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(12) Patent Application Publication (10) Pub. No.: US 2011/0274.679 A1 Pietrzkowski (43) Pub US 2011 O274.679A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2011/0274.679 A1 Pietrzkowski (43) Pub. Date: Nov. 10, 2011 (54) COMPOSITIONS AND METHODS OF SIRT Publication Classification ACTIVATION (51) Int. Cl. (75) Inventor: Zbigniew Pietrzkowski, Aliso A63/675 (2006.01) Viejo, CA (US) C07F 9/58 (2006.01) s A6IP 43/00 (2006.01) (73) Assignee: VDF FutureGeuticals, Inc., C07D 475/4 (2006.01) Momence, IL (US) A6II 3/525 (2006.01) s CI2N 5/00 (2006.01) A6II 3/74 (2006.01) (21)21) Appl. NoNo.: 13/127,7969 C7H 23/00 (2006.01) (22) PCT Filed: Nov. 5, 2009 (52) U.S. Cl. .............. 424/94.1: 514/89: 514/52:546/24: 536/26.4:544/251; 514/251; 435/375 (86). PCT No.: PCT/USO9/63358 (57) ABSTRACT .."St. L. 25, 2011 Compositions and methods of SIRT activation are presented s e a? a 9 in which one or more vitamin compounds, and especially O O Vitamin B compounds are used to significantly increase SIRT Related U.S. Application Data activity in vitro and in vivo. In especially preferred composi (60) Provisional application No. 61/111.538, filed on Nov. tions, vitamin B6, vitamin B12, and vitamin B2 are present in 5, 2008. synergistic quantities. Patent Application Publication Nov. 10, 2011 Sheet 1 of 2 US 2011/0274.679 A1 Figure 1 Figure 2 Patent Application Publication Nov. 10, 2011 Sheet 2 of 2 US 2011/0274.679 A1 E 2 hrs & 4 hrs 700mg 2100mg US 2011/0274.679 A1 Nov. 10, 2011 COMPOSITIONS AND METHODS OF SIRT increased by administration of one or more vitamins, and ACTIVATION especially by oral administration of vitamin B compounds, where such administration uses dosages that are ordinarily taken as dietary Supplements. 0001. This application claims priority to our copending 0008 Consequently, a method of providing a composition U.S. provisional patent application with the Ser. No. 61/111. that increases SIRT activity in a mammal is contemplated that 538 filed Nov. 5, 2008 which is incorporated by reference has a step in which a composition is formulated that includes herein in its entirety. at least one vitamin, and particularly a vitamin B compound FIELD OF THE INVENTION in an amount effective to increase SIRT activity in the mam mal. In another step, a test result is obtained that indicates that 0002. The field of the invention is activation of SIRT, the vitamin B compound increases SIRT activity in the mam especially as it relates to activation of SIRT using nutritional mal, in yet another step, the composition is provided to the Supplements, and vitamins in particular. mammal in association with the test result. In especially preferred aspects, the vitamin B compound is vitamin B. BACKGROUND OF THE INVENTION Vitamin B, and/or vitamin B, more preferably vitamin Be 0003 Sirtuins are ubiquitously found in animals, plants, and vitamin B, and most preferably vitamin B vitamin and various microorganisms, and are thought to play a key B, and vitamin B. Additionally, it is contemplated that the role in an organism's response to various stress signals. On a vitamin B vitamin B, and vitamin B are present in a molecular level, Sirtuins can be characterized as protein (and synergistic amount. Where desired, the composition may fur especially histone) deacetylases that use NAD" as cofactor ther comprise vitamin B, Vitamin Bs, and/or vitamin B. (EC number 3.5.1). Remarkably, increased SIRT activity has Optionally, contemplated compositions will further include a been associated in experimental systems with lifespan-ex flavone, a stilbene, a flavanone, and/or an anthocyanidin. tending effects of calorie restriction, improved glucose/lipid 0009. It is further generally preferred that vitamin B is metabolism, and increased PON1 (Paraoxonase 1) activity, present in an amount of between 60 and 600 mg, vitamin B which is known as the major anti-atherosclerotic component is present in an amount of between 30 and 300 mcg, and that of high-density lipoprotein. vitamin B is present in an amount of between 30 and 300 mg. 0004. Not surprisingly, SIRT activation has become an Where additional vitamin B compounds are present, it is attractive target for pharmaceutical and nutraceutical compa preferred that vitamin B is present in an amount of between nies, and numerous platforms to identify SIRT activators have 30 and 300 mg, vitamin Bs is present in an amount of between been reported as can be taken from WO 06/081329, U.S. Pat. 30 and 300 mg, and that vitamin B is present in an amount of App. No. 2008/0021063, or U.S. Pat. No. 7,273,713. While between 3 and 30 mg. Such methods are at least conceptually promising, various 0010 Most preferably, vitamin B is present in an amount difficulties still remain. Most significantly, compounds iden of about 220 mg. the vitamin B is