Saturday, November 10, 2018

CCH A summary of antihyperlipidemic effects of representative Chinese herbal medicines


Currently there are more than 50 TCM formulae in the form of patent drugs that have been approved by China Food and Drug Administration used for treating hyperlipidemia [16]. This implies that there is a great demand on hyperlipidemic TCM products in the market.

Chinese herbal medicines  
Sources  
Possible bioactive compounds  
Effects mentioned in TCMs [54, 94]  
Possible hypolipidemic mechanisms  
Alismatis Rhizoma (Zexie)  
Dried rhizome of Alisma orientale (Sam.) Juzep.  
Alisol-triterpenes [59]  
(i) Promoting urination to drain dampness(ii) Discharging heat(iii) Resolving turbidity and lowering lipid  
(i) Decreasing the liver synthesis of cholesterol [57](ii) Lessening lipid peroxidation and activating antioxidant enzymes [58]  
  
Coptidis Rhizoma(Huanglian/Goldthread)  
Dried rhizome of Coptis chinensis Franch. or C. deltoidea C. Y. Cheng et Hsiao.  
Alkaloids [64], esp. berberine [66, 67]  
(i) Clearing heat and drying dampness(ii) Discharging fire and removing toxin  
(i) Reducing lipid peroxidation [63, 64](ii) Upregulating PPARα (iii) Negative modulation of FXR to upregulate the gene expression of CYP7A1 for cholesterol conversion into bile acids [64](iv) Decreasing degradation of dietary polysaccharides [65](v) Upregulation of LDLR in vitro and in vivo [66]  
  
Crataegi Fructus (Shanzha/Hawthorn)  
Dried ripe fruit of Crataegus pinnatifida Bge. and C. pinnatifida Bge. var. major N. E. Br.  
Polyphenols [70] and triterpenic acids for example oleanolic acid and ursolic acid [71]  
(i) Promoting digestion and invigorating the stomach(ii) Resolving turgidity and lowering lipid(iii) Moving Qi and dissipating blood stasis  
(i) Activating PPARα [69](ii) Inhibiting intestinal ACAT activity in human colon carcinoma cell line Caco-2 [71]  
  
Ginseng Radix et Rhizoma (Renshen/Asian ginseng)  
Dried root of Panax ginseng C. A. Mey.  
(i) Saponins [78, 79](ii) Acidic polysaccharides [81](iii) Phenolic extract [83]  
(i) Greatly tonifying the original Qi (ii) Resuming pulse and securing collapse(iii) Replenishing "lung " and "spleen "(iv) Engendering fluid and nourishing blood(v) Calming the mental state and enhancing intelligence   
(i) Improving lipid peroxidation in liver by reduction in serum MDA [76, 83, 87](ii) Activating LPL activity [81](iii) Inhibiting pancreatic lipase [82](iv) Inhibiting food appetite via modifying the serum content and mRNA expression of neuropeptide Y, Y2 receptor, and peptide YY [85]  
  
Notoginseng Radix et Rhizoma (Sanqi)  
Rhizome and root of Panax notoginseng (Burk.) F. H. Chen  
Sanqi saponins [95]  
(i) Dissipating stasis and stanching bleeding(ii) Dispelling swelling and relieving pain  
(i) Reducing HMG-CoA reductase (ii) Reducing lipid peroxidation by increase in the activity of antioxidant hepatic SOD and glutathione peroxidase [95](iii) Inducing the biosynthesis of bile acids from cholesterol and promoting the β -oxidation of FA in the liver [96](iv) Acting as a dual FXR/LXR α agonist [124]  
  
Oryzae cum Monasco Semen (Red yeast rice/Hongqu)  
Washed and cooked rice fermented with Monascus purpureus Went  
Monacolins, esp. monacolin K [104, 110]  
(i) Strengthening "spleen " to improve food digestion(ii) Promoting blood circulation to dissipate blood stasis  
Containing a family of monacolins that resemble HMG-CoA reductase inhibitors [104]  
  
Puerariae Lobatae Radix (Gegen/Kudzu root)  
Dried root of Pueraria lobata (Willd.) Ohwi  
Puerarin [113]  
(i) Resolving the flesh and reducing fever(ii) Engendering fluid to quench thirst(iii) Promoting eruption(iv) Uprasing the middle Qi to relieve diarrhea(v) Unblocking meridian and activating collaterals(vi) Removing wine toxin  
(i) Promoting cholesterol and bile acids excretion in liver [113](ii) Estrogen-like effect on lipid metabolism in liver and adipose tissues [116](iii) Hepatoprotective effect in OVX-induced hepatic steatosis [114]  
  
Rhei Radix et Rhizoma (Dahuang)  
Root and rhizome of Rheum palmatum L., R . tanguticum Maxim or R . officinale Baill.   
Rhein [123-125]  
(i) Relaxing the bowels(ii) Cooling the blood and removing toxin(iii) Expelling stasis to unblock the meridian  
(i) Inhibitory effect on HMG-CoA reductase [123](ii) Having LXR antagonism and regulation of uncoupling protein-1 expression in brown adipose tissues [125]  
  
