It is the inability to keep a firm erection that is strong enough for sexual intercourse. It is very demoralizing for the men because of the embarrassment of failure to run the full race and give the wife satisfaction. It is basically failure in bed. 

In older men, weak erection usually has a physical cause such as dysfunction of the organs, disease, injury or side effects of drugs. Any disorder that causes injury to the nerves or impairs blood flow in the penis has the potential to cause erection problems.

Causes

Doctors used to tell their patients that impotence problem is "all in the head". Times have changed and doctors now view the problem differently. Now allopathic science sees erection  as a series of mechanical instructions and impotence as a failure of any of these linkages:

• The brain sends the message
• Impulses from the brain and local nerves cause the muscles of the corpora cavernosa to relax
• Blood to flow in and fill the spaces
• Blood creates pressure in the corpora cavernosa
• The penis expand
• The tunica albuginea helps trap the blood in the corpora cavernosa
• Thereby sustaining erection

If the muscles of the corpora cavernosa failed to relax then erection fails. If the nerves, arteries, smooth muscles or fibrous tissues is/are damaged then erection can also fail.

These instructions can be interfere or disrupted by any of the following diseases or problems:

• Diseases: diabetes, kidney disease, chronic alcoholism, multiple sclerosis, atherosclerosis, cardiovascular disease (hypertension) and neurologic disease
• Lifestyle problems: smoking, being overweight and avoiding exercise
• Common medicines: blood pressure drugs, antihistamines, antidepressants, tranquilizers, appetite suppressants, and cimetidine (an ulcer drug)
• Psychological factors: stress, anxiety, guilt, depression, low self-esteem, and fear of sexual failure

But for herbal scientists they see impotence as the failure of the body's organs to function properly. For example let us look at the kidneys. For herbal scientists, the dysfunction of the kidneys would lead to ED problems.

Kidneys and Weak Erection

The healthy function of the kidneys is affected by:

• The adrenaline-like secretions of the adrenal medulla
• The androgenic hormones secreted by the adrenal cortex
• The thyroid hormone and growth hormone from the anterior pituitary gland.
• The secretion of erythropoietin by cells in the kidneys
• The liver which stimulates the bone marrow to create erythrocytes. 

The failure of the kidneys to function properly would result in: 

• coldness of the body
• lack of libido 
• impotence
• premature ejaculation
• edema of the lower limbs
• weakness of the lower extremities
• cold sensation in the lower half of the body

Coldness refers to the hypometabolic function of the body. Lack of sympathetic stimulation from the adrenal medulla is one cause of coldness. The adrenal medulla secretes two catecholamines: epinephrine and norepinephrine. The importance of these secretions is in their relationship to the sympathetic nervous system and the ability thereby to maintain healthy function of the body’s organs. A lack of erythropoietin in the kidneys will lead to kidney deficiency. Testosterone, being kidney hormone, also stimulates the secretion of erythropoietin.  A diminished secretion of thyroid hormone will also result in physical coldness.

Treatment: "Hot" herbs which have strong sympathetic stimulants in them may increase warmth by stimulating the secretion of adrenergic hormones such as testosterone and  consequently erythropoietin by kidney cells. 

Mineral Salt and Aldosterone

Let us look at how mineral salts and "electrolyte" imbalance can eventually lead to body suffering from impotence.

Mineral salt is important to body because the healthy function of our organs depends on the “electrolyte” balance in the body. Sodium chloride tends to attract and hold fluids whereas potassium has a discharging and eliminative effects on extra cellular fluid.

The osmotic process by which salt and potassium exchange ions affects the passage of other nutrients necessary for cellular metabolism. The ability of the kidneys to control this mineral content in the body would affect the health and functions of the body’s organ.

