| Reference | 1. Antioxidants (Basel). 2019 Nov 20;8(12):571. doi: 10.3390/antiox8120571.
<br>
Andrographolide, a Natural Antioxidant: An Update.
<br>
Mussard E(1), Cesaro A(1), Lespessailles E(1)(2)(3), Legrain B(4),
Berteina-Raboin S(5), Toumi H(1)(2)(3).
<br>
Author information:<br>
(1)Laboratory I3MTO, EA 4708, Université d’Orléans, 45067 Orléans Cedex 2,
France.<br>
(2)Service de Rhumatologie, Centre Hospitalier Régional d’Orléans 14 Avenue de
l’Hôpital, 45100 Orléans, France.<br>
(3)Plateforme Recherche Innovation Médicale Mutualisée d’Orléans, Centre
Hospitalier Régional d’Orléans CHRO, 41220 St Laurent Nouan, France.<br>
(4)NOVAXIA-6 Rue des champs Godin, 41220 St Laurent Nouan, France.<br>
(5)Institut de Chimie Organique et Analytique, Université d’Orléans-Pôle de
Chimie, UMR CNRS 7311, Rue de Chartres, 45067 Orléans, France.
<br>
Traditionally, Andrographis paniculata has been used as an herbal remedy for
lung infection treatments. Its leaves contain a diterpenoid labdane called
andrographolide responsible for a wide range of biological activities such as
antioxidant, anti-inflammatory, and anti-cancer properties. This manuscript is a
brief review of the antioxidant mechanisms and the regulation of the Nrf2
(nuclear factor (erythroid-derived 2)-like 2) signaling pathway by
andrographolide.
<br><br>
2. Biochem Pharmacol. 2017 Sep 1;139:71-81. doi: 10.1016/j.bcp.2017.03.024. Epub
2017 Apr 2.
<br>
Is there a future for andrographolide to be an anti-inflammatory drug?
Deciphering its major mechanisms of action.
<br>
Tan WSD(1), Liao W(1), Zhou S(1), Wong WSF(2).
<br>
Author information:<br>
(1)Department of Pharmacology, Yong Loo Lin School of Medicine, National
University Health System, 16 Medical Drive, Singapore 117600, Singapore.<br>
(2)Department of Pharmacology, Yong Loo Lin School of Medicine, National
University Health System, 16 Medical Drive, Singapore 117600, Singapore;
Immunology Program, Life Science Institute, National University of Singapore, 28
Medical Drive, Singapore 117456, Singapore. Electronic address:
[email protected].
<br>
Andrographis paniculata has long been part of the traditional herbal medicine
system in Asia and in Scandinavia. Andrographolide was isolated as a major
bioactive constituent of A. paniculata in 1951, and since 1984, andrographolide
and its analogs have been scrutinized with modern drug discovery approach for
anti-inflammatory properties. With this accumulated wealth of pre-clinical data,
it is imperative to review and consolidate different sources of information, to
decipher the major anti-inflammatory mechanisms of action in inflammatory
diseases, and to provide direction for future studies. Andrographolide and its
analogs have been shown to provide anti-inflammatory benefits in a variety of
inflammatory disease models. Among the diverse signaling pathways investigated,
inhibition of NF-κB activity is the prevailing anti-inflammatory mechanism
elicited by andrographolide. There is also increasing evidence supporting
endogenous antioxidant defense enhancement by andrographolide through Nrf2
activation. However, the exact pathway leading to NF-κB and Nrf2 activation by
andrographolide has yet to be elucidated. Validation and consensus on the major
mechanistic actions of andrographolide in different inflammatory conditions are
required before translating current findings into clinical settings. There are a
few clinical trials conducted using andrographolide in fixed combination
formulation which have shown anti-inflammatory benefits and good safety profile.
A concerted effort is definitely needed to identify potent andrographolide lead
compounds with improved pharmacokinetics and toxicological properties. Taken
together, andrographolide and its analogs have great potential to be the next
new class of anti-inflammatory agents, and more andrographolide molecules are
likely moving towards clinical study stage in the near future.
<br><br>
3. Int J Mol Sci. 2017 Jul 27;18(8):1638. doi: 10.3390/ijms18081638.
<br>
Multi-Targeting Andrographolide, a Novel NF-κB Inhibitor, as a Potential
Therapeutic Agent for Stroke.
<br>
Yang CH(1), Yen TL(2)(3), Hsu CY(4), Thomas PA(5), Sheu JR(6)(7), Jayakumar
T(8).