present in an amount of tified using Such methods will typically require a full inves about 90mcg, vitamin B is present in an amount of about 100 tigation into their pharmacologic, pharmacodynamic, and/or mg, Vitamin B is present in an amount of about 100 mg. toxicologic profile prior to marketing. vitamin Bs is present in an amount of about 100 mg, and that 0005 To avoid disadvantages associated with new drug Vitamin Bo is present in an amount of about 15 mg. entities, certain naturally occurring compounds have been 0011. It is still further contemplated that test result is a test considered suitable for SIRT activation as they have been result obtained from a human test subject, and/or that the reported to stimulate SIRT. Among other compounds, various increase SIRT activity is at least 10%, more typically at least flavones, stilbenes, catechins, flavanones, and anthocyani 50%, and most typically at least 80% over untreated control. dins, were described in U.S. Pat. App. No. 2006/0084135 as SIRT activators. Similarly, resveratrol was demonstrated to 0012. Therefore, a method of increasing SIRT activity in a activate Sir2 in Saccharomyces cerevisiae (see e.g., Nature mammal is contemplated in which to a mammal is adminis 2004; 430(7000): 686-689.), and implications for treatment tered a synergistic combination of vitamin B compounds in an of various conditions in human and ageing were described amount effective to increase SIRT activity in the mammal. elsewhere (see e.g., Clin Intery Aging. 2008; 3(2):331-9). Preferably, the synergistic combination of vitamin B com While resveratrol and related natural compounds are gener pounds comprises vitamin B vitamin B, and vitamin B. ally regarded as safe and readily available from various natu and may further include vitamin B, Vitamin Bs, and/or Vita ral materials, significant quantities are typically required to min B. elicit a measurable effect in vitro. Moreover, resveratrol has I0013. In particularly contemplated methods, vitamin B is relatively poor solubility in water and bioavailability is thus present in an amount of between 60 and 600 mg, vitamin B severely restricted, typically producing serum concentrations is present in an amount of between 30 and 300 mcg, and of resveratrol that are insufficient for significant biological vitamin B is present in an amount of between 30 and 300 mg. effects in vivo. and where added, vitamin B is present in an amount of 0006 Thus, there is still a need to improved compositions between 30 and 300 mg. vitamin Bs is present in an amount of and methods of SIRT activation in mammals, and especially between 30 and 300 mg, and/or vitamin B is present in an with pharmaceutically or nutritionally acceptable composi amount of between 3 and 30 mg. Most preferably, vitamin B tions. is present in an amount of about 220 mg, Vitamin B is present in an amount of about 90mcg, Vitamin B is present in SUMMARY OF THE INVENTION an amount of about 100 mg, vitamin B is present in an amount of about 100 mg, Vitamin Bs is present in an amount 0007. The inventor has discovered that SIRT activity in a of about 100 mg, and vitamin Bo is present in an amount of mammal, and especially in human can be significantly about 15 mg. US 2011/0274.679 A1 Nov. 10, 2011 0014 Preferably, the vitamin blend comprises a vitamin Silent mating type Information Regulation-2 protein). As also B compound and a vitamin B, and most preferably a vita used herein, the terms “SIRT activation' or “increases SIRT min B compound, a vitamin B, and a vitamin B com activity” mean that the overall observable catalytic activity of pound, typically at a concentration that induces SIRT activity SIRT is increased, which may be caused by various factors, at least 50%, and most typically at least 100% over an including increased transcription, increased translation, and/ untreated control using an experimental system as described or increased catalytic activity (increased specific activity). below. In still further contemplated formulations, the blend 0022 Based on the inventor's observations and experi further comprises a vitamin B compound, a vitamin B com mental data (infra), the inventor thus contemplates a method pound, a pantothenate compound, and/or a folate compound. of providing a composition that increases SIRT activity in a Consequently, all methods are contemplated in which a con mammal in which in one step a composition is formulated that Sumer (wholesale and/or retail) is advised that the composi has at least one vitamin B compound in an amount effective to tions according to the inventive subject matter are effective to increase SIRT activity in the mammal. In another step, a test increase SIRT activity in a mammal when administered to the result is obtained that indicates that the vitamin B compound mammal.
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