Aldosterone, the most important mineral corticoid is mainly controlled by the renin-angiotensin mechanism and by the concentration of potassium in the extra cellular fluid. Aldosterone is triggered by high concentrations of potassium in the extra cellular fluid causing a concomitant decrease of concentrations of sodium and chloride. With the decrease of sodium chloride, there is a reciprocal decrease of total extra cellular fluid and blood volume. In Herbalism this reduction of fluid and blood is one of the conditions of wasting and is often associated with kidney hypertension. This kidney problem if left untreated would eventually lead to ED problems.

Treatment

Allopathic Science uses drug to treat impotence. Some of them are:

• Phosphodiesterase (PDE) inhibitors: They work by enhancing the effects of nitric oxide, a chemical that relaxes smooth muscles in the penis during sexual stimulation and allows increased blood flow. They are taken one hour before intimacy. None of these PDE inhibitors should be used more than once a day. The common complain is that it gives you a headache. After 2 years they do not work so well.

• Oral testosterone: It can reduce ED in some men but it is often ineffective and may cause liver damage

• Injected drugs: Drugs such as papaverine hydrochloride, phentolamine, and alprostadil (marketed as Caverject) can be injected into the penis to widen blood vessels, causing it to become engorged with blood thus giving it an erection. These drugs may create unwanted side effects like persistent erection and scarring.

• Muscle relaxant: Nitroglycerin can sometimes enhance erection when rubbed on the penis.

• Others:  A pre-filled applicator is used to insert a pellet of alprostadil into the urethra to deliver a pellet about an inch deep into the urethra. An erection will begin within 8 to 10 minutes and may last 30 to 60 minutes. Side effects: Aching in the penis, testicles and area between the penis and rectum; warmth or burning sensation in the urethra; redness from increased blood flow to the penis; and minor urethral bleeding or spotting.

One can see that the above treatment is symptomatic. It is using various means of artificially probing up the dysfunction organ.

Herbal Science: To treat ED problems herbal science would use herbs to rejuvenate, nourish and strengthen the function of the body and its organs so that the root problem would be treated. Herbs can be used to strengthen the kidneys and liver, to nourish the blood and relax the smooth muscles (That is what Viagra does. The synthetic chemical relaxes the smooth muscles to cause an erection but with the added side effects). This is TCM's way to of restoring the body to better health and vitality. All these herbs used by herbal scientists have been proven to improve the functions of the body without any side effects or causing seriously long-term damage to the body unlike allopathic drugs.

TCM knows that kidneys control bone growth. For bone to grow, the body needs bone marrow. In TCM bone marrow is derived from kidney essence. That explains why those who suffers from osteoporosis also suffers from dysfunction kidneys. In recent years, many bone disorders have been successfully treated by TCM practitioners through treatment of the kidney.

The above researches have shown that these herbs improve the functions of the kidneys, liver, control and reduce cholesterol, improve blood essence and relax the smooth muscles. They work synergistically to restart the men’s engine to make life more meaningful. It has long lasting rejuvenation effect compare to Viagra which only relax the smooth muscles and can give headache and other side effects.

Herbs like Radix Morinda Officinalis, Radix Achyranthis Bidentatae, Rehmannia Root, Cornus Officinalis, Radix Paeonia and Radix Dipsaci are used for nourishing and rejuvenating the liver, kidneys, to nourish the blood and relaxing the smooth muscles.  Energy herbs like Ligusticum ChuanXiong and Panax Quinquefolium are used supplement the body with extra energy. All these provides holistic treatment.

