Ligusticum sinense 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

Main Characteristics:

Active Compounds (2,3,4,5) 

1. Ligustrazine (Tetramethylpyrazine or TMP) 

2. Ligustilide (a phthalide)

3. Ferulic acid 

4. Senkyunolide 

Pharmacodynamic Studies 

 

1. Ligustrazine Tetramethylpyrazine (TMP)

 

Systematic Review:

"Ligusticum Chuanxiong reduces arterial resistance, increases cerebral blood flow, improves microcirculation, reduces capillary permeability, and has protective effects on brain injury (10)."

 

Controlled Studies:

Suppresses vasoconstriction produced by Endothelin-1 (ET-1). Prevents tissue damage from ET-1 and increases 6-keto-PGF1, a natural degraded form of prostacyclin (PGI2), an important lipid that induces antithrombotic, anti-inflammatory effects (9). Also promotes adenylyl cyclase to produce cAMP which inhibits platelet activation, activates endothelial smooth muscle relaxation, and encourage vasodilation.

TMP has a neuroprotective effect by inhibiting neutrophil activation, mediating free radical oxidation activity, resulting in reduction of infarct volume and helps prevent and improve the function of ischemia reperfusion brain injuries and related disorders.

TMP regulates epinephrine, serotonin, calcium levels, and cAMP. 

 

Antithrombotic, anti-inflammatory effects of TMP, antiplatelet, smooth muscle relaxation, vasodilatory factors  assists diabetic complication, nephropathy, or renal disorder (6). 

 

Renal vasodilation via endothelial stimulation seems to assist patients with chronic heart failure in a clinical trial comparing renal dilation effects of acetylcholine and nitroglycerin (13). In theory, TMP, which causes renal vasodilation and increases renal blood flow should assist chronic heart failure. 

 

Ligustrazine (Tetramethylpyrazine) can protect HUVECs (human umbellical vein endothelial cells) against peroxide injuries by regulating indicators related to oxidative stress, and suppressing the overexpression of caspase dependent anti-apoptotic mechanism, which provide important information treating and preventing oxidative stress induced atherosclerosis (7,8). 

 

2. Phthalides

 

Bioactive phthalides: from Ligusticum sinense Oliv cv. ChaxiongSummary: 5 New phthalides, natural oil, found in Ligusticum sinense, tested against SK-N-SH cell depriving oxygen and glucose showing increase of cell survival. “Among which [compounds a few] showed higher cell survival rates than ginsenoside Rg1. The new compounds (new phthalides, natural products and known phthalides) when isolated and compared with ginsenoside Rg1 as positive control, shows “protective activity” against “neuronal impairement induced by the deprival of oxygen and glucose.” Especially in compounds 1,4,8 where there were a respective 11.16%, 10.35%, 9.47% increased SK-N-SH cell survival (11). 

 

Attenuation of LPS induced pro-inflammatory responses (12). 

 

 

 

 

 

 

 

 

References:

1. History of Aspirin. (n.d.). Retrieved from http://www.aspree.org/AUS/aspree-content/aspirin/history-aspirin.aspx

 

2. Wang J, Yang JB, Wang AG, Ji TF, Su YL. [Studies on the chemical constituents of Ligusticum sinense]. Zhong Yao Cai. 2011 Mar;34(3):378-80. Chinese. PubMed PMID: 21823452.

 

3. Xiao YQ, Li L, You XL, Taniguchi M, Baba K. [Studies on chemical constituents of the rhizomae of Ligusticum chuanxiong]. Zhongguo Zhong Yao Za Zhi. 2002 Jul;27(7):519-22. Chinese. PubMed PMID: 12776516.

 

4. Zhu CF, Shi QX, Yan YP, Liu SW, Sun LY, Liu FJ, Tong LQ. [Determination and fingerprint analysis of tetramethylpyrazine and ferulic acid in Ligusticum chuanxiong]. Zhong Yao Cai. 2008 Aug;31(8):1113-5. Chinese. PubMed PMID: 19112885.

