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. 2023 Mar 7;12(6):1220.
doi: 10.3390/plants12061220.

Evaluations of Andrographolide-Rich Fractions of Andrographis paniculata with Enhanced Potential Antioxidant, Anticancer, Antihypertensive, and Anti-Inflammatory Activities

Sya'ban Putra Adiguna  1   2 , Jonathan Ardhianto Panggabean  1   2 , Respati Tri Swasono  1 , Siti Irma Rahmawati  2 , Fauzia Izzati  2 , Asep Bayu  2 , Masteria Yunovilsa Putra  2 , Carmen Formisano  3 , Chianese Giuseppina  3
Affiliations

Evaluations of Andrographolide-Rich Fractions of Andrographis paniculata with Enhanced Potential Antioxidant, Anticancer, Antihypertensive, and Anti-Inflammatory Activities

Sya'ban Putra Adiguna et al. Plants (Basel). .

Abstract

Andrographis paniculata is widely used as a traditional medicine in Asian countries. It has been classified as a safe and non-toxic medicine by traditional Chinese medicine. The investigation of the biological activities of A. paniculata is still focused on the crude extract and isolation of its main active compound, andrographolide, and its derivatives. However, the use of andrographolide alone has been shown to exacerbate unwanted effects. This highlights the importance of developing a fraction of A. paniculata with enhanced efficacy as an herbal-based medicine. In this study, the extraction and fractionation of A. paniculata, followed by quantitative analysis using high-performance liquid chromatography coupled with a DAD detector, were established to quantify the andrographolide and its derivative in each fraction. Biological activities, such as antioxidant, anticancer, antihypertensive, and anti-inflammatory activities, were evaluated to study their correlations with the quantification of active substances of A. paniculata extract and its fractions. The 50% methanolic fraction of A. paniculata exhibited the best cytotoxic activities against CACO-2 cells, as well as the best anti-inflammatory and antihypertensive activities compared to other extracts. The 50% methanolic fraction also displayed the highest quantification of its main active compound, andrographolide, and its derivatives, 14-deoxy-11,12-didehydroandrographolide, neoandrographolide, and andrograpanin, among others.

Keywords: Andrographis paniculata; andrographolide; anti-inflammatory; anticancer; antihypertensive; antioxidant; traditional Chinese medicine.

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Conflict of interest statement

All the authors declare no conflict of interest regarding this work.

Figures

Figure 1
Figure 1
Chemical structures of four diterpene lactones from A. paniculata.
Figure 2
Figure 2
(a) An HPLC chromatogram of the standard compounds of andrographolide and its derivatives and (b) an HPLC chromatogram of extract and fractions compared with the standard compounds. ME, F1, F2, F3, and std are methanolic crude extract, fraction 1, fraction 2, fraction 3, and the standard solution. The details of the chromatographic analysis can be found in the experimental method.
Figure 3
Figure 3
Morphological changes in CACO-2 cell lines when treated with F2 and F3 and doxorubicin when compared to a blank control (untreated cell).
Figure 4
Figure 4
Cytotoxic activity of Andrographis paniculata extract and its fractions expressed as 50% inhibition concentration (IC50) values. F2, which contains the highest levels of the four investigated diterpene lactone compounds, shows the lowest IC50 value, followed by ME and F1. F3, which contains only a small amount of andrographolide, has the highest IC50 value.
Figure 5
Figure 5
Inhibition of angiotensin-converting enzyme (ACE) activity by A. paniculata extract and fractions that showed antihypertensive activity (expressed as percentages) (p < 0.05).
See this image and copyright information in PMC

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