1) Radix Morinda Officinalis

Function of the herb:

a) It is used to reinforce the vital function of the kidneys especially that of sexual organs for the treatment of impotence and premature ejaculation of men. The herb is pungent and sweet in flavour, slightly warm in nature, it is tropistic to the liver and kidney channels. Being sweet and warm, it can invigorate kidney-yang; as a pungent and warm agent, it is capable of dispelling wind-dampness. Being slightly warm, moist and dry, it has effects of invigorating Yang and supplementing vital essence and is especially effective in strengthening muscles and bones, serving to treat insufficiency of kidney-yang and deficiency-cold of essence and blood marked by impotence, infertility and athralgia due to wind-dampness. It tonifies the kidney, invigorating Yang, strengthening muscles and bones, dispelling wind and eliminating dampness.Source: "Legendary Chinese Healing Herbs" - Dr. Henry Lu- Academy of Oriental Heritage, Blaine, USA. The author is best known for his translation of "Yellow Emperor's Classics of Internal Medicine" written around 300 B.C. from Chinese to English; "Dictionary Of Traditional Chinese Medicine" written by Prof. Lou Zhicen - Professor of Pharmacognosy, Prof. Li Shuncheng - Associate Professor of Medicine and Prof. Tang Zijin - Associate Professor of Medicine of Beijing Medical College.

b) Research showed that it benefits the reproductive organs A 30g/kg/day dose of Radix Morindae Officinalis decoction was administered to castrated mice once a day for 15 days. Results showed that the weights of levator ani muscles, seminal vesicle and prostate were not significantly effected. Qiao Zhisheng, et al. Comparison of pharmacological activities of different Radix Morindae Officinalis species, Chinese Journal of Integrated Traditional and Western Medicine. 1991; 11(7):415.

2) Radix Achyranthes Bidentatae

Function of the herb:

• Nourish liver, kidney and strengthen sinew and bones

• Treats aching backs and knees

• Treats asthenia (loss of strength/debility) of lower limbs

• Regulates and activates blood

• Tones up liver and kidneys

Researches by scientists have shown that Radix Achyrantes can be used to improve bone quality. Bones are formed from bone marrows. Bone marrows come from kidney essence. One of the reasons why men suffer from ED problems is because of weakening kidneys. One of the phyto-chemicals of Achyrantes is beta-sitosterol. Researches by scientists have discovered that beta-sitosterol reduces blood levels of cholesterol, and is sometimes used in treating hypercholesterolemia (high level of cholesterol in the blood. It is a well known fact high cholesterol can cause ED problems. Beta-sitosterol also prevents the oxidation of LDL cholesterol thereby reducing the risk of atherosclerosis.

a) TCM believes that kidneys control bone growth. For bone to grow, the body needs bone marrow. In TCM bone marrow is derived from kidney essence. That explains why those who suffers from osteoporosis also suffers from dysfunction kidneys. In recent years, many bone disorders have been successfully treated by TCM practitioners through treatment of the kidney. Bioassay-directed fractionation of a butanol-soluble fraction of methanol extract of the root of Achyranthes bidentata resulted in the isolation of 5 new oleanolic acid glycosides 1-5, namely, 18-(beta-D-glucopyranosyloxy)-28-oxoolean-12-en-3beta-yl 3-O-(beta-D-glucopyranosyl)-beta-D-glucopyranosiduronic acid methyl ester (1), achyranthoside C dimethyl ester (2), achyranthoside C butyl dimethyl ester (3), achyranthoside E dimethyl ester (4), and achyranthoside E butyl methyl ester (5), together with 10 known compounds. Their structures were established on the basis of spectroscopic interpretation and chemical methods. All the oleanolic acid glycosides inhibited the formation of osteoclast-like multinucleated cells (OCLs) induced by 1alpha,25(OH)2D3 in a co-culture assay system. (An osteoclast (from the Greek words for "bone" and "broken") is a type of bone cell that removes bone tissue by removing the bone's mineralized matrix. This process is known as bone resorption. Osteoclasts and osteoblasts are instrumental in controlling the amount of bone tissue. Osteoblasts form bone; osteoclasts resorb bone. Osteoclasts are formed by the fusion of cells of the monocyte cell line. Osteoclasts are characterized by high expression of tartrate resistant acid phosphatase (TRAP) and cathepsin K.). "Five new oleanolic acid glycosides from Achyranthes Bidentata with inhibitory activity on osteoclast formation." 76739

