Apocynin As a Potential Drug For

Neurodegenerative diseases

Presented by: Vandana Tyagi

(2023 PESF-104)
 01 Background

02 Mechanism of Action

CONTENTS 03 Pharmacological Action

04 Literature Review

05 Conclusion

06 References
2
 Background
01 • About Apocynin and its Properties.
• Neurodegenerative Diseases

3
 APOCYNIN
• Apocynin (4′-hydroxy-3′-methoxyacetophenone or
aceto vanillone) was identified as the biologically
active substance in the roots of Picrorhiza kurroa.

• Picrorhiza kurroa – also known as Kutki - Katki,

Katuka, Katuko, Katurohini, Katvi, Kuru.

• Native of Himalayan region.

• Ayurvedic medicine - use of root and rhizome.

• It is an selective inhibitor of NADPH Oxidase.

[1] Almeleebia, T. M., Alsayari, A., & Wahab, S. (2022). Pharmacological and Clinical Efficacy of Picrorhiza kurroa and Its Secondary Metabolites: A Comprehensive Review. Molecules, 27(23),
8316. MDPI AG. Retrieved from http://dx.doi.org/10.3390/molecules27238316 4
 Table1: Taxonomy Of Picrorhiza kurroa

Source Picrorhiza kurroa

Kingdom Plantae

Division Dicotiledonae

Class Asteride

Order Scrophulariales

Family scrophulariaceae

Genus Picrorhiza

Species Kurroa

[1] Masood, Maria, et al. "Picrorhiza kurroa: An ethnopharmacologically important plant species of Himalayan region." Pure and Applied Biology 4.3 (2015): 407. 5
5
 Table2: CHEMICAL CONSTITUENT OF PICRORHIZA
Picrorhiza species Plant part Class of compounds Chemical constituents
(Constituent structure)
Phenolic glycoside vanillic acid
Iridoid glycoside Kutkin
Roots
Phenolic glycoside Apocynin
picroside-II
kutkoside
Iridoid glycoside
picroside-III
picroside-I
P. kurroa
picrorhiza acid
picrorhizoside A
Aliphatic homocyclic
Seeds picrorhizoside B
picrorhizoside C
Shikimic acid
Gallic acid
Phenolic glycoside
isocorilagin
Isochebulic acid

[2] Petrônio, M. S., Zeraik, M. L., Fonseca, L. M., & Ximenes, V. F. (2013). Apocynin: chemical and biophysical properties of a NADPH oxidase inhibitor. Molecules
(Basel, Switzerland), 18(3), 2821–2839. https://doi.org/10.3390/molecules18032821 6
6
7
 NEURODEGNERATIVE DISEASES
• Neurodegenerative disorders are characterized by progressive and irreversible loss of neurons
from specific region of Brain.

• Many Neurodegnerative Diseases Such as:

✓ Alzheimer's disease.
✓ Amyotrophic lateral sclerosis.
✓ Friedreich ataxia.
✓ Huntington's disease.
✓ Lewy body disease.
✓ Parkinson's disease.
✓ Spinal muscular atrophy.

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 Mechanism of Action
02 • Mechanism of Action of NADPH Oxidase for
neurodegenerative disease
• Inhibition of Reactive Oxygen Species (ROS) by
Apocynin

9
 Mechanism of Action of NADPH Oxidase(NOX)
(NOX)
O2 O2.- ROS

gp 91 P22
phox phox

Rac
GTP P47 phox

P67
P40 phox phox P P P

NADPH NADP+

Activated
Resting
Figure 2: Mechanism of Action of NADPH Oxidase(NOX)

[3] t Hart, Bert A., Sjef Copray, and Ingrid Philippens. "Apocynin, a low molecular oral treatment for neurodegenerative disease." BioMed research international 2014 (2014). 10
 gp 91
phox P22
phox Reactive
oxygen
Species(ROS)
Neuronal cell
Rac
Apocynin damage and
GDP degeneration
P47 phox
P40 phox

P67
phox

Figure 3: Inhibition of NADPH Oxidase(NOX) by metabolically activated Apocynin

[4] Chen, Qian, et al. "Apocynin Exerts Dose-Dependent Cardioprotective Effects by Attenuating Reactive Oxygen Species in Ischemia/Reperfusion." Cardiovascular Pharmacology 5.2 (2016).
11
 Pharmacological Action
03

12
 Figure 4: Pharmacological action of Apocynin

[5] Stefanska, J., and R. Pawliczak. "Apocynin: molecular aptitudes." Mediators of inflammation 2008 (2008).
13
 LITERATURE REVIEW
04 • In vivo and in silico characterization of apocynin in reducing organ
oxidative stress: A pharmacokinetic and pharmacodynamic study.
• Novel NADPH Oxidase-2 Inhibitors as Potential Anti-Inflammatory
and Neuroprotective Agents.

14
[6]Liu, F., Fan, L. M., Michael, N., & Li, J. M. (2020). In vivo and in silico characterization of apocynin in reducing organ oxidative stress: A pharmacokinetic and pharmacodynamic
study. Pharmacology Research & Perspectives, 8(4), e00635.
15
[7] Juric, M., Rawat, V., Amaradhi, R., Zielonka, J., & Ganesh, T. (2023). Novel NADPH Oxidase-2 Inhibitors as Potential Anti-Inflammatory and Neuroprotective Agents. Antioxidants, 12(9),
1660. MDPI AG. Retrieved from http://dx.doi.org/10.3390/antiox12091660 16
 CONCLUSION
05

17
 CONCLUSION
• APOCYNIN- is a potential neuroprotective agent.
• Medicinal usage of Apocynin is limited
• Degradation of apocynin in GI tract before absorption.
• Low bioavailability and minimal absorption
• Vigorous biotransformation
• Rapid elimination
• Need – novel, stable and efficient formulation.
• Along with alternative drug delivery route for targeted delivery.

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 REFRENCES
06

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 Refrences:
1. Masood, Maria, et al. "Picrorhiza kurroa: An ethnopharmacologically important plant species of Himalayan
region." Pure and Applied Biology 4.3 (2015): 407.
2. Sah, Jit Narayan, and Vinay Kumar Varshney. "Chemical constituents of Picrorhiza genus." American Journal of
Essential Oils and Natural Products 1.2 (2013): 22-37.
3. Simonyi, Agnes, et al. "The neuroprotective effects of apocynin." Frontiers in bioscience (Elite edition) 4 (2012):
2183.
4. t Hart, Bert A., Sjef Copray, and Ingrid Philippens. "Apocynin, a low molecular oral treatment for
neurodegenerative disease." BioMed research international 2014 (2014).
5. Chen, Qian, et al. "Apocynin Exerts Dose-Dependent Cardioprotective Effects by Attenuating Reactive Oxygen
Species in Ischemia/Reperfusion." Cardiovascular Pharmacology 5.2 (2016).
6. Stefanska, J., and R. Pawliczak. "Apocynin: molecular aptitudes." Mediators of inflammation 2008 (2008).
7. Liu, F., Fan, L. M., Michael, N., & Li, J. M. (2020). In vivo and in silico characterization of apocynin in reducing organ
oxidative stress: A pharmacokinetic and pharmacodynamic study. Pharmacology Research & Perspectives, 8(4),
e00635.

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