Pharmazie. 2011 Aug;66(8):628-30.
Growth inhibiting activity of lipophilic extracts from Dipsacus sylvestris Huds. roots against Borrelia burgdorferi s. s. in vitro.
Liebold T1, Straubinger RK, Rauwald HW.
Author information
Abstract
Fresh first year roots from Dipsacus sylvestris HUDS. were extracted with 70% ethanol, ethyl acetate as well as dichloromethane. Extracts were solubilized in water (lipophilic extracts with addition of polysorbate 80) and tested for their activity against Borrelia burgdorferi sensu stricto in vitro during an eight-day period using amoxicillin as standard. The hydroethanolic extract showed no growth inhibition whereas significant growth inhibiting activity could be shown in the two less polar fractions for the first time. Strongest inhibition was found in the ethyl acetate extract. The effect of polysorbate 80 on bacterial growth was examined and found to be negligible. As the nature of bioactive constituents has not been clarified yet, a micellar electrokinetic capillary chromatography fingerprint analysis for a methanolic extract was applied including loganin, chlorogenic acid, cantleyoside and caffeic acid as marker substances.
As for your question...
J Nutr Biochem. 2013 Jul;24(7):1276-84. doi: 10.1016/j.jnutbio.2012.10.003. Epub 2013 Jan 17.
Citrus flavonoid naringenin inhibits TLR2 expression in adipocytes.
Yoshida H1, Watanabe W, Oomagari H, Tsuruta E, Shida M, Kurokawa M.
Abstract
Toll-like receptors (TLRs) were recently shown to be involved in obesity-induced inflammation in adipose tissue, which contributes to the development of insulin resistance and type 2 diabetes. Thus, the appropriate regulation of TLR expression or activation is an important strategy for improving obesity-related diseases. In this report, we show that naringenin, a citrus flavonoid, inhibits TLR2 expression during adipocyte differentiation. This effect is mediated in part through peroxisome proliferator-activated receptor γ activation. In addition, naringenin suppresses TLR2 expression induced by the co-culture of differentiated adipocytes and macrophages and also inhibits tumor necrosis factor-α (TNF-α)-induced TLR2 expression by inhibiting the activation of nuclear factor-κB and c-Jun NH2-terminal kinase pathways in differentiated adipocytes. Furthermore, naringenin decreases TLR2 expression in adipose tissue of high-fat diet-fed mice. These results are correlated with the improvement of hyperglycemia and the suppression of inflammatory mediators, including TNF-α and monocyte chemotactic protein-1. Taken together, these data suggest that naringenin exhibits anti-inflammatory properties, presumably by inhibiting TLR2 expression in adipocytes. Our findings suggest a molecular mechanism by which naringenin exerts beneficial effects against obesity-related diseases.
Inflammation. 2011 Oct;34(5):463-70. doi: 10.1007/s10753-010-9254-8.
Baicalin inhibits TLR2/4 signaling pathway in rat brain following permanent cerebral ischemia.
Tu XK1, Yang WZ, Shi SS, Chen Y, Wang CH, Chen CM, Chen Z.
Abstract
Recent work from our laboratory demonstrated that baicalin attenuates inflammatory reaction and cerebral ischemia injury in rats. Toll-like receptor 2 and 4 (TLR2/4) and the downstream nuclear factor-kappa B (NF-κB) signaling pathway, which mediate the inflammatory reaction, are involved in the pathophysiological processes of cerebral ischemia. In this study, we investigated whether baicalin inhibits TLR2/4 signaling pathway in a rat model of permanent focal cerebral ischemia. Adult Sprague-Dawley rats underwent permanent middle cerebral artery occlusion (MCAO). Baicalin was administered by intraperitoneally injected twice at 2 and 12 h after the onset of ischemia. Cerebral infarct area and infarct volume were measured 24 h after MCAO. Expression of TLR2/4, NF-κB, inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) were determined by RT-PCR or western blot. NO and PGE2 production in rat brain were measured 24 h after MCAO. Serum content of tumor necrosis factor-alpha (TNF-α) and interleukin-1β (IL-1β) were detected by ELISA. Baicalin reduced cerebral infarct area and infarct volume. Baicalin reduced the expression of TLR2/4 and NF-κB, decreased the expression and activity of iNOS and COX-2 in rat brain. Baicalin also attenuated the serum content of TNF-α and IL-1β. Our results suggest that baicalin inhibits the TLR2/4 signaling pathway in cerebral ischemia, which may be a mechanism underlying the baicalin's neuroprotection.
