. 2002; 132 (1) : 11-9.  

9.   Lugea A, Videla S, Villaseca J, Guarner F.  Antiulcerogenic and antiinflammatory actions of fatty acids on the gastrointestinal tract. Prostaglandins Leukot Essent Fatty Acids. 1991; 43 (3) : 135-40.

 

ALTRI STUDI

 

Aliment Pharmacol Ther. 2003 Aug 15;18(4):433-42.
 
Essential fatty acid status in paediatric Crohn's disease: relationship with disease activity and nutritional status.

Trebble TM, Wootton SA, May A, Erlewyn-Lajeunesse MD, Chakraborty A, Mullee MA, Stroud MA, Beattie RM.

Institute of Human Nutrition, School of Medicine, University of Southampton, Southampton, UK. tt2@soton.ac.uk

BACKGROUND: Active paediatric Crohn's disease is associated with nutritional deficiencies and altered nutrient intake. The availability of essential fatty acids (linoleic and alpha-linolenic acids) or their derivatives (arachidonic and eicosapentaenoic acids) may alter in plasma and cell membrane phospholipid in protein-energy malnutrition in children and in Crohn's disease in adults. AIM: To investigate the relationship of fatty acid phospholipid profiles with disease activity and nutritional status in paediatric Crohn's disease.
 
 METHODS: The fatty acid (proportionate) composition of plasma and erythrocyte phosphatidylcholine was determined in 30 patients (10.3-17.0 years) stratified into active and quiescent Crohn's disease (paediatric Crohn's disease activity index) and high and low body mass (body mass index centile).
 
 RESULTS: In plasma phosphatidylcholine, active disease activity was associated with a lower level of alpha-linolenic acid compared with that in quiescent disease (P < 0.05). A body mass index below the 50th centile was associated with active Crohn's disease, low linoleic and alpha-linolenic acids and high arachidonic acid (P < 0.05) in plasma phosphatidylcholine, and low alpha-linolenic acid in erythrocyte phosphatidylcholine. These findings could not be explained through differences in habitual dietary fat intake. 
 
CONCLUSION: In paediatric Crohn's disease, a low body mass index centile and high disease activity are associated with altered profiles of essential fatty acids and their derivatives, which may reflect altered metabolic demand.

 


J Gastroenterol. 1995 Nov;30 Suppl 8:98-101. 
Therapeutic efficacy of N-3 polyunsaturated fatty acid in experimental Crohn's disease.

Shoda R, Matsueda K, Yamato S, Umeda N.

Division of Gastroenterology, International Medical Center of Japan, Tokyo, Japan.

We investigated the therapeutic efficacy of n-3 polyunsaturated fatty acids (PUFAs) on trinitro-benzene sulfonic acid (TNBS)-induced colitis in the rats, which condition is considered an experimental Crohn's disease (CD). In rats with TNBS-induced colitis, feeding with an elemental diet (ED) plus 2% n-3 PUEA-rich perilla oil significantly suppressed plasma leukotriene (LT) B4 and ulcer index compared to that in rats fed with ED plus 2% n-6 PUFA-rich safflower oil (34.2 +/- 12.3 s 63.8 +/- 13.2 pg/ml and 8.8 +/- 12.1 vs 66.4 +/- 33.1, P < 0.01, respectively). Moreover, the plasma LTB4 and the ulcer index were significantly correlated (P < 0.05).


Feeding with ED plus 2% alpha-linolenic acid (ALA-omega 3)-rich vegetable oil significantly reduced plasma LTB4 and colonic weight compared to that in rats fed with ED plus 2% eicosapentaenoic acid (EPA)/docosahexaenonic acid (DHA)-rich fish oil in this model (61.6 +/- 10.5 vs 85.0 +/- 20.9 pg/ml and 0.83 +/- 0.13 vs 0.96 +/- 0.08g, P < 0.05, respectively). This study suggested that dietary fat manipulation with perilla oil can reduce colonic damage and that this is correlated with the suppression of plasma LTB4. 

The therapeutic efficacy of A-LA in controlling intestinal inflammation in experimental CD may be superior to that of EPA and DHA.



Br J Nutr. 2002 Jan;87 Suppl 1:S83-8. 
Impact of parenteral n-3 fatty acids on experimental acute colitis.

Campos FG, Waitzberg DL, Habr-Gama A, Logullo AF, Noronha IL, Jancar S, Torrinhas RS, Furst P.

