Department of Pharmacology, Yong Loo Lin School of Medicine, National University Health System, Singapore.
Clin Exp Pharmacol Physiol. 2012 Mar;39(3):300-10. doi: 10.1111/j.1440-1681.2011.05633.x.
1. Andrographis paniculata (Burm. f) Nees, commonly known as 'king of bitters', is a herbaceous plant belonging to the Family Acanthaceae. It has been widely used for centuries in Asian countries like China, India, Thailand and Malaysia for the treatment of sore throat, flu and upper respiratory tract infections. 2. Andrographolide, 14-deoxy-11,12-didehydroandrographolide and neoandrographolide are examples of the major labdane diterpenoids isolated from A. paniculata. These bioactive molecules have exhibited varying degrees of anti-inflammatory and anticancer activities in both in vitro and in vivo experimental models of inflammation and cancer. 3. Extensive libraries of andrographolide analogues have been synthesised mainly by modifying the α,β-unsaturated γ-butyrolactone moiety, the two double bonds Δ(8,(17)) and Δ(12,(13)) and the three hydroxyls at C-3 (secondary), C-14 (allylic) and C-19 (primary). Many of these synthetic analogues exhibit superior anticancer activity over the naturally occurring andrographolides. 4. Andrographolide and its derivatives have been shown to have anti-inflammatory effects in experimental models of asthma, stroke and arthritis, as well as in patients with upper respiratory tract infections. Andrographolide reduces the production of cytokines, chemokines, adhesion molecules, nitric oxide and lipid mediators, probably via inhibition of the nuclear factor (NF)-κB signalling pathway. 5. The anticancer mechanisms for andrographolide include inhibition of Janus tyrosine kinases-signal transducers and activators of transcription, phosphatidylinositol 3-kinase and NF-κB signalling pathways, suppression of heat shock protein 90, cyclins and cyclin-dependent kinases, metalloproteinases and growth factors, and the induction of tumour suppressor proteins p53 and p21, leading to inhibition of cancer cell proliferation, survival, metastasis and angiogenesis. 6. Andrographolide drug discovery is a promising strategy for the development of a novel class of anti-inflammatory and anticancer drugs.
穿心莲（Burm. f） Nees，俗称“苦中之王”，是一种属于爵床科的草本植物。几个世纪以来，它在中国、印度、泰国和马来西亚等亚洲国家被广泛用于治疗喉咙痛、流感和上呼吸道感染。
从穿心莲中分离出的主要贝壳烯二萜类化合物有穿心莲内酯、14-脱氧-11,12-二去氢穿心莲内酯和新穿心莲内酯。这些生物活性分子在炎症和癌症的体内外实验模型中表现出不同程度的抗炎和抗癌活性。
主要通过修饰 α,β-不饱和γ-丁内酯部分、两个双键 Δ(8,(17))和 Δ(12,(13))以及 C-3（仲）、C-14（烯丙基）和 C-19（伯）的三个羟基，合成了广泛的穿心莲内酯类似物文库。这些合成类似物中的许多表现出比天然穿心莲内酯更高的抗癌活性。
在哮喘、中风和关节炎的实验模型以及上呼吸道感染患者中，穿心莲内酯及其衍生物表现出抗炎作用。穿心莲内酯通过抑制核因子（NF）-κB 信号通路，减少细胞因子、趋化因子、粘附分子、一氧化氮和脂质介质的产生。
穿心莲内酯的抗癌机制包括抑制 Janus 酪氨酸激酶-信号转导和转录激活因子、磷脂酰肌醇 3-激酶和 NF-κB 信号通路、抑制热休克蛋白 90、细胞周期蛋白和细胞周期蛋白依赖性激酶、金属蛋白酶和生长因子，以及诱导肿瘤抑制蛋白 p53 和 p21，从而抑制癌细胞增殖、存活、转移和血管生成。
穿心莲内酯药物发现是开发新型抗炎和抗癌药物的有前途的策略。