J Immunol Res. 2014;2014:740549. doi: 10.1155/2014/740549. Epub 2014 Jul 23.
Glycyrrhizin attenuates Toll like receptor-2, -4 and experimental vasospasm in a rat model.
Chang CZ1, Wu SC2, Kwan AL3.
Abstract
Upregulated TLRs are observed in the serum of animals following experimental subarachnoid hemorrhage. This study was to examine glycyrrhizin's effect on proinflammatory cytokines and TLRs in SAH rats. Administration with glycyrrhizin was initiated 24 hr before and 1 hr later using osmotic minipump. Basilar arteries were harvested to examine TLRs mRNA and protein (rt-PCR and western blot) and CSF cytokines (rt-PCR). Morphologically, deformed endothelium, tortuous elastic lamina, and smooth muscle necrosis were observed in the SAH rats, but were absent in the glycyrrhizin pretreatment group. The TLR-3 protein level was not increased in SAH animals, compared with the controls, while that of TLR-2 and -4 in the SAH only and SAH plus vehicle groups was significantly elevated (P < 0.01). Pretreatment and treatment with glycyrrhizin reduced TLR-2 and -4 by 28 ± 8% and 33.4 ± 9.2%, respectively. Likewise, glycyrrhizin was able to reduce the IL-1β and MCP-1 mRNA levels. This study shows glycyrrhizin exerts anti-inflammatory effects on SAH induced vasospasm and attenuates the ultrashort time expression of TLRs, like TLR-2 and -4. It corresponds to SAH induced early brain injury. These findings offer credit to the antivasospastic effect of glycyrrhizin and its effect on SAH induced early brain injury.
Thank you so much! I am taking heparin via picc line for Babesiosis, seems to also affect Burgdorferi spirochete, at least by making them more susceptible to antibiotics, plus it seems to help bring down inflammation but only for a few hours.
And dipsacus sylvestris is just a synonym for dipsacus fullonum or Teasal Root, which I believe can be found on amazon as extracts in tincture form. Not sure if they are equiolent to the extract used in the study you linked.
Highest inhibition was found in the ethyl acetate fraction (99.7± 1.0% on day 4). In this fraction all visible forms of Bbss were immobile within the first day, their number did not increase within eight days.
So ethyl acetate extract of Teasal Root would be the best bet at inhibiting growth of spirochetes in vitro, not sure in vivo but regardless patients have had good results with it.
What I find very interesting is that Baicalin from what I know as a chemical found in Skullcap is an inhibitor of TLR2 and so isn't Naringenin from grape fruits, both have significant killing ability in vitro against all forms of Lyme, including cystic forms! Actually, so far Baicalin is the strongest herbal plant extract that has high affinity on all forms of B. Burgdorferi and garnii. Just a matter of administration and if it works in vivo. Hesperidin is found in plasma and tissue after ingestion so that's a plus.
Curcumin inhibits TLR2/4-NF-κB signaling pathway and attenuates brain damage, I've also read some studies that it works synergistically with antibiotics.
This study looks at various antibiotic combos against spirochetes, biofilms, etc. Right now, I have at home rifampin, Hydroxychlorquine, Doxycycline, and a PICC line administering Rocephin, which is in the same class as cefoporazone. They didn't combine Daptomycin with Rocephin and Doxy but in the chart two combo administration of Rocephin with Daptomycin had a significant reduction in live cell percentage equivalent to that of a cefoporazone, daptomycin combo.
I say this because cefoporazone is discontinued and I wouldn't know where to get it. I'm not sure of the side effects of daptomycin but it sure seems to be the best bet when combined with an inter-cellular like doxy and a cell wall inhibitor like Rocephin or cefoporazone.
Edited by birthdaysuit, 14 October 2016 - 08:44 AM.