Scienca

Scienca is an epigenetic, anti-proliferative and anti-inflammatory compound, based upon the common spice turmeric/curcumin, long used in Indian cooking and by Ayurvedic practitioners. A secondary flavonoid quercetin is added to the formula to enhance its epigenetic effects. Bromelain, an enzyme from pineapple stems help insure sufficient assimilation.

Turmeric (from Curcuma Longa Root).  The curcuminoids in turmeric are polyphenols and are responsible for the yellow color of turmeric. Curcumin can exist in at least two tautomeric forms, keto and enol. The enol form is more energetically stable in the solid phase and in solution:

Quercetin (from Dimorphandra mollis Seed Pods).  Quercetin is a flavonoid and more specifically a flavanol. It is the aglycone form of a number of other flavonoid glycosides, such as rutin and quercetin found in citrus fruit. Quercetin is found to be the most active of the flavonoids in studies and many medicinal plants owe much of their activity to their high quercetin content. Quercetin has demonstrated significant anti- inflammatory activity because of direct inhibition of several initial processes of inflammation. It inhibits both the manufacture and release of histamine and other allergic/inflammatory mediators. In addition, it exerts potent antioxidant activity and vitamin C-sparing action.

Bromelain.  Bromelain's anti-inflammatory activity appears to be due to a variety of physiological actions. Evidence indicates that bromelain's action is in part a result of inhibiting the generation of bradykinin at the inflammatory site via depletion of the plasma kallikrein system, as well as limiting the formation of fibrin by reduction of clotting cascade intermediates. Bromelain has also been shown to stimulate the conversion of plasminogen to plasmin, resulting in increased fibrinolysis. (18) Bromelain was added to this formula to help with the absorption of quercetin and for its anti-inflammatory activity. Research from F.B. Giller from his 1962 study in the American Journal of Pharmacology indicated that bromelain affects the level of absorption in rabbits of a few different antibiotics including penicillin.

Turmeric (from Curcuma longa Root).  The applicable part of turmeric is the rhizome. Little curcumin, when eaten, is absorbed-- 2 grams of curcumin alone resulted in undetectable to very low serum levels. (11) However, the use of bromelain, an enzyme in pineapple stems, has traditionally be thought to increase absorption.

Turmeric’s major active constituents are curcuminoids including curcumin (diferuloylmethane).

It seems to have anti-inflammatory activity, possibly by inhibiting cyclooxygenase-2 (COX-2), prostaglandins, and leukotrienes. (1, 2, 3, 4) Turmeric also exhibits chemopreventive and growth inhibitory activity against several tumor cell lines. It seems to induce apoptosis in cancer cells and may inhibit angiogenesis. (4, 5, 6) Curcumin might have antithrombotic effects. Preliminary research suggests it might inhibit platelet-activating factor and arachidonic acid platelet aggregation, possibly by interfering with thromboxane synthesis. (7) Other preliminary research suggests that turmeric might also have antioxidant and immunostimulatory effects. (3, 8) It also seems to have activity against some bacteria, human immunodeficiency virus (HIV), and the protozoan Leishmania amazonensis. (2)

Curcumin acts as a free radical scavenger and antioxidant, inhibiting lipid peroxidation and oxidative DNA damage. Curcuminoids induce glutathione S-transferase and are potent inhibitors of cytochrome P450.

Curcumin is known for its antitumor, antioxidant, anti-amyloid and anti-inflammatory properties. Anti-inflammatory properties may be due to inhibition of eicosanoid biosynthesis. (9) A 2004 UCLA-Veterans Affairs study involving genetically altered mice suggests that curcumin might inhibit the accumulation of destructive beta-amyloid in the brains of Alzheimer’s disease patients and also break up existing plaques associated with the disease. (10)

Reactive oxygen species (ROS) play a key role in enhancing the inflammation through the activation of NF-kappaB and AP-1 transcription factors, and nuclear histone acetylation and deacetylation in various inflammatory diseases. Such undesired effects of oxidative stress have been found to be controlled by the antioxidant and/or anti-inflammatory effects of dietary polyphenols such as curcumin (diferuloylmethane, a principal component of turmeric) and resveratrol (a flavonoid found in red wine). The phenolic compounds in fruits, vegetables, tea and wine are mostly derivatives, and/or isomers of flavones, isoflavones, flavonols, catechins, tocopherols, and phenolic acids. Polyphenols modulate important cellular signaling processes such as cellular growth, differentiation and host of other cellular features.

Curcumin appears to have potent epigenetic effects in the body, modifying gene expression without producing changes in DNA sequence. Many such changes may be heritable. The primary mechanisms of epigenetics are histone acetylation (causing gene expression), histone deacetylation (causing gene silencing), histone methylation and DNA methylation (usually causing gene silencing).

Curcumin is a potent histone deacetylase inhibitor, blocking the expression of class I HDACs (HDAC1, HDAC3, and HDAC8). (13) Histone acetyltransferase (HAT) and histone deacetylase (HDAC) are the enzymes controlling the state of histone acetylation in vivo. Curcumin was able to effectively block histone hyperacetylation in both PC3-M prostate cancer cells and peripheral blood lymphocytes induced by the histone deacetylase inhibitor MS-275. Dietary polyphenols (curcumin-diferuloylmethane and resveratrol), the bronchodilator theophylline and glucocorticoids have all been shown to play a role in either controlling NF-kappaB activation or chromatin remodeling through modulation of HDAC activity and subsequently inflammatory gene expression. (14)

Curcumin seems to have protective effects against cell damage caused by some forms of chemotherapy. One study investigated the effect of curcumin on Adriamycin (ADR) nephrosis in rats. The results indicate that ADR-induced kidney injury was remarkably well prevented by treatment with curcumin. Treatment with curcumin markedly protected against ADR- induced proteinuria, albuminuria, hypoalbuminemia and hyperlipidemia. Curcumin restored renal function in ADR rats, as judged by the increase in GFR. The data also demonstrate that curcumin protects against ADR-induced renal injury by suppressing oxidative stress and increasing kidney glutathione content and glutathione peroxidase activity. This suggests that administration of curcumin is a promising approach in the treatment of nephrosis caused by ADR. (12)

Curcumin is a potent inhibitor of polyamine synthesis. Topical application of commercial grade curcumin, pure curcumin or desmethoxycurcumin had an equally potent inhibitory effect on 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced increases in ornithine decarboxylase activity and TPA-induced tumor promotion in 7,12-dimethylbenz[a]anthracene-initiated mouse skin. (16)

Quercetin.  Quercetin is a very strong antioxidant, capsable of reducing LDL oxidation.

It also possesses sirtuin-like deacetylase action. The silent information regulator 2 (Sir2) family of proteins (sirtuins or SIRTs), which belong to class III histone/protein deacetylases, have been implicated in calorie restriction, aging, and inflammation.

Like Curcumin, quercetin is an inhibitor of polyamine synthesis. (15)

Quercetin inhibits COMT (Catechol-O-MethylTransferase) enzyme thereby reducing epinephrine breakdown. This can lead to increased levels of epinephrine, potentially enhancing fat oxidation and energy expenditure.

Quercetin inhibits heat shock proteins that can promote apoptosis in cancer cells and other cells. Quercetin is also an inhibitor of aldose reductase. (17)

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18. North American Pharmcal TRM 2018 Bromelain.