Assessment of a Novel Bioflavonoids and Phytonutrient Formulation in Enhancing Cellular Aerobic Glycolysis, Immunity, Sports Performance, and Mitigating Inflammation

INTRODUCTION

An ideal sports nutrition formulation can be designed by applying a novel nutrition strategy to boost physical activity; tissue, blood, and cellular oxygenation and hydration; and facilitate the repair, regrowth, and rebuilding of damaged tissues for optimal functioning.^[1-3] Such a formulation should supplement fuel to the muscles and optimize athletic performance; boost endurance, vitality, and vigor; as well as promote overall health and wellness.^[1,4] The term “athlete” refers to a person who is proficient in sports and other forms of physical exercise; that is, an individual that engages in more intense exercise activities than a casual manner; including more extreme amateur and professional individuals.^[1,2,5] A great deal of differences exists in specific nutrient requirements for diverse athletes, restructuring and revitalizing the exciting challenge of individualizing sports nutrition plans. Thus, proper nutrition concepts and strategies are required by intertwining the understanding of physical training and dietary requirements, which are interdependent on each other, to produce optimal performance for diverse amateur and professional athletes in a wide range of sports or fitness endeavors.^[5-8] It is important to provide a solid nutritional foundation along with additional nutritional customization strategies specific for individual athletes participating in a particular sport, exercise, or physical activity. To keep up with the specific physical requirements of diverse sports, athletes need to fuel their bodies adequately on a regular basis. However, this fueling procedure, in conjunction with regular physical activities, requires a strategic and specialized approach, and accordingly, sports nutrition and exercise trainers are required to develop individualized plans based on the specific requirements of the athlete.^[5-8]

A human body requires six essential nutrients, namely, carbohydrates, proteins, fats, vitamins, minerals, and water to boost energy, contributing to the growth, repair, regulation, revitalizing and optimization of gene expression, cellular and tissue functions, metabolic homeostasis, and prevention of degenerative diseases.^[1,2,4] However, it is quite impossible to derive all the essential nutrients from diet alone. Macronutrients including carbohydrates, proteins, and fats have a caloric value, which are essential in larger quantities, while micronutrients including vitamins, antioxidants, and essential minerals are required in comparatively smaller amounts.^[1,2,4] To maintain metabolic homeostasis, carbohydrate, proteins, and fats release energy during metabolic events in the cellular system that breaks down the ingested foods into their molecular components, carbon dioxide, and water. However, part of this energy is conserved and utilized to produce adenosine triphosphate, the direct source of cellular energy; the remaining “unused” portions are “wasted” as heat.^[1,2,5-7] Major minerals including calcium, sodium, potassium, chloride, phosphorus, magnesium, and sulfur, and trace minerals such as iron, zinc, copper, selenium, iodine, fluoride, molybdenum, and manganese are required daily.^[1,8-10] However, water or cellular hydration, essential for cellular biochemical transactions, falls into its own unique category, and its requirements greatly vary among individuals. Several nutrients/supplements are available, which are well established to retain and maintain hydration status.^[1,9-11]

In athletes, hydration is important for temperature control, lubrication of joints and tissues, transportation of nutrients to different cellular sites, and providing an aqueous environment to facilitate biochemical reactions.^[10-12] In addition, appropriate oxygenation of tissues and organs is essential for normal biochemical and physiological functions.^[12,13]

Proper integration of all these elements is essential to promote optimal exercise performance and recovery after exercise. Dietary sources of bioflavonoids and antioxidants are even more important to strengthen connective tissues and assist in the reduction of oxidative stress, damage, and inflammatory sequelae.^[14-17]

Our earlier research studies emphasized the clinical efficacy of a patent pending VMP35 Multinutrient Complex (“Prodovite^®”), a bioflavonoid-based phytochemical formulation rich in structurally diverse bioflavonoids, polyphenols, stilbenes, nutritionally valuable saccharides (and phenolic glycosides), etc. [Table 1]. This iron-free liquid formulation is valuable for antioxidant protection, immune support, blood and tissue oxygenation, and hydration to boost sports performance, endurance, vitality, and vigor. A diverse range of water-extracted nano-emulsified VMP35 phytonutrient ingredients fortified with vitamins and minerals is encapsulated in a complex concentric configuration of proprietary SK713 SLP multi-lamellar phospholipid envelopes (Prodosomes^®) to yield a highly stable and rapidly bioavailable formulation. This patent pending iron-free formulation was shown to be absorbed and bioavailable within 5 min, rapidly restoring iron-dependent hemoglobin (Hb) (and its oxygen-carrying capabilities) and cellular hydration.^[18-21]

