4.7 Review

Andrographolide, a natural anti-inflammatory agent: An Update

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Review Chemistry, Medicinal

Andrographolide: A review of its pharmacology, pharmacokinetics, toxicity and clinical trials and pharmaceutical researches

Bin Zeng et al.

Summary: Andrographis paniculata, known as "Chuan Xin Lian" in China, is a widely used herb in traditional Chinese medicine for various ailments. Its main active compound, andrographolide, has multiple therapeutic actions, but there is a lack of systematic summaries on its specific mechanisms, safety issues, and clinical transformation bottlenecks. Further research is needed to fully understand its efficacy and safety.

PHYTOTHERAPY RESEARCH (2022)

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Andrographolide suppresses osteoarthritis progression by regulating circ_Rapgef1/miR-383-3p/NLRP3 signaling axis

Wei Yan et al.

Summary: This study revealed that circ_Rapgef1 suppressed the protective effects of AD in osteoarthritis by regulating the miR-383-3p/NLRP3 signaling pathway.

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Andrographolide as a potential inhibitor of SARS-CoV-2 main protease: an in silico approach

Sukanth Kumar Enmozhi et al.

Summary: The SARS-CoV-2 virus has caused a global pandemic with over 1.2 million confirmed cases and nearly 65,000 deaths, leading to a search for effective treatments. Clinical trials are being conducted on antiviral drugs, but the lack of approved treatments highlights the need for novel compounds. Andrographolide from Andrographis paniculata shows promise as an inhibitor for SARS-CoV-2 main protease, with in silico studies suggesting good solubility, pharmacodynamics properties, and target accuracy.

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Andrographolide suppresses NLRP3 inflammasome activation in microglia through induction of parkin-mediated mitophagy in in-vitro and in-vivo models of Parkinson disease

Sahabuddin Ahmed et al.

Summary: The communication between microglia activation and dopaminergic neuronal loss plays an important role in the progression of Parkinson's disease. Studying the NLRP3 inflammasome activation and its relation to mitochondrial dysfunction in microglia could provide insights into potential strategies to control neurodegeneration. Mitophagy regulation through Andrographolide treatment may help inhibit NLRP3 activation and rescue dopaminergic neuron loss.

BRAIN BEHAVIOR AND IMMUNITY (2021)

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Synthesis, extracorporeal nephrotoxicity, and 3D-QSAR of andrographolide derivatives

Lili Gu et al.

Summary: The study found that modification of andrographolide structure can reduce its nephrotoxicity, with compounds III, V, and IX(c) showing lower nephrotoxicity. Additionally, the established 3D-QSAR model proposed five new compounds with lower theoretical nephrotoxicity, which could be further studied for synthesis and evaluation.

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Andrographolide attenuates inflammatory response induced by LPS via activating Nrf2 signaling pathway in bovine endometrial epithelial cells

Kaiqiang Fu et al.

Summary: Andrographolide exhibits significant anti-inflammatory effects in the LPS-induced inflammatory response of bEECs by reducing the production of inflammatory factors through the activation of Nrf2.

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Andrographolide inhibits IL-1β release in bone marrow-derived macrophages and monocyte infiltration in mouse knee joints induced by monosodium urate

Chia-Wen Lo et al.

Summary: The study aimed to investigate the effects of Andrographolide (AND) on gout-induced joint inflammation. The results demonstrated that AND attenuated MSU-induced joint inflammation by inducing HO-1 expression and inhibiting ROS-mediated NLRP3 inflammasome assembly and subsequent IL-1 beta release.

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Contraceptive potential of Andrographis paniculata is via androgen suppression and not induction of oxidative stress in male Wistar rats

A. F. Ogundola et al.

Summary: Andrographis paniculata may induce reproductive toxicity by suppressing testosterone rather than inducing oxidative stress, suggesting its potential as a male contraceptive.

TISSUE & CELL (2021)

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Anti-SARS-CoV-2 Activity of Andrographis paniculata Extract and Its Major Component Andrographolide in Human Lung Epithelial Cells and Cytotoxicity Evaluation in Major Organ Cell Representatives

Khanit Sa-ngiamsuntorn et al.

Summary: This study investigated the anti-SARS-CoV-2 activity of Andrographis paniculata extract and andrographolide in human lung epithelial cells, showing that they significantly inhibited the production of infectious virions with low cytotoxicity. These findings suggest that A. paniculata and andrographolide have potential as monotherapy or in combination with other drugs against SARS-CoV-2 infection.

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Inhibition of Inducible Nitric Oxide Synthase (iNOS) by Andrographolide and In Vitro Evaluation of Its Antiproliferative and Proapoptotic Effects on Cervical Cancer

Akbar Pasha et al.

Summary: This study aimed to investigate the expression of inducible nitric oxide synthase (iNOS) in cervical cancer and identified a potential iNOS inhibitor. The research found that elevated iNOS levels were associated with poor survival and increased tumor aggressiveness in cervical cancer, and andrographolide may exert anti-cancer effects by inhibiting iNOS expression.