Department of Gastroenterology, University of Sao Paulo Medical School, SP, Brazil. fgcampos@osite.com.br

The present study was undertaken to investigate the effects of parenteral lipid emulsions (LE) enriched with n-3 fatty acids (n-3 FA) in experimental acute colitis. Seventy-four adult male Wistar rats were randomized into six groups, five of which had acetic acid-induced colitis. The animals received a fat-free diet and water ad libitum in individual metabolic cages. By a central venous catheter, saline was infused (0.5 ml/h) into the control groups CS (without colitis) and CC (with colitis), while the test groups received specific LE for 7 days. The n-3/n-6 FA ratio and the lipidic compositions regarding long chain (LCT) and medium chain (MCT) triglycerides were: group L--1:7.7 (LCT, n = 12), M--1:7.0 (MCT and LCT, n = 12), LW-3--1:4.5 (LCT plus n-3 FA, n = 12) and MW-3--1:3.0 (MCT and LCT plus n-3 FA, n = 13). The frequency of diarrhea, oral intake/body weight ratio, intestinal alterations, macrophage cellularity were evaluated and colonic concentrations of leukotrienes (LTB4, LTC4), prostaglandins (PGE2) and thromboxanes (TXB2) were measured. Groups M, MW-3 and LW-3 had less diarrhea than the CC group (P<0.05). Average oral intake/body weight ratio in MW-3 animals was comparable to the CS and better than the CC group. n-3 FA treated rats (LW-3 and MW-3) presented less intestinal inflammatory alterations than CC rats. Mucosal ulcer formation in MW-3 group did not differ from CS rats. M and MW-3 rats had less macrophages in the colon than the CC group. Compared with CC group, lower concentrations of LTB4 in the CS, LW-3 and MW-3 groups; of PGE2 in the CS, M and MW-3 groups; and of TXB2 in the CS and MW-3 groups were found. Mean concentrations of LTC4 did not differ among the groups. Thus, a LCT-containing LE with a low n-3-n-6 ratio does not modify inflammatory colitis manifestations; LE with a high n-3-n-6 ratio reduces diarrhea, preserves oral intake-weight ratio, attenuates morphological consequences and decreases colonic concentrations of inflammatory mediators; MCT/LCT-containing LE with 1:3 n-3-n-6 ratio exerts the most profound beneficial impact on the inflammatory response.


Vopr Pitan. 1996;(6):35-7. 
Optimization of dietary fat composition in erosive and ulcerative diseases of the gastroduodenal area

Matushevskaia VN, Shakhovskaia AK, Karagodina ZV, Lupinovich VL, Korf II, Loranskaia TI, Levachev MM.

Fish oil preparation "Polyen" was used for treatment 21 patients with ulcerative diseases of the stomach or duodenum. The cicatrization of ulcer was diagnosed in 85% of patients treated by "Polyen" and in 60% of those who did not take fish oil. "Polyen" influenced fatty acid composition of erythrocyte membranes and lipid peroxidation. Authors draw a conclusion that omega-3 PUFA's can stimulate the reparative processes.


Food Chem Toxicol. 1995 Jul;33(7):553-8. 
Effect of acute administration of fish oil (omega-3 marine triglyceride) on gastric ulceration and secretion induced by various ulcerogenic and necrotizing agents in rats.

al-Harbi MM, Islam MW, al-Shabanah OA, al-Gharably NM.

Department of Pharmacology, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

The fish oil commercially known as Marine-25 (omega-3 marine triglyceride) is an eicosapentaenoic acid (EPA)-rich oil. It was investigated for its ability to inhibit gastric secretion and to protect the gastric mucosa against the injuries caused by pyloric ligation, non-steroidal anti-inflammatory drugs (NSAIDs--aspirin and indomethacin), reserpine, hypothermic restraint stress and necrotizing agents [0.6 M HCl 0.2 M NaOH or 80% (v/v) aqueous ethanol]. The results showed that the fish oil, at a dose of 5 or 10 ml/kg body weight, provided significant protection in the various experimental models used. It produced a significant inhibition of gastric mucosal damage induced by pyloric ligation, NSAIDs, reserpine or hypothermic restraint ulcers. Fish oil also exerted a significant inhibitory action on gastric mucosal lesions produced by various necrotizing agents. Our findings show that fish oil rich in eicosapentaenoic acid possesses both antisecretory and antiulcerogenic effects.



Gut. 1994 Nov;35(11):1557-61. 

Inhibitory effect of polyunsaturated fatty acids on the growth of Helicobacter pylori: a possible explanation of the effect of diet on peptic ulceration.

Thompson L, Cockayne A, Spiller RC.

Department of Therapeutics, University Hospital, Nottingham.