b) Eight compounds were separated from the roots of Achyrathes bidentata by repeated chromatography. On the basis of physicochemical properties and spectral analysis their structures were elucidated as alpha-spinasterol (1), beta-sitosterol (2), chrysophanol (3), dibutyl phthalate (4), palmitic acid (5), alpha-spinasterol-3-O-beta-D-glucoside (6), daucosterol (7) and ecdysterone (8). Compounds 1-7 were isolated from the plant for the first time. “Separation and identification of the compounds from Achyranthes bidentata Bl” 38963

c) Beta-sitosterol (BS) is a compound that has shown various activities potentially useful for human health. In the present study, we determined its antigenotoxic capacity and lymphocyte induction potential in mouse as well as its capacity to trap free radicals in vitro. BS, in doses from 200 to 1,000 mg/kg, was able to significantly reduce the frequency of sister chromatid exchanges induced by 10 mg/kg of doxorubicin (DX) in bone marrow cells. The same range of BS doses also gave rise to a strong reduction in the rate of micronucleated, polychromatic erythrocytes induced by DX. In addition, we determined an increase in the production of lymphocytes in mice administered with BS. By means of the DPPH assay, the compound was shown to trap free radicals in a concentration dependent manner as high as 78.12% using 250 μg/ml. Our research established three relevant biological activities of BS which show its potential as a chemopreventive (The use of chemical agents, drugs, or food supplements to prevent disease) agent. “Cell protection induced by beta-sitosterol: inhibition of genotoxic damage, stimulation of lymphocyte production, and determination of its antioxidant capacity”.  02773

d)   Research by scientists showed that beta-sitosterol decreases cholesterol synthesis.  CaCo-2 cells were used to address the effect of the plant sterol, beta-sitosterol, on cholesterol trafficking, cholesterol metabolism, and apoB secretion.  Compared to cells incubated with micelles (5mM taurocholate and 250 microM oleic acid) containing cholesterol, which caused an increase in the influx of plasma membrane cholesterol to the endoplasmic reticulum and increased the secretion of cholesteryl esters derived from the plasma membrane, beta-sitosterol did not alter cholesterol trafficking or cholesteryl ester secretion. Including beta-sitosterol in the micelle together with cholesterol attentuated the influx of plasma membrane cholesterol and prevented the secretion of cholesteryl esters derived from the plasma membrane. Stigmasterol and campesterol had effects similar to beta-sitosterol although campesterol did not promote a modest influx of plasma membrane cholesterol. Including beta-sitosterol in the micelle with cholesterol  decreased the uptake of cholesterol.Compared to cholesterol, 60% less beta-sitosterol was taken up by CaCo-2 cells.  No observable esterification of beta-sitosterol was appreciated and the transport of the plant sterol to the basolateral medium was negligible. Cholesterol synthesis and HMG-CoA reductase activities were decreased in cells incubated with beta-sitosterol. This was associated with a decrease in reductase mass and mRNA levels. Cholesteryl ester synthesis and ACAT activities were unaltered by beta-sitosterol. Both stigmasterol and campesterol decreased reductase activity, but only campesterol increased ACAT activity. Beta-sitosterol did not affect the secretion of apoB mass. The results suggest that beta-sitosterol does not promote cholesterol trafficking from the plasma membrane to the endoplasmic reticulum. Beta-sitosterol interferes with the uptake of micellar cholesterol causing less plasma membrane cholesterol to influx and less cholesteryl ester to be secreted. Despite its lack of effect on cholesterol trafficking, beta-sitosterol decreases cholesterol synthesis at the level of HMG-CoA reductase gene expression.  "Effect of micellar beta-sitosterol on cholesterol metabolism in CaCo-2 cells." 348360

e) Some of the researches done on the relationship between beta-sitosterol and cholesterol:

i) At McGill University in Montreal (Can. J. Physiol. Pharmacol. 75, 1997, p. 217-27) doctors did a review of the literature on beta-sitosterol and cholesterol metabolism. They researched in detail 18 major studies that used sitosterols to lower cholesterol and triglycerides. They concluded, "addition to diet of phytosterols represents an effective means of improving circulating lipid profiles to reduce risk of coronary heart disease." This study came complete with forty high quality references and left no doubt about the effectiveness of phytosterols on humans. Also at McGill University (Metabolism Clinic Experiments 47, 1998, p. 751-6) patients on a fixed diet were given sterols from pine oil for a mere ten days in a strict, randomized crossover study. This was not a low fat or low cholesterol diet at all. They successfully lowered both their total cholesterol and LDL levels in this short term placebo controlled experiment. They concluded, these results demonstrate the short term efficacy of pine oil plant sterols as cholesterol lowering agents"

ii) A very interesting study was done at the Center for Human Nutrition in France (Ann. Nutr. Metab. 39, 1995, p. 291-5) in that healthy people with normal cholesterol levels were given beta- sitosterol to see if their normal levels could be lowered even further. We always think of studies as using unhealthy people with pathological cholesterol levels given supplements to make them normal again. Amazingly enough the healthy people lowered their normal cholesterol levels even more with no change in diet or exercise. In fact, they were a full 10% lower in only a month. This kind of effect is really fascinating. They said, "The present results may be of great interest in the prevention of high cholesterol diet-associated risks, especially in the prevention of cardiovascular diseases. Since beta-sitosterol was so effective for people who didn't even need it, think what it will do for those people who do need to lower their blood lipids. They concluded, "These findings suggest that a significant lowering of plasma total and LDL cholesterol can be effected by a modest dietary intake of soybean phytosterols"

iii) A good study was done at the Wageningen Agricultural Institute in the Netherlands, the same clinic that did so much good research on trans fatty acids (Am. J. Clin. Nutr. 72, 2000, p. 1510-5). They gave men and women a margarine containing plant sterols and got very significant reductions in cholesterol as well as lower LDL levels in only three weeks. Why a clinic would give margarine to people after studying the negative effects of hydrogenated oils is another matter. Again, these were healthy subjects with normal cholesterol levels, yet they still got great benefits very quickly with no change in diet or exercise.

iv) At Uppsala University in Sweden (Eur. Heart J. Supp. 1, 1999, p. S80-S90) the doctors wanted to give the volunteers the phytosterols in conjunction with a cholesterol lowering diet to see the results of a more comprehensive lifestyle program. The results were really impressive in that the men and women lowered total cholesterol a full 15% and LDL cholesterol a full 19% in less than a month. The shows the very dramatic results you can get with just adding some reasonable dietary changes even without any exercise program at all.

v) At the University of British Columbia at their St. Paul's Hospital (American Journal of Medicine 107 (1999) p. 588-94) a very impressive review was done complete with 86 references of using plant sterols to lower total cholesterol and LDL. They said of the recent research, "In 16 recently published human studies that used phytosterols to decrease plasma cholesterol levels in a total of 590 subjects, phytosterol therapy was accompanied by an average 10% decrease in total cholesterol and 13% decrease in LDL cholesterol levels." This is the best review to date and should convince anyone of the effectiveness of sterols over drugs.

vi) At the University of Kagawa in Tokyo two studies were done. The first was done on healthy young men who were given plant sterols for only five days. In this short time their cholesterol levels fell measurably (Joshi Eiyo Daigaku Kiyo 14, 1983, p. 165-72). The second study was done on healthy young women (same journal 15, 1984 p. 11-18) again giving them plant sterols for only five days. "Administration of phytosterol (mainly sitosterol) increased the output of fecal cholesterol." These were all healthy young Japanese people eating a traditional low-fat diet who did not have a cholesterol problem to begin with, yet they received measurable results in only five days.

