Andrographis paniculata or also known as Sambiloto Plant is a plant that has been utilized in traditional herbal medicine for thousands of years. Sambiloto has the nickname “King of Bitter” or the king of bitter taste due to its very bitter flavor on the tongue. However, the plant is still often used and consumed because it can be used to reduce symptoms of fever, sore throat, and reduce swelling1,2. Behind the benefits of sambiloto, there is a unique compound that is its main content, namely andrographolide.
Sambiloto, “King of Bitter”
Sambiloto (Andrographis paniculata) is an herbaceous plant from the family Acanthaceae. This plant grows naturally in India, Sri Lanka, Pakistan, as well as Southeast Asian countries like Indonesia, but is also widely cultivated in China3. This plant is reported to have antibacterial, antifungal, antiviral activities, as well as choleretic, hypoglycemic, hypocholesterolemic, and adaptogenic effects4.
In the region of India, this plant is one of the most widely used plants in the Ayurveda herbal book. Meanwhile, in China, the herb from the leaves of Sambiloto is called Chuanxinlian, Yijianxi or Lanhelian which is used as an antipyretic, anti-inflammatory, and blood detoxifier4. Due to its widespread use around the world, this plant has various local names from different regions, including “kalmegh” in India, “senshinren” in Japan, “hempedu bumi” in Malaysia, “fah talai” in Thailand, and “green chiretta” in Scandinavian countries5.
Main Compound Sambiloto: Andrographolide
Andrographolide (C20H30O5) is a diterpene lactone compound that is one of the main components of the Sambiloto plant (Andrographis paniculata). This compound was first isolated from the plant in 19514. Andrographolide is suspected to be the main cause of the bitterness of this plant, however, further research shows that the bitterness is generally caused not only by andrographolide but also by another compound called kalmeghin6.
The compound Andrographolide is insoluble in water but can dissolve in acetone, methanol, chloroform, and ether. This results in andrographolide having low bioavailability and its use in oral formulations is very limited. However, optimization of andrographolide use can be developed with various formulation methods such as the use of nanoparticles or microparticles5.
Pharmacological Effects Andrographolide
In addition to being the main compound and the compound responsible for the bitter taste in the sambiloto plant, Andrographolide is also noted as the compound that plays the most significant role in various pharmacological effects of the sambiloto plant. The pharmacological effects of andrographolide that have been widely studied include anti-viral, anti-thrombotic, hepatoprotective, anticancer, and anti-inflammatory effects5.
1. Anti-inflammatory
Inflammation can be found in various diseases in various systems, such as asthma, chronic obstructive pulmonary disease (COPD), pneumonia, and pulmonary fibrosis in respiration, colitis and toxic liver fibrosis in the digestive system, osteoarthritis, multiple sclerosis, and gout in the immune system, as well as Alzheimer’s and Parkinson’s disease in the nervous system. Therefore, the anti-inflammatory effects of andrographolide can be applied in the management or reduction of the effects of these various conditions4.
Various studies have been conducted regarding the utilization of andrographolide for the various conditions mentioned above, yielding satisfactory results. For example, in a study involving the administration of andrographolide to asthma-induced mice, it was found that andrographolide could influence that condition by inhibiting NF-κB signalling, NLRP3 inflammasome, and ROS7. Inhibition of NF-κB pathway also found in tests of andrographolide use in rats induced with acute colitis8. In addition, the role of andrographolide on NLRP3 inflammasome also found in tests of the effects of andrographolide on rats induced with parkinson’s disease9.
2. Antioxidant
Andrographolide acts as an antioxidant by directly neutralizing free radicals. In addition, indirectly, andrographolide can also play a role in preventing the formation of free radicals by protecting mitochondrial integrity or inhibiting pro-oxidant enzymes, as well as activating antioxidant enzymes by activating signaling pathway of Nrf25.
3. Cancer Treatment
Andrographolide is known to have anti-tumor effects. Therefore, the potential of andrographolide in cancer treatment has become one of the topics that is widely studied. In various tests of the anti-tumor effects of andrographolide both in vitro and in vivo, it can be concluded that several pharmacological activities of andrographolide such as inhibiting proliferation, angiogenesis, metastasis, and tumor invasion, and immune escape of tumors, inducing cell death, to damaging tumor microenvironment. When used together with chemotherapy and radiotherapy, andrographolide shows ability to enhance tumor cell sensitivity to treatment, providing synergistic effects with other anticancer drugs. However, currently no main molecular targets associated with these activities have been found, so further research is still needed to improve the safety and effectiveness of using this compound in cancer management10.
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References
1. Zeng, B., Wei, A., Zhou, Q., Yuan, M., Lei, K., Liu, Y., Song, J., Guo, L., & Ye, Q. (2021). Andrographolide: A review of its pharmacology, pharmacokinetics, toxicity and clinical trials and pharmaceutical researches. Phytotherapy Research, 36(1), 336–364. https://doi.org/10.1002/ptr.7324
2. Chen, X., Ren, J., Yang, J., Zhu, Z., Chen, R., & Zhang, L. (2023). A critical review of Andrographis paniculata. Medicinal Plant Biology, 2(1), 0. https://doi.org/10.48130/mpb-2023-0015
3. Mishra, S. K., Sangwan, N. S., Sangwan, R. S. (2007-07-25). Andrographis paniculata (Kalmegh): A Review. Pharmacognosy Reviews, 1(2), 283-298.
4. Li, X., Yuan, W., Wu, J., Zhen, J., Sun, Q., & Yu, M. (2022). Andrographolide, a natural anti-inflammatory agent: An Update. Frontiers in Pharmacology, 13, 920435. https://doi.org/10.3389/fphar.2022.920435
5. Mussard, E., Cesaro, A., Lespessailles, E., Legrain, B., Berteina-Raboin, S., & Toumi, H. (2019). Andrographolide, a natural antioxidant: an update. Antioxidants, 8(12), 571. https://doi.org/10.3390/antiox8120571
6. Akbar, S. (2011). Andrographis paniculata: a review of pharmacological activities and clinical effects. PubMed, 16(1), 66–77. https://pubmed.ncbi.nlm.nih.gov/21438648
7. Peng, S., Hang, N., Liu, W., Guo, W., Jiang, C., Yang, X., et al. (2016). Andrographolide sulfonate ameliorates lipopolysaccharide-induced acute lung injury in mice by down-regulating MAPK and NF-κB pathways. Acta Pharm. Sin. B 6 (3), 205–211. doi:10.1016/j.apsb.2016.02.002
8. Kim, N., Lertnimitphun, P., Jiang, Y., Tan, H., Zhou, H., Lu, Y., et al. (2019). Andrographolide inhibits inflammatory responses in LPS-stimulated macrophages and murine acute colitis through activating AMPK. Biochem. Pharmacol. 170, 113646. doi:10.1016/j.bcp.2019.113646
9. Ahmed, S., Kwatra, M., Ranjan Panda, S., Murty, U. S. N., and Naidu, V. G. M. (2021). Andrographolide suppresses NLRP3 inflammasome activation in microglia through induction of parkin-mediated mitophagy in in-vitro and in-vivo models of Parkinson disease. Brain Behav. Immun. 91, 142–158. doi:10.1016/j.bbi.2020.09.017
10. Hu, J., Li, Y., Xie, X., Song, Y., Yan, W., Luo, Y., & Jiang, Y. (2024). The therapeutic potential of andrographolide in cancer treatment. Biomedicine & Pharmacotherapy, 180, 117438. https://doi.org/10.1016/j.biopha.2024.117438
Editorial Team:
- Rafi Rif'atul Rizki, S.I.Kom.