Diets high in polyunsaturated fatty acids may protect against duodenal ulcer, possibly through inhibiting the growth of Helicobacter pylori. This hypothesis was tested in vitro by incubating H pylori microaerophilically with a range of polyunsaturated fatty acids. omega-3 alpha-Linolenic acid (ALA) significantly, but reversibly, inhibited growth at 1.8, 2.5, and 5 x 10(-4) M (p < 0.01), while concentrations of 10(-3) M killed virtually all organisms, with cell lysis observed by electron microscopy. Similar inhibitory effects were seen with other polyunsaturated fatty acids, at concentrations of 2.5 x 10(-4) M the relative inhibitory potencies were oleic (C18:1) < linoleic (C18:2) < arachidonic (C20:4) < omega-3 linolenic (C18:3) = omega-6 linolenic (C18:3) = eicosapentanoic (C20:5) acid. Cell fractionation studies with 14C labelled linolenic acid showed that the linolenic acid was associated with the membrane fraction. Commonly ingested dietary polyunsaturated fatty acids inhibit the growth of H pylori in vitro, an effect which deserves further in vivo study.

 

 

Proprietà Anti-infiammatorie dei Fitosteroli

 

Oltre alle ben note proprietà anticolesterolo, i fitosteroli sono ampiamente usati per le loro proprietà antinfiammatorie sia a livello dermatologico che gastro-intestinale. 

Si consiglia di leggere la seguente monografia: Plant Sterols and Sterolins Monograph

 

Seguono alcuni interessanti abstracts.

  

Curr Opin Clin Nutr Metab Care. 2001 Nov;4(6):471-5.
The role of phytosterols and phytosterolins in immune modulation: a review of the past 10 years.

Bouic PJ.

Faculty of Health Sciences, University of Stellenbosch, South Africa. pjdb@gerga.sun.ac.za

Although plant sterols (phytosterols) were chemically described in 1922, their biological role in human and animal health has been underestimated. Their ability to control cholesterol plasma levels in hypercholesterolimic patients was first described in 1983 when the structure of phytosterols implied that they could, by steric hindrance, inhibit the absorption of cholesterol from our diets. This has led to the development of functional foods containing high contents of these plant molecules or their esters as cholesterol controlling foods. Over the last 15 years, however, several reports have appeared in the literature indicating that phytosterols have some immunological activity as highlighted in animal models of inflammation or even in in-vitro and in-vivo models of cancer (colorectal and breast cancer). These findings were paralleled by epidemiological studies correlating the reduced risk of numerous diseases and the dietary intake of phytosterols. It is only in the last 10 years, however, that their direct immune modulatory activity on human lymphocytes has been proven and the mechanism of action in cancer cells has been elucidated. The use of phytosterols as supportive therapies in certain chronic conditions has been tested under clinical trial conditions. This review presents a summary of the in-vitro and in-vivo studies published to date.

 

  

 J Agric Food Chem. 2000 Jun;48(6):2313-9
Triterpene alcohol and sterol ferulates from rice bran and their anti-inflammatory effects.

Akihisa T, Yasukawa K, Yamaura M, Ukiya M, Kimura Y, Shimizu N, Arai K.

College of Science and Technology, Nihon University, Tokyo, Japan. akihisa@chem.cst.nihon-u.ac.jp

Six novel feruloyl esters of triterpene alcohols and sterols, viz., two trans-ferulates, cycloeucalenol and 24-methylenecholesterol trans-ferulates, and four cis-ferulates, cycloartenol, 24-methyelenecycloartanol, 24-methylcholesterol, and sitosterol cis-ferulates, besides five known trans-ferulates, cycloartenol (CAR), 24-methylenecycloartanol (24-MCA), 24-methylcholesterol, sitosterol, and stigmastanol trans-ferulates, and one known cis-ferulate, stigmastanol cis-ferulate, were isolated from the methanol extract of edible rice bran. These and eight other synthetic trans- and cis-ferulates of triterpene alcohols and sterols, along with the corresponding free alcohols, were evaluated with respect to their anti-inflammatory activity against 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation (1 microg per ear) in mice. All of the ferulates showed marked inhibitory activity, and their 50% inhibitory dose (ID(50)) was 0. 1-0.8 mg per ear. On the other hand, whereas two free triterpene alcohols, CAR and 24-MCA, showed strong inhibition (ID(50) 0.2-0.3 mg/ear), eight free sterols examined showed weaker activity (ID(50) 0.7-2.7 mg/ear) than their corresponding ferulates.

 


 

Int J Sports Med. 1999 May;20(4):258-62.
The effects of B-sitosterol (BSS) and B-sitosterol glucoside (BSSG) mixture on selected immune parameters of marathon runners: inhibition of post marathon immune suppression and inflammation.