vii) At the University of California in San Diego men were isolated in a hospital ward and fed 350 mg of cholesterol and then beta-sitosterol supplements (American Journal of Clinical Nutrition 35, 1982, p. 697-700). This resulted in a 42% decrease in cholesterol absorption in the intestines. They said, "Evidently, the judicious addition of beta-sitosterol to meals containing cholesterol rich foods will result in a decrease in cholesterol absorption with a consequent decrease in plasma cholesterol"

viii) The University of Helsinki took a big interest in lowering cholesterol with plant sterol therapy back in 1988. The first study (Clinical Chimica Acta 178, p. 41-9) studied familial (genetic) hypercholesteremia. The higher the sterol levels they found in the patients blood the more cholesterol was excreted rather than absorbed. The second study was in 1989 (Metabolism Clinical Experiments 38, p. 136-40). Men were studied again for blood levels of sterols and they found the higher the levels the more cholesterol was excreted successfully. The third study in 1994 (American Journal of Clinical Nutrition 59, p. 1338-46) studied vegetarians who eat twice as many plant sterols as normal people. They showed one reason vegetarians have lower cholesterol levels besides the food they eat is the efficiency of their cholesterol excretion due to their intakes of plant sterols. In the last study in 1999 (Current Opinion Lipidology 10, p. 9-14) they said, "Plant sterols may be useful for the treatment of hyper-cholesteremiaフhey may have a potent cholesterol lowering effect as shown in normal and hypercholesteremic men and women with and without coronary heart disease and diabetes mellitus"

ix) The best study of all was a review from the University of British Columbia (American Journal of Medicine 107, 1999, p. 588-94). This included a full 86 references, and went over seventeen different human studies using plant sterols to lower cholesterol since 1951 (Proceedings of the Society for Biological Medicine 78, 1951, p. 143-7). A total of 590 men and women were used in these studies with phytosterol therapy resulting in an average 10% reduction in total cholesterol and a 13% reduction in LDL cholesterol. They found this worked best in high-fat diets; the worse the diet the more results the researchers got.

3) Radix Rehmannia Glutinosa

Function of the herb:

• It is used to nourish the vital essence

• It is an effective blood tonic

The Chinese have a famous riddle "I have visited a new place and returned to an old place simultaneously, what herb am I?" Glutious Rehmannia in its raw form is called "new place" and processed Rehmannia is called "old place" (in their Chinese character). Processed Rehmannia is derived from raw Rehmannia by steaming it for ten times and drying in the sun nine times. The functions (clinical usage) of raw and processed Rehmannia are totally different altogether. One herb plus steam and sun gives you two different herbs. That is the magical wonder of herbal science. This knowledge has to be passed down from generation to generation. It cannot be done using laboratory research. It is something that allopathic science cannot explain.

Research by scientists showed that Rehmannia improves blood movement. Effects of 50% ethanolic extract (JR-ext) from Chinese Rehmanniae Radix (the steamed and dried root of Rehmannia glutinosa, "Jyuku-Jio" in Japanese) on the hemorheology of inflammatory, thrombosic and intact animals were examined in the in vivo models. JR-ext (200 mg/kg, p.o.) inhibited the reduction of fibrinolytic activity and erythrocyte deformability, the decrease in erythrocyte counts and the increase in connective tissue of the thoracic artery in a chronic inflammatory model, adjuvant-induced arthritis. However, JR-ext was ineffective on the development of edema in the arthritic rats and on acute and chronic inflammation. JR-ext inhibited the reduction of erythrocyte deformability, but not the decrease of coagulative factors in a thrombosic model, endotoxin-induced disseminated intravascular coagulation (DIC). JR-ext also showed a promoting effect on erythrocyte deformability and fibrinolytic activity in intact rats. These results suggest that orally administered JR-ext can prevent an inducement of impediment in the peripheral microcirculation of various chronic diseases through the improvement of hemorheology (blood movement). “Studies on rehmanniae radix. I. Effect of 50% ethanolic extract from steamed and dried rehmanniae radix on hemorheology in arthritic and thrombosic rats.” 841954