MANUFACTURING TECHNOLOGY: NOVEL VMP35 MNC FORMULATION

The Prodosome-fortified liquid nutraceutical formulation is manufactured by incorporating a novel proprietary SK713 SLP multi-lamellar clustoidal non-GMO phospholipid Prodosome nutrient absorption/delivery technology, which is biodegradable and biocompatible, in a multistep cGMP and NSF-certified manufacturing facility. The first step involves manufacturing the SK713 SLP, which was performed using a minimum of 85% non-GMO phosphatidylcholine, and subsequently impregnated and saturated the phospholipids with solar-dried electrolytes to ensure the enhanced availability of free ions, which will amplify the ionic properties of the multi-lamellar clustoidal phospholipid spheres, resulting in a net negative charge. The second step consists of thorough blending of a combination of research-affirmed botanicals containing structurally diverse natural polyphenolic antioxidants, multivitamins, micro- and macronutrients, and naturally occurring phytonutrients, utilizing an advanced wet milling technology to create a nano-emulsion. The final step consists of a combination of a specific blending sequence and an encapsulation technology to obtain the patent pending multi-lamellar energetically fortified clustoidal “Prodosomal” liposome-type encapsulated supplement (VMP35 Prodovite^®).^[18-22]

A randomized controlled one-way crossover clinical investigation

A randomized controlled one-way crossover study was performed in a total of 38 male and female subjects (male: 11 subjects; female: 27 subjects; age: 22–82 years) to assess the clinical efficacy of an iron-free VMP35 MNC (1 oz dose) on blood oxygenation and hydration in the treatment group as compared to the water-control subjects at baseline (0 min), 5 min, and 30 min post-treatment, respectively. An Institutional Review Board approval was obtained (Path Foundation in New York, NY [#13-009 April 25, 2013]) and all subjects signed an informed consent form. Adverse event monitoring was strictly enforced.

This study evaluated the absorption rate of the iron-free VMP35 and its effects by assessing the changes in peripheral blood smears from baseline (0 min), incorporating live blood cell imaging using phase contrast microscopy (Olympus BX-30 light microscope equipped with a phase contrast condenser [Tokyo, Japan] in conjunction with a 150 W lightbox and fiber-optic cable assembly) at 5 min post-control and post-VMP35 intake and 30 min post-VMP35 intake, respectively. It is important to indicate that the lens configuration was adjusted using a ×10 eyepiece and ×100 oil immersion objective magnification to approximate a ×1000. Specifically, the lighting generated a superior level of cell definition, brightness, and clearly showed the presence, morphology, and rheology of RBCs and neutrophils in the blood.

Significant efficacy of the iron-free VMP35 was observed on hemoglobinization, blood oxygenation, hydration, and neutrophil morphology at 5 and 30 min evaluations following VMP35 intake, respectively [Figures 1-3]. In fact, VMP35 instantly enhanced the morphological, hematological, and rheological properties of live human blood, which indicates that the iron-free VMP35 produced adequate nutritional benefits to restore intracellular iron-dependent RBC Hb within 5 min of intake, which was further sustained for an extended period. In addition, neutrophils demonstrated dramatic improvement in numbers and morphology. No adverse events were observed.

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Figure 1:

A representative baseline live blood cell imaging before consuming water.

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Figure 2:

A representative live blood cell imaging of the same subject 5 min after consuming water.

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Figure 3:

A representative live blood cell imaging of the same subject 30 min after VMP35 consumption.

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An additional athletic case study and two concept validation pilot studies have been conducted in a diverse population of well-trained athletes to assess and confirm the effects of the World Anti-Doping Association (“WADA”) compliant iron-free VMP35 on athletic performance.

ATHLETIC CASE STUDY IN A POWER LIFTER

This case study was undertaken by researchers and an extreme athlete (power lifter) to test the hypothesis that improving properties of the blood (i.e. oxygenation, hemoglobinization, hydration, energy enhancement, and immunity) could improve athletic performance. The athlete signed an affidavit regarding the results of the power lifting experiment. He has used a very extensive supplement regimen to support his intense power lifting workouts over the previous 12 months of serious strength training. His personal best in squat weightlifting was 395 lbs. He was attempting to achieve a new personal record of 405 lbs. Before supplementing with VMP35, to ensure his system was totally clean from any supplement influence, he did a 6-week washout and stopped taking the 20 other supplements his research indicated that he should be using up to that time.