Bouic PJ, Clark A, Lamprecht J, Freestone M, Pool EJ, Liebenberg RW, Kotze D, van Jaarsveld PP.

Dept. Medical Microbiology, Tygerberg, South Africa. pjdb@maties.sun.ac.za

A pilot study was undertaken to investigate the effects of the intake of capsules containing the plant sterols and sterolins (BSS:BSSG mixture) on selected immune parameters of volunteers participating in an ultra-marathon in Cape Town, South Africa. Those runners having received active capsules (n=9) showed less neutrophilia, lymphopenia and leukocytosis when compared to their counterparts having received placebo capsules (n=8): the placebo treated individuals showed significant increases in their total white blood cell numbers as well as in their neutrophils (p=0.03 and 0.03 respectively). Furthermore, statistically significant increases within lymphocyte subsets were observed in the runners having received the active capsules: CD3+ cells increased (p=0.02) as did CD4+ cells (p=0.03). In parallel, the BSS:BSSG capsules decreased the plasma level of IL6 in the runners using the active capsules (p=0.08) and significantly decreased the cortisol: DHEAs ratio (p=0.03), suggesting that these volunteers had less of an inflammatory response and were less immune suppressed during the post-marathon recovery period. These findings justify further investigations into the use of the phytosterols to prevent the subtle immunosuppression associated with excessive physical stress.

 

 

 

 

Phytother Res. 2002 Aug;16(5):417-21.
Bioactivity studies on beta-sitosterol and its glucoside.

Villasenor IM, Angelada J, Canlas AP, Echegoyen D.

Institute of Chemistry, University of the Philippines, Diliman, Quezon City 1101, Philippines.

Beta-sitosterol and beta-sitosteryl-beta-D-glucoside were isolated as analgesic constituents from the leaves of Mentha cordifolia Opiz. The acetic acid-induced writhing test showed that beta-sitosterol and beta-sitosteryl-beta-D-glucoside decreased the number of squirms induced by acetic acid by 70.0% and 73.0%, respectively, at a dose of 100 mg / kg mouse. Statistical analysis using the Kruskall Wallis one-way analysis of variance by ranks showed that these isolates approximate the analgesic activity of mefenamic acid at a 0.001 level of significance. The hot plate method confirmed their analgesic activities, as beta-sitosterol and beta-sitosteryl-beta-D-glucoside exhibited a 300% and 157% increase in pain tolerance, respectively, while mefenamic acid, a known analgesic, showed a 171% increase. Neither isolate exhibited antiinflammatory activity using the carrageenan-induced mouse paw oedema assay. Beta-sitosterol also exhibited anthelminthic and antimutagenic activities. In vitro tests using live Ascaris suum as test animals showed that the behaviour of worms treated with beta-sitosterol approximated that of the positive controls, Combantrin and Antiox. An in vivo micronucleus test showed that beta-sitosterol inhibited the mutagenicity of tetracycline by 65.3% at a dose of 0.5 mg /kg mouse. At the same dose, it did not exhibit chromosome-breaking activity.

 

 

J Ethnopharmacol. 2002 Mar;79(3):383-8. Click here to read 
Principles of root bark of Hippocratea excelsa (Hippocrataceae) with gastroprotective activity.

Navarrete A, Trejo-Miranda JL, Reyes-Trejo L.

Departamento de Farmacia, Facultad de Quimica, Universidad Nacional Autonoma de Mexico, Ciudad Universitaria, Coyoacan 04510, Mexico D.F., Mexico. anavarrt@servidor.unam.mx

The aqueous and ethanol extracts of the root bark of Hippocratea excelsa HBK. Locally known as 'Cancerina', showed an important gastroprotective effect in several experimental ulcer models in rats. Fractionation of the methanol extract led to four pools of active fractions (F1-F4). Sitosterol-3-O-beta-glucoside, beta-sitosterol and (-) epicatechin were isolated from the active fractions and showed an important gastroprotective activity (93.4,85.7 and 72.1% of gastroprotection, respectively), whereas bismuth subsalicylate, used as positive control, showed 46.2% of gastroprotection. A mixture of alpha-amyrin and beta-amyrin showed 50% of gastroprotection. Friedelin, canophyllal and canophyllol were isolated from the active fractions, but they were inactive as gastroprotective compounds. These results provide additional support for the popular use of this plant as an antiulcer remedy in the Mexican traditional medicine.

 

Biol Pharm Bull. 2001 May;24(5):470-3.
Anti-inflammatory and immunomodulating properties of a sterol fraction from Sideritis foetens Clem.

Navarro A, De las Heras B, Villar A.

Departamento de Farmacologia, Facultad de Farmacia, Universidad Complutense de Madrid, Spain.

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