Salviae Miltiorrhizae Radix (Danshen)  
Dried root of Salvia miltiorrhiza Bunge.  
(i) Danshensu(ii) Rosmarinic acid(iii) Salvianolic acid A and B [133]   
(i) Promoting blood circulation and dispelling stasis(ii) Nourishing the blood and calming mental state(iii) Regulating menstruation and suppressing pains(iv) Cooling blood and eliminating carbuncle  
(i) Containing antioxidant (esp. salvianolic acid B) for prevention of endothelial damage and inhibition of LDL oxidation [133](ii) Acting as a FXR/LXR α coagonist [134]  
Table 3: A summary of antihyperlipidemic effects of different TCM formulae.
TCM formulae  
Herbs (weight ratio in dose if applicable)  
Effects mentioned in TCMs  
Effects on blood lipid profile  
Possible hypolipidemic mechanisms  
Danggui-Buxue decoction  
Astragali Radix and Angelicae Sinensis Radix (1 : 5) [153]  
(i) Raising the Qi (ii) Nourishing the blood [17]  
(i) Lowering serum TC and LDL-C levels(ii) Increasing HDL-C level(iii) No significant difference in TG level as compared with diabetic atherosclerosis model group [49, 154]  
Downregulating the mRNA expression of MCP-1, ICAM-1, and CD36 [49, 154]  
  
Danshen-Gegen formula  
Salviae Miltiorrhizae Radix and Puerariae Lobatae Radix (7 : 3) [53]  
(i) Promoting blood circulation (ii) Removing blood stasis [200]  
(i) A significant dose-dependent decrease in free and esterified TC in the human monocyte derived macrophages in vitro [147](ii) Lowering TC and LDL-C levels mildly in patients suffering from coronary artery disease compared with placebo [56](iii) Lowering TC and LDL levels in postmenopausal women with hypercholesterolemia [52]  
Dose-related suppression of acetylated LDL uptake by human macrophages [53]  
  
Erxian decoction  
Curculiginis Rhizoma, Epimedii Folium, Angelicae Sinensis Radix, Morindae Officinalis Radix, Anemarrhenae Rhizoma, and Phellodendri Chinensis Cortex (no fixed ratio) [60]  
(i) Warming "kidney " Yang (ii) Nourishing "kidney " Yin (iii) Clearing ministerial fire (iv) Harmonizing thoroughfare and conception vessels(v) Balancing Yin-Yang [60]  
(i) Suppressing serum TC and LDL-C levels(ii) No significant effect on HDL-C and TG levels in a menopausal rat model [54]  
(i) Downregulating HMG-CoA(ii) Upregulating the LDL receptor [54]  
  
Ling-Gui-Zhu-Gan decoction  
Poria, Cinnamomi Ramulus, Atractylodis Macrocephalae Rhizoma, and Glycyrrhizae Radix (4 : 3 : 3 : 2) [63]  
(i) Warming Yang for resolving fluid retention(ii) Strengthening the "spleen" to resolve dampness [63]  
(i) Reducing TG and TC levels in HFD induced rat models of NAFLD [57](ii) Lowering ghrelin level in HFD rat groups fasting intermittently supplemented with LGZD [63]  
(i) Increasing serum thyroid hormone levels [57](ii) Improving β -oxidation via modulation of TRβ 1 and CPT1A expression in liver [57](iii) Enhancing metabolism and transport of FA through modulation of SREBP-1c, ACSL and ApoB100 expression [57]  
  
Shengmai Yin  
Ginseng Radix et Rhizoma, Ophiopogonis Radix, and Schisandra Chinensis Fructus (2 : 1 : 2) [58]  
(i) Replenishing both Qi and Yin energies(ii) Generating body fluids(iii) Restoring the pulses [17]  
(i) No significant effect on lipids of Wistar rats fed with HCD(ii) Lowering hepatic cholesterol and TG contents (iii) No effect on fecal cholesterol excretion but higher fecal bile acid content [59]  
(i) Stimulating the biosynthesis of bile acid using cholesterol as the precursor (ii) Increasing hepatic cholesterol catabolism [59]  
  
Turtle jelly  
Testudinis Plastrum, plus various Chinese medicinal herbs such as Smilacis Glabrae Rhizoma, Millettiae Speciosae Radix, Mesonae Chinensis Herba, and Lonicerae Japonicae Flos [173]  
(i) Clearing heat(ii) Removing toxin(iii) Promoting urination [51]  
(i) Lowering serum TC and LDL levels(ii) Increasing HDL level diet-induced hypercholesterolemic SD rats [50]  
(i) Blocking the downregulation of LDLR and PEPCK mRNA and protein expressions (ii) Suppressing the upregulation of PPARα mRNA and protein expressions in the liver [173]  
  
Xuefu-Zhuyu decoction  
Bupleuri Chinensis Radix, Angelicae Sinensis Radix, Rehmanniae Radix, Paeoniae Rubra Radix, Carthami Flos, Persicae Semen, Aurantii Fructus Immaturus, Glycyrrhizae Radix, Platycodi Radix, Chuanxiong Rhizoma, and Achyranthis Bidentatae Radix [61]  
(i) Promoting blood circulation to remove blood stasis (ii) Moving Qi to relieve pain [17]  
(i) Lowering serum TC and LDL-C levels (ii) Increasing HDL-C level(iii) No significant difference in TG level in HFD fed SD rats as compared with the model group [62](iv) Lowering TG level and TC/HDL-C ratio in HCD fed Wistar rats [182]  
(i) Reversing energy and lipid metabolism disturbance(ii) Decreasing the accumulation acetyl-glycoproteins (iii) Enhancing glutathione biosynthesis [62](iv) Inhibiting proinflammatory interleukin 8 production [182]  

Tung-Ting Sham, Chi-On Chan, You-Hua, W., Jian-Mei, Y., Mok, D. K., & Shun-Wan, C. (2014). A review on the traditional chinese medicinal herbs and formulae with hypolipidemic effect. BioMed Research International, 2014 doi:http://dx.doi.org.ezp-prod1.hul.harvard.edu/10.1155/2014/925302 

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