Shortly before starting an intense powerlifting workout session, he took 1 ounce of iron-free liquid VMP35, swishing it in his mouth 30 s before swallowing. He also added 1 ounce of VMP35 to his regular workout beverage and sipped on it between his sets of squats, swishing it each time briefly before swallowing. He ended his first workout session by achieving a squat lift of 515 lbs! (Contrary to peer warnings, the following day he had no muscle pain). In the following 2 weeks, with continued use of the WADA compliant VMP35 as previously indicated, he continued to experience strength increases in squat training exercises ranging from 545 lbs to 575 lbs; a 180 lb increase over the 395 lb personal best at baseline.

A CONCEPT VALIDATION PILOT INVESTIGATION

To confirm the validity of the previous athletic case study, we conducted a 15-day concept validation pilot clinical investigation in three healthy young male high-level resistance-trained athletes (age: 32–36 years), on the effects of VMP35 on athletic performance. Duly signed informed consent forms were obtained from the study participants. Regulatory approvals were obtained, and adverse events were critically monitored. The daily dose was 1 ounce BID and swished in mouth for 30 s before swallowing. The first dose was about 20–30 min before engaging in a rigorous exercise regimen. The second dose was consumed in the afternoon. Over the course of the 15-day study, the most significant improvements were experienced within the first 2 days.

ATHLETIC CYCLISTS CASE STUDY

We also did a pilot study evaluating the effects of VMP35 in trained cyclists to confirm the beneficial effects across a range of athletic endeavors.

A 47-year-old male cyclist consumed 1 oz bid of VMP35 for 2 consecutive weeks. His power output (W) improved from 317 to 325.5 (a 2.7% increase), and his heart rate increased by only 1%.

In another 52-year-old male cyclist who consumed 1 oz bid of VMP35 for 2 consecutive weeks, power output (W) improved from 225 to 241.5 (7.3% increase), while the heart rate decreased by 0.3%, demonstrating increased cardiovascular strength and output.

In another 39-year-old male cyclist who consumed 1 oz bid of VMP35 for 2 consecutive weeks, his power output (W) improved from 262 to 286.5 (9.4% increase), while the heart rate increased by only 1.4%.

These effects of VMP35 supplementation in male cyclists are shown in Table 2.

Subjects reported that increased performance results also increased their enthusiasm levels significantly. No adverse events were reported by these well-trained athletic cyclists. It is evident that the power output (W) increased quite a bit, while the heart rate (beats per minute) increased only slightly in two of the subjects and decreased slightly in one subject that also experienced an increase in power output.

DISCUSSION

Both people with serious health problems and extreme athletes have in common a need for increased nutritional support to provide nourishment for greater than routine health maintenance. Food sources for the masses include those provided by conventional agribusiness practices (i.e. using chemical fertilizers, pesticides, herbicides, fungicides, growth enhancers, GMO, gassing, irradiation, coloring agents, etc.), food processing (including blanching, preservatives, flavor enhancers, functional food additives, food colorings, etc.), snack food products, and fast food outlets.^[24-26] Food stuffs from these sources are not only generally inadequate to meet the special and increased metabolic needs of these special populations but also are to some extent implicated as a cause of nutritional inadequacies and chemical/toxic insults underlying the shortfalls in both health and enhanced physical performance needs.^[27,28] Dietary supplementation is becoming increasingly commonplace to augment the dietary practices and meet nutrition requirements to achieve even the minimal functional competence of human biology.^[29-33] It is practically mandatory that people with injuries or chronic disorders and people who engage in more advanced and/or extreme athletic activities increase their nutritional resources through consuming various dietary supplements.^[29-31] The primary etiological factor underlying chronic degenerative diseases is the increase in anaerobic events and pathologies; that is, the inability to effectively use oxygen and water, and therefore nutrients, for cellular energy production, management, and waste removal.^[18-21] Anaerobic pathologies are the consequence of an overburdened pH buffering capability and generate a significant increase in reactive oxygen species (ROS). Given this, in addition to making healthier food choices, supplementation should include ingredients/products that restore aerobic metabolic events, minimizing free radical generation, and provide additional antioxidants to neutralize ROS as well.^[29,32,33]

CONCLUSION

Clinical research, case studies, and concept validation pilot studies have demonstrated that a WADA compliant iron-free liquid VMP35 dietary supplement supplies an abundant reservoir of pH buffers to restore aerobic metabolism by restoring iron-dependent Hb to RBCs, bolstering neutrophils, and improving performance output in a diverse range of extreme athletes. VMP35 provides a highly bioavailable source of vitamins, macro and trace minerals, ions, phospholipids, and botanicals containing a wide range of flavonoids, stilbenes, alkaloids, quinones, phytosaccharides, glycosides, sesquiterpenes, coumarins, polyacetylenes, and carotenoids. Overall, these data strengthen the antioxidant and physiological benefits of structurally diverse phytonutrients in VMP35 to achieve overall health maintenance for metabolic competence and athletic performance.