Natural Products Insider

SEP-OCT 2018

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52 INSIDER September/October 2018 kinase that would allow for the production of these infl ammatory cytokines. 48 And another in vitro study demonstrated MSM to be a selective inhibitor of NLRP3 infl ammasome activation, a multiprotein complex operating as a platform for the infl ammatory response mediator IL-1β. 49 Boswellia serrata (frankincense) has been used anecdotally for millennia, but only in recent decades has its clinical potential been analyzed in Western trials. A systematic review noted collective "data seem to indicate that B. serrata extracts are effective in treating a range of conditions caused or maintained by infl ammatory processes," and that it's traditionally been used against infl ammatory diseases. 50 Additionally, "Its main pharmacologically active ingredients are α and β boswellic acid, as well as other pentacyclic triterpenic acids. These compounds have been shown to inhibit pro-infl ammatory processes by their effects on 5-lipooxygenase and cyclooxygenase and on the complement system [part of immune health]." The inhibitory effects of Boswellia serrata extract (as WokVel ® , from Verdure Sciences) on OA were investigated in an in vitro and in vivo rat study. 51 Of the botanical, the authors wrote, "Extract treatment signifi cantly reduced and normalized the productions of pro-infl ammatory factors, nuclear transcription factor kβ, cyclooxygenase-2, tumor necrosis factor-α, and interleukin-6 at a concentration of 20 μg/mL. Treatment of chondrocytes with [WokVel] extract signifi cantly reduced 5-lipoxygenase activity and production of prostaglandin E2, especially at a concentration of 10 to 20 μg/mL." The lignans magnolol and honokiol are phenolic compounds found in magnolia (Magnolia offi cinalis) bark extract. A study investigating the anti-infl ammatory effect of magnolol on pleurisy in mice found it reduced PGE2 and leukotriene B4 (LTB4) levels in the pleural fl uid. 52 The researchers concluded magnolol may be a dual COX and LOX inhibitor, whose effects are at least partly dependent on the reduction of the formation of eicosanoids mediators in the infl ammatory site. Magnolol also suppressed NF-kβ- mediated infl ammatory mediator synthesis in a rat model involving periodontitis—of which oral pathogen-driven infl ammation is a hallmark. 53 Another study looked at the potential role of honokiol in a collagen-induced arthritis model in mice. 54 Researchers summarized honokiol played a "prominent anti-infl ammatory role … potentially in both the cognitive phase of the immune response, as well as the effector phase, by inhibiting cytokines that lead to chronic infl ammation and additional pathology." Acacia gum (AG) is a prebiotic fi ber from the acacia tree. With impairment of gut wall functionality common in many infl ammatory diseases such as irritable bowel syndrome (IBS), one study examined the potential of AG (as Fibregum™, from Nexira) in aiding infl ammation and gut barrier issues. 55 Under LPS stimulation, experiments on pro-infl ammatory cytokines involving IBS patient donors indicated Fibregum completely inhibited NF-kβ/AP1 activity by the end of the treatment. For TNF-α the trend fl uctuated, and IL-8 secretion was mildly reduced. In a complementary way, the anti-infl ammatory cytokine IL-10 was increased by Fibregum. Regarding the pro-infl ammatory cytokines involving IBS patient donors, Fibregum produced the strongest decrease in NF-kβ/ AP-1 activity in the proximal and distal colon, where secretion of IL-8 and IL-6 was also reduced. IL-10 was increased in the distal colon. According to Julie Impérato, marketing manager at Nexira, the results demonstrated the anti-infl ammatory effect of Fibregum is based on two combined actions: inhibition of pro-infl ammatory cytokines and stimulation of anti- infl ammatory ones. Grape seed extract (GSE) has also been studied for its anti-infl ammatory effects. One study looked at the potential of GSE (as Meganatural Gold Extract, from Polyphenolics) in improving vascular risk markers (such as infl ammation) in high-risk cardiovascular subjects with type 2 diabetes. 56 Meganatural Gold Extract "signifi cantly improved markers of infl ammation" such as hsCRP over a four-week period. Scientists concluded GSE "may have a therapeutic role in decreasing cardiovascular risk." Vitamin E (as EVNol ® and EVNol SupraBio™ full-spectrum tocotrienol/ tocopherol complex extracted from virgin red palm oil [Elaeis guineensis], from ExcelVite Inc.) offers anti-infl ammatory properties. An in vitro study examined the effects of EVNol on artifi cially induced infl ammation in cell culture by measuring various infl ammatory mediators including NO, PGE2, COX-1, COX-2 and cytokines. 57 Cells were exposed to an infl ammatory agent (1µg/ml LPS) alone or with various concentrations of EVNol (0.5, 1.0 & 5.0µg/ ml) to study palm tocotrienol complex's ability to inhibit infl ammatory reactions. EVNol prevented infl ammation-induced cell death, exhibiting potent anti-infl ammatory properties as evidenced by a dose- dependent reduction of NO and PGE2 production. It also signifi cantly inhibited the production of pro-infl ammatory cytokines and displayed selective inhibition of COX-2 while sparing COX-1, which protects against gastric ulcer. In other studies, EVNol demonstrated immunoregulatory effects on LPS-induced infl ammatory responses of microglia by inhibiting NO production and reducing CD40 (a microglial co-stimulator molecule) expression of BV2 microglia. 58,59 Increased expression of CD40 on microglia is implicated in various types of neurodegenerative diseases including multiple sclerosis and Alzheimer's disease. The prebiotic dietary fi ber partially hydrolyzed guar gum (PHGG, as Sunfi ber ® , from Taiyo) decreased hsCRP signifi cantly in glucose-intolerant subjects after 12 months, revealing its potential to slow infl ammation during prolonged supplementation. 60 And a preclinical study showed improved outcomes of IBS and attenuation of pro-infl ammatory cytokine TNF-α when mice were fed Sunfi ber. 61 The anti-infl ammatory therapeutics market is projected to reach US$130.6 billion by 2026 with a compound annual growth rate (CAGR) of 8.5 percent from 2018 to 2026. 62 "At some point, virtually everyone will have infl ammation somewhere in the body, and will seek out a way to resolve it," Dockery said. With increasing numbers of individuals seeking out natural anti- infl ammatories—especially for long-term use—she concluded, "The potential is great for this area of the dietary supplement industry to grow." Inflammation For a list of references, email

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