<br>
Author information:<br>
(1)Department of Pharmacology, Taipei Medical University, Taipei 110, Taiwan.
[email protected].<br>
(2)Department of Pharmacology, Taipei Medical University, Taipei 110, Taiwan.
[email protected].<br>
(3)Division of Cardiology, Department of Internal Medicine, Cathay General
Hospital, Taipei 200, Taiwan. [email protected].<br>
(4)Department of Life Science, College of Life Sciences, National Chung Hsing
University, Taichung 402, Taiwan. [email protected].
(5)Department of Ocular Microbiology, Institute of Ophthalmology, Joseph Eye
Hospital, Tiruchirappalli 620001, Tamil Nadu, India.
[email protected].<br>
(6)Department of Pharmacology, Taipei Medical University, Taipei 110, Taiwan.
[email protected].<br>
(7)Graduate Institute of Clinical Medicine, Taipei Medical University, Taipei
110, Taiwan. [email protected].<br>
(8)Department of Pharmacology, Taipei Medical University, Taipei 110, Taiwan.
[email protected].
<br>
A key focus in the field of drug discovery has been motivated by the
neuroprotection of natural compounds. Cerebral ischemia is a multifaceted
pathological process with a series of mechanisms, and a perspective for the
development of neuroprotectants from traditional herbal medicine or natural
products is a promising treatment for this disease. Natural compounds with the
effects of anti-oxidation, anti-inflammation, anti-apoptosis, and
neurofunctional regulation exhibit therapeutic effects on experimental ischemic
brain injury. Conferring to the pharmacological mechanisms underlying
neuroprotection, a study found that androgapholide, a diterpene lactone
compound, exhibits varying degrees of neuroprotective activities in both in
vitro and in vivo experimental models of stroke. The neuroprotective mechanisms
of andrographolide are suggested as: (I) increasing nuclear factor E2-related
factor 2-heme oxygenase (Nrf2-HO-1) expression through p38-mitogen activated
protein kinase (MAPK) regulation, (II) inducing cerebral endothelial cells (CEC)
apoptosis and caspase-3 activation, (III) down regulating Bax, inducible nitric
oxide synthase (iNOS), and (IV) inhibiting hydroxyl radical (OH-) formation, and
activating transcription factor NF-κB signaling pathways. Recently, several
researchers have also been trying to unveil the principal mechanisms involved in
the neuroprotective effects of andrographolide. Therefore, this review aims to
summarize an overview on the neuroprotective effects of andrographolide and
exemplifies the essential mechanisms involved. This paper can provide
information that andrographolide drug discovery may be a promising strategy for
the development of a novel class of neuroprotective drug.
<br><br>
4. Bioorg Chem. 2020 Jan;95:103511. doi: 10.1016/j.bioorg.2019.103511. Epub 2019
Dec 17.
<br>
Andrographolide: Chemical modification and its effect on biological activities.
<br>
Kumar G(1), Singh D(2), Tali JA(2), Dheer D(2), Shankar R(3).
<br>
Author information:<br>
(1)Bio-organic Chemistry Division, CSIR-Indian Institute of Integrative
Medicine, Jammu 180001, India.<br>
(2)Bio-organic Chemistry Division, CSIR-Indian Institute of Integrative
Medicine, Jammu 180001, India; Academy of Scientific and Innovative Research
(AcSIR), CSIR-IIIM, Jammu Campus, Jammu 180001, India.<br>
(3)Bio-organic Chemistry Division, CSIR-Indian Institute of Integrative
Medicine, Jammu 180001, India; Academy of Scientific and Innovative Research
(AcSIR), CSIR-IIIM, Jammu Campus, Jammu 180001, India. Electronic address:
[email protected].
<br>
The major natural bioactive constituent of Andrographis paniculata (AP) (Burm.
f.) Nees Andrographolide (1) and its derivatives are well acknowledged in
literature for its biological activities such as anti-cancer, anti-diabetic,
anti-inflammatory, anti-bacterial, anti-malarial, antihepatitis, anti-HIV,
anti-atherosclerosis, hepatoprotective, FXR antagonist, and α-glucosidase
inhibition. Many reports are available related to Andrographolide (1) but a
consolidated review on the chemical modification of andrographolide with special
emphasis on its different functional groups with respect to their biological
activities is still missing from the previous literature. Therefore, herein we
have collected a literature for the period 2009 onwards in relation to chemistry
on andrographolide (1) and its effect on respective biological activity. Also,
special attempt on increasing the bioavailability of andrographolide (1) has
been given for the designing of various targeted drug delivery systems.
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