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

Abstract

Andrographis paniculata (Burm. f.) Wall. ex Nees, a renowned herb medicine in China, is broadly utilized in traditional Chinese medicine (TCM) for the treatment of cold and fever, sore throat, sore tongue, snake bite with its excellent functions of clearing heat and toxin, cooling blood and detumescence from times immemorial. Modern pharmacological research corroborates that andrographolide, the major ingredient in this traditional herb, is the fundamental material basis for its efficacy. As the main component of Andrographis paniculata (Burm. f.) Wall. ex Nees, andrographolide reveals numerous therapeutic actions, such as antiinflammatory, antioxidant, anticancer, antimicrobial, antihyperglycemic and so on. However, there are scarcely systematic summaries on the specific mechanism of disease treatment and pharmacokinetics. Moreover, it is also found that it possesses easily ignored security issues in clinical application, such as nephrotoxicity and reproductive toxicity. Thereby it should be kept a lookout over in clinical. Besides, the relationship between the efficacy and security issues of andrographolide should be investigated and evaluated scientifically. In this review, special emphasis is given to andrographolide, a multifunctional natural terpenoids, including its pharmacology, pharmacokinetics, toxicity and pharmaceutical researches. A brief overview of its clinical trials is also presented. This review intends to systematically and comprehensively summarize the current researches of andrographolide, which is of great significance for the development of andrographolide clinical products. Noteworthy, those un‐cracked issues such as specific pharmacological mechanisms, security issues, as well as the bottleneck in clinical transformation, which detailed exploration and excavation are still not to be ignored before achieving integration into clinical practice. In addition, given that current extensive clinical data do not have sufficient rigor and documented details, more high‐quality investigations in this field are needed to validate the efficacy and/or safety of many herbal products.

Use of Andrographis paniculata (Burm.f.) Wall. ex Nees and risk of pneumonia in hospitalised patients with mild coronavirus disease 2019: A retrospective cohort study

“…In contrast to the results from a trial of Xiyanping from which andrographolide was given as an intravenous route and significant recovery was found in an active group, ( 11 ) our results were from oral administration of AP. Although there is no direct comparison study of the efficacy of AP in different dosage forms, it has been shown that andrographolide has a poor oral bioavailability (<3%) primarily due to undergoing rapid metabolism at duodenal and jejunal cells ( 17 ).…”

“…In contrast to the results from a trial of Xiyanping from which andrographolide was given as an intravenous route and significant recovery was found in an active group, (11) our results were from oral administration of AP. Although there is no direct comparison study of the efficacy of AP in different dosage forms, it has been shown that andrographolide has a poor oral bioavailability (<3%) primarily due to undergoing rapid metabolism at duodenal and jejunal cells (17). ¶ Worsening symptoms were the composite of receiving antiviral drugs, systemic corticosteroids, or ventilator support; having oxygen saturation drop along with worsening signs and symptoms; or presenting regressive chest X-ray findings (i.e., category three or above).…”

Use of Andrographis paniculata (Burm.f.) Wall. ex Nees and risk of pneumonia in hospitalised patients with mild COVID-19: a retrospective cohort study

“…Although there is no direct comparison study of the efficacy of AP in different dosage forms, it has been shown that andrographolide has a poor oral bioavailability (<3%) primarily due to undergoing rapid metabolism at duodenal and jejunal cells. (17)…”

Andrographolide, a natural anti-inflammatory agent: An Update

“…The results of a randomized controlled trial of 44 patients showed that andrographolide in the treatment of multiple sclerosis showed a trend to reduce the rate of brain atrophy and disability progression, but andrographolide had adverse events of rash and dysgeusia ( Ciampi et al, 2020 ). Some people have pointed out that their nephrotoxicity and reproductive toxicity are more common ( Zeng et al, 2022 ). In terms of hepatotoxicity, from the application of andrographolide in liver diseases, we can find that andrographolide has a good repairing effect on hepatotoxicity, but there is no evidence that it can induce liver damage.…”