Hamdan Medical Journal

LETTER TO EDITOR
Year
: 2019  |  Volume : 12  |  Issue : 4  |  Page : 242--243

Comparative pharmacokinetics of synthetic and natural pterostilbene


Roopesh Jain 
 Laurus Labs Limited, Hyderabad, Telangana, India

Correspondence Address:
Roopesh Jain
Laurus Labs Limited, Serene Chambers, Road #7, Banjara Hills, Hyderabad - 500 034, Telangana
India




How to cite this article:
Jain R. Comparative pharmacokinetics of synthetic and natural pterostilbene.Hamdan Med J 2019;12:242-243


How to cite this URL:
Jain R. Comparative pharmacokinetics of synthetic and natural pterostilbene. Hamdan Med J [serial online] 2019 [cited 2020 Jan 18 ];12:242-243
Available from: http://www.hamdanjournal.org/text.asp?2019/12/4/242/270669


Full Text



Sir,

Pterostilbene is a methylated stilbene molecule and has structural similarity with resveratrol (two hydroxyl groups of resveratrol are replaced with methoxy groups). In other words pterostilbene is a dimethylated derivative of resveratrol and reported more potent in some biological activates.[1] It is also found to be better absorbed and generally known as a 'better resveratrol'. Pterostilbene has been noted to reduce anxiety, blood glucose, blood pressure (diastolic and systolic) in hypercholesterolemic adults, inflammation and serum triglycerides.[2] It was also reported to reduce low-density lipoprotein cholesterol (57%) and improve in high-density lipoprotein cholesterol (73.1%) in diabetic rats.[3] Its effect on longevity and life extension, memory and learning, different solid tumors and antioxidant activity is well learnt.[4],[5]

Pterocarpus marsupium (Malabar Kino Tree or Indian Kino Tree) is a well-known commercial source of pterostilbene but it is listed as a vulnerable plant in the IUCN red data list therefore many companies such as Laurus Labs Limited has opted synthetic route of manufacturing which also gives highest purity >99% and is equivalent to API quality. This controlled process avoids batch to batch variation therefore suitable for standardized formulations. Laurus Labs Limited also conducted pharmacokinetics study at National Accreditation Board for Testing and Calibration Laboratories (NABL) accredited premier preclinical research facility in India. The objective of this study was to assess the comparative pharmacokinetic of different forms of pterostilbene (synthetic and natural) in Sprague–Dawley rats at dose of 15 mg/kg by oral administration.

In this study rats were administered orally with test formulation – high pure (99% by high-performance liquid chromatography) synthetic pterostilbene manufactured by Laurus Labs Limited, and natural pterostilbene (Pterocarpus extract) as a single dose in a dose volume of 10 mL/kg through gavage. Approximately, 250–300 μL of blood sample was collected from each rat at predose and at 0.25, 0.5, 1.0, 2.0, 4.0, 6.0, 8.0, 12.0, and 24.0 h postdose via retro-orbital plexus in prelabelled K2 EDTA coated micro centrifuge tubes. The blood samples were centrifuged and separated plasma samples were assessed for the levels of pterostilbene by LC-MS/MS method. Mean plasma concentration versus time profile was used to calculate pharmacokinetic parameters by using noncompartmental analysis tool WinNonlin®Software V 6.2.1 (Pharsight Corporation, a Certara™ company). The protocol was approved by the Institutional Animal Ethics Committee of expiring lab vide Protocol No. PCD/Pharmacokinetic/01 (Version 2) and all the ethical practices as laid down in the CPCSEA guidelines for animal care were followed during the conduct of the study.

In female rats, peak plasma concentration (Cmax) and the extent of absorption (AUC0-24) of synthetic pterostilbene were reported higher by 107% and 92% respectably when compared with natural extract. Results clearly indicated better pharmacokinetics profile of pterostilbene manufactured by synthesis than natural extract. Laurus Labs Limited also tested thermodynamic stability of both forms of pterostilbene and found synthetic more thermodynamically stable than natural. High purity seems to be reason of the better thermodynamic stability of synthetic pterostilbene. A clinical study published in 'Journal of Toxicology' has established safety of synthetic pterostilbene for use in humans up to 250 mg/day.[6] Other than P. marsupium, pterostilbene is reported in low quantities in a few plants such blueberries and grapes which otherwise may be used as a food product in a sustainable manner therefore manufacturing through synthetic route gives an alternative.

Financial support and sponsorship

Nil.

Conflicts of interest

There are no conflicts of interest.

References

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2McCormack D, McFadden D. A review of pterostilbene antioxidant activity and disease modification. Oxid Med Cell Longev 2013;2013:575482.
3Pari L, Satheesh MA. Effect of pterostilbene on hepatic key enzymes of glucose metabolism in streptozotocin-and nicotinamide-induced diabetic rats. Life Sci 2006;79:641-5.
4Li YR, Li S, Lin CC. Effect of resveratrol and pterostilbene on aging and longevity. Biofactors 2018;44:69-82.
5Zhang X, Zhang J, Xu L, Ma Z, Di S, Gao Y, et al. Emerging actions of pterostilebene on cancer research. Zhongguo Fei Ai Za Zhi 2018;21:931-6.
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