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Efficacy and safety of Xiyanping injection in the treatment of COVID-19: A multicenter, prospective, open-label and randomized controlled trial

Xin-Yi Zhang et al.

Summary: XYP injection showed promising results in reducing symptom duration and virus clearance time in patients with mild to moderate COVID-19, with lower risk of disease progression to severe stage. Further studies are needed to evaluate its efficacy in a larger cohort of COVID-19 patients.

PHYTOTHERAPY RESEARCH (2021)

Article Integrative & Complementary Medicine

Andrographolide Inhibition of Th17-Regulated Cytokines and JAK1/STAT3 Signaling in OVA-Stimulated Asthma in Mice

Qian Yu et al.

Summary: This study found that Andrographolide can inhibit the inflammatory response of asthma in OVA-stimulated mice by blocking the activation of Th17-regulated cytokines and the JAK1/STAT3 signaling pathway.

EVIDENCE-BASED COMPLEMENTARY AND ALTERNATIVE MEDICINE (2021)

Article Pharmacology & Pharmacy

Andrographolide improves PCP-induced schizophrenia-like behaviors through blocking interaction between NRF2 and KEAP1

Xiying Wang et al.

Summary: Andrographolide, a compound from Andrographis paniculate, shows potential in ameliorating schizophrenia-like behaviors induced by PCP through inhibition of inflammation and oxidative stress. It not only inhibits the production of inflammatory cytokines but also enhances antioxidative enzyme activity and NRF-2 pathway, leading to improvements in schizophrenia-like symptoms.

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A Computational Approach Identified Andrographolide as a Potential Drug for Suppressing COVID-19-Induced Cytokine Storm

Mohd Rehan et al.

Summary: This study identified andrographolide, a drug molecule naturally present in Andrographis paniculata, as a potential candidate to reduce the cytokine storm induced by SARS-CoV-2 infection, offering a new drug strategy in the fight against COVID-19.

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Protective effect of andrographolide against STZ induced Alzheimer's disease in experimental rats: possible neuromodulation and Aβ(1-42) analysis

Royal Patel et al.

Summary: Andrographolide (ANDRO) shows neuroprotective effects against ICV-STZ induced AD-like symptoms in rats, improving behavioral deficits and alterations in biochemical, neuroinflammatory mediators, and neurotransmitters in the hippocampus.

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Andrographolide attenuates synovial inflammation of osteoarthritis by interacting with tumor necrosis factor receptor 2 trafficking in a rat model

Rongliang Wang et al.

Summary: Andro can suppress synovial inflammation and OA progression by regulating TNFR2 trafficking and degradation, providing a potential novel therapeutic approach for OA and pain management.

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Improvement of Oxazolone-Induced Ulcerative Colitis in Rats Using Andrographolide

Liuhong Zhang et al.

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Andrographolide mitigates cartilage damage via miR-27-3p-modulated matrix metalloproteinase13 repression

Shaojian Chen et al.

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Andrographolide and its fluorescent derivative inhibit the main proteases of 2019-nCoV and SARS-CoV through covalent linkage

Tzu-Hau Shi et al.

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Andrographolide derivative ameliorates dextran sulfate sodium-induced experimental colitis in mice

Bao-Jian Guo et al.

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Synthesis of andrographolide analogues and their neuroprotection and neurite outgrowth-promoting activities

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Andrographolide Ameliorates Rheumatoid Arthritis by Regulating the Apoptosis-NETosis Balance of Neutrophils

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Beneficial effects of andrographolide in a rat model of autoimmune myocarditis and its effects on PI3K/Akt pathway

Qi Zhang et al.

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Andrographolide ameliorates silica induced pulmonary fibrosis

Sachin Karkale et al.

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Andrographolide relieved pathological pain generated by spared nerve injury model in mice

Huang-Chi Wang et al.

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Andrographolide attenuates viral myocarditis through interactions with the IL-10/STAT3 and P13K/AKT/NF- signaling pathways

Yaxin Zhao et al.

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Attenuation of Innate Immunity by Andrographolide Derivatives Through NF-κB Signaling Pathway

Xin Nie et al.

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Is there a future for andrographolide to be an anti-inflammatory drug? Deciphering its major mechanisms of action

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Andrographolide protects liver cells from H2O2 induced cell death by upregulation of Nrf-2/HO-1 mediated via adenosine A2a receptor signalling

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Andrographolide reduces cognitive impairment in young and mature AβPPswe/PS-1 mice

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Andrographolide protects against cigarette smoke-induced oxidative lung injury via augmentation of Nrf2 activity

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Protective Mechanism of Andrographolide against Carbon Tetrachloride-Induced Acute Liver Injury in Mice

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Absorption of andrographolides from Andrographis paniculata and its effect on CCl4-induced oxidative stress in rats

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Reproductive and Fertility Effects of an Extract of Andrographis paniculata in Male Wistar Rats

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Andrographolide interferes with T cell activation and reduces experimental autoimmune encephalomyelitis in the mouse

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