 

5. Yang, Qi-Hong; Liang, Yong; Xu, Qiang; Zhang, Yi; Xiao, Li; Si, Liang-Yi. [Protective effect of tetramethylpyrazine isolated from Ligusticum chuanxiong on nephropathy in rats with streptozotocin-induced diabetes]. Phytomedicine: International Journal of Phytotherapy & Phytopharmacology. 2011 Oct; Retrieved from http://www.thefreelibrary.com/Protective+effect+of+tetramethylpyrazine+isolated+from+Ligusticum...-a0274956554

 

6. Yang QH, Liang Y, Xu Q, Zhang Y, Xiao L, Si LY. Protective effect of tetramethylpyrazine isolated from Ligusticum chuanxiong on nephropathy in rats with streptozotocin-induced diabetes. Phytomedicine. 2011 Oct 15;18(13):1148-52. doi: 10.1016/j.phymed.2011.05.003. Epub 2011 Jun 12. PubMed PMID: 21665452.

 

7. Gui-dong, H., Jian, M., & Zhong-wei, J. (2013). Anti-oxidative Effect of Ligustrazine on Treatment and Prevention of Atherosclerosis. Tropical Journal Of Pharmaceutical Research, 12(6), 949-957. doi:10.4314/tjpr.v12i6.13

 

8. Zhang, F., Ni, C., Kong, D., Zhang, X., Zhu, X., Chen, L., & ... Zheng, S. (2012). Ligustrazine attenuates oxidative stress-induced activation of hepatic stellate cells by interrupting platelet-derived growth factor-β receptor-mediated ERK and p38 pathways. Toxicology & Applied Pharmacology, 265(1), 51-60. doi:10.1016/j.taap.2012.09.016

 

9. Peng, W., Chun-hua, L., Qun-xing, W., Qian-yuan, L., Peng, L., & Xiao-hui, Y. (2013). Antithrombotic effect of ligustrazine hydrochloride injection on the model of induced arteriovenous shunt thrombosis. Journal Of Research In Medical Sciences, 18(8), 704-706.

 

10. Mingfei Zeng, Linmei Pan, Shunmei Qi, Yuntai Cao, Huaxu Zhu, Liwei Guo, Jing Zhou, Systematic review of recent advances in pharmacokinetics of four classical Chinese medicines used for the treatment of cerebrovascular disease, Fitoterapia, Volume 88, July 2013, Pages 50-75, ISSN 0367-326X, http://dx.doi.org/10.1016/j.fitote.2013.04.006. (http://www.sciencedirect.com/science/article/pii/S0367326X13001044) Keywords: ADME (absorption, distribution, metabolism and excretion); Cerebrovascular disease; Chinese medicine; Pharmacokinetics; Bioavailability; Drug interaction

 

11. Qian Wei, Jianbo Yang, Jin Ren, Aiguo Wang, Tengfei Ji, Yalun Su, Bioactive phthalides from Ligusticum sinense Oliv cv. Chaxiong, Fitoterapia, Volume 93, March 2014, Pages 226-232, ISSN 0367-326X, http://dx.doi.org/10.1016/j.fitote.2014.01.010. (http://www.sciencedirect.com/science/article/pii/S0367326X14000161) Keywords: Ligusticum sinense Oliv cv. Chaxiong; Aerial parts; Phthalide; CD; Modified Mosher's method; Neuronal impairment protective effect

 

12. Shao M, Qu K, Liu K, Zhang Y, Zhang L, Lian Z, et al. Effects of ligustilide on lipopolysaccharide-induced endotoxic shock in rabbits. Planta Med 2011;77:809–16

 

13. Elkayam U, Cohen G, Gogia H, Mehra A, Johnson JV, Chandraratna PA. Renal vasodilatory effect of endothelial stimulation in patients with chronic congestive heart failure. J Am Coll Cardiol. 1996 Jul;28(1):176-82. PubMed PMID: 8752811.