4) Fructus Cornus Officinalis

 Function of the herb:

• It is used to replenish the vital essence of the liver and kidneys

In our previous study, we reported the renoprotective effect of Corni Fructus (Cornus officinalis SIEB. et ZUCC. In this study, we investigated the effects of morroniside isolated from Corni Fructus on renal damage in streptozotocin-treated diabetic rats. Oral administration of morroniside at a dose of 20 or 100 mg/kg body weight/d for 20 d to diabetic rats resulted in significant decreases in increasing serum glucose and urinary protein levels. Moreover, the decreased levels of serum albumin and total protein in diabetic rats were significantly increased by morroniside administration at a dose of 100 mg/kg body weight/d. In addition, morroniside significantly reduced the elevated serum urea nitrogen level and showed a tendency to reduce creatinine clearance. Morroniside also significantly reduced the enhanced levels of serum glycosylated protein, and serum and renal thiobarbituric acid-reactive substances. Protein expressions related to the advanced glycation endproduct (AGE) level and actions, oxidative stress such as N(epsilon)-(carboxyethyl)lysine, as well as receptors for AGE and heme oxygenase-1 were increased in diabetic rats, but the levels were also significantly decreased by the administration of morroniside. This suggests that morroniside exhibits protective effects against diabetic renal damage by inhibiting hyperglycemia and oxidative stress. These results indicate that morroniside is one component partly responsible for the protective effects of Corni Fructus and Hachimi-jio-gan against diabetic renal damage. “Protective Effects of Morroniside Isolated from Corni Fructus against Renal Damage in Streptozotocin-Induced Diabetic Rats.” 591786

5) Rhizoma Ligusticum Chuanxiong

Function of the herb:

• It is used to invigorate blood circulation and promote the flow of vital energy

a) Ligustilide is the most abundant bioactive ingredient in Rhizoma Chuanxiong, a Chinese medicinal herb commonly used for the treatment of cardiovascular ailments. The present study reported, for the first time, the pharmacokinetics of ligustilide, administered in its pure form and in an herbal extract, in rats. After i.v. administration of pure ligustilide, it was distributed extensively (V_d, 3.76 ± 1.23 l/kg) and eliminated rapidly (t_1/2, 0.31 ± 0.12 h). The i.v. clearance (CL) of ligustilide after Chuanxiong extract administration was significantly higher than that dosed in its pure form [CL, 20.35 ± 3.05 versus 9.14 ± 1.27 l/h/kg, p < 0.01; area under the curve (AUC), 0.79 ± 0.10 versus 1.81 ± 0.24 mg · h/l, p < 0.01], suggesting significant interaction between ligustilide and components present in the extract. Dose-dependent pharmacokinetics was observed after i.p. administration, and a significantly higher dose-normalized AUC (1.77 ± 0.23 mg · h/l) at 52 mg/kg was obtained than that at 26 mg/kg (0.93 ± 0.07 mg · h/l, p < 0.05). Oral bioavailability of ligustilide was low (2.6%), which was partly because of extensive first-pass metabolism in the liver. Seven metabolites of ligustilide were identified, and three of them were unequivocally characterized as butylidenephthalide, senkyunolide I, and senkyunolide H. These three compounds also occurred naturally in the herb and were reported to be bioactive. “Pharmacokinetics and Metabolism of Ligustilide, a Major Bioactive Component in Rhizoma Chuanxiong, in the Rat.” 017707

b) The purpose of the present study was to investigate the effect of ligustilide on vasodilatation in rat mesenteric artery and the mechanisms responsible for it. Isometric tension of rat mesenteric artery rings was recorded by a sensitive myograph system in vitro. The results showed that ligustilide at concentrations more than 10 μM relaxed potassium chloride (KCl)-preconstricted rat mesenteric artery in a concentration-dependent manner. The vasodilatation effect of ligustilide was not dependent on endothelium. Ligustilide rightwards shifted concentration-response curves induced by KCl, calcium chloride (CaCl₂), noradrenaline (NA) or 5-hydroxytryptamine (5-HT) in a non-parallel manner. This suggests that the vasodilatation effects were most likely via voltage-dependent calcium channel (VDCC) and receptor-operated calcium channel (ROCC). Propranolol, glibenclamide, tetraethylammonium and barium chloride did not affect the vasodilation induced by ligustilide, showing that p-adrenoceptor, ATP sensitive potassium channel, calcium-activated potassium channel and inwardly rectifying potassium channel were not involved in the vasodilatation. Ligustilide concentration-dependently inhibited the vasoconstriction induced by NA or CaCl₂ in Ca²⁺-free medium, indicating that the vasodilatation relates to inhibition of extracellular Ca²⁺ influx through VDCC and ROCC, and intracellular Ca²⁺ release from Ca²⁺ store. Since caffeine-induced contraction was inhibited by ligustilide, inhibition of intracellular Ca²⁺ released by ligustilide occurred via the ryanodine receptors. Our results suggest that ligustilide (from Rhizoma Ligusticum Chuanxiong) induces vasodilatation in rat mesenteric artery by inhibiting the VDCC and ROCC, and receptor-mediated Ca²⁺ influx and release. “Ligustilide induces vasodilatation (relaxes the smooth muscle in blood vessels, a key factor for erection to take place: this is how Viagra works) via inhibiting voltage dependent calcium channel and receptor-mediated Ca²⁺ influx and release.” 171176

c) Tetramethylpyrazine (TMP) and salvianolic acid B (SAB) are effective ingredients of Rhizoma Ligustici chuanxiong Hort. and Radix Salviae miltiorrhizae Bge., accordingly. The inhibitive effects of TMP, SAB and their combination on shear-induced platelet aggregation (SIPA) were investigated in the present study. SD rats were used as blood donors to collect anticoagulated blood, the concentration of platelet-rich-plasma (PRP) was adjusted to 5×10⁵ μl. HAAKE rheometer RS 600 with sensor C60/0.5° was used as shear generator. Different doses of TMP and SAB and their combinations were added to the PRP. After constant shear of 15 Pa at 37°C for 360 seconds, PRP was transferred to a platelet aggregometer and SIPA was determined by turbidity. SIPA was inhibited by TMP and SAB in a dose-dependent manner. SIPA was decreased from 48.6±4.6% of the control to 12.5±2.1% in the presence of TMP (1.46 mM) and SAB (10 μM) (P<0.0001). In conclusion, TMP and SAB have additive effects on inhibiting platelet aggregation induced by high shear stress. “Inhibition of shear-induced platelet aggregation in rat by tetramethylpyrazine and salvianolic acid B, active component of Rhizoma Ligustici Chuanxiong”.  97103

6) Radix Dipsacus Asper

Function of the herb

• It is used to replenish and tonifys the liver and kidneys

The methanol extract from Dipsacus asper Wall (Dipsacaceae) was found to show antioxidant activity against free radical and Cu(2+)-mediated LDL oxidation. In further study, to identify active constituents from the plant, six caffeoyl quinic acid derivatives: 3,4-di-O-caffeoylquinic acid (1), methyl 3,4-di-O-caffeoyl quinate (2), 3,5-di-O-caffeoylquinic acid (3), methyl 3,5-di-O-caffeoyl quinate (4), 4,5-di-O-caffeoylquinic acid (5) and methyl 4,5-di-O-caffeoyl quinate (6) were isolated. Their structures were identified by spectroscopic methods including 2D-NMR. The isolated compounds, 1-6, were found to be potent scavengers of the free radical 1,1-diphenyl-2-picrylhydrazyl (DPPH), and are more potent than butylated hydroxyl toluene (BHT) used as a positive control. The compounds 1-6 also inhibited Cu(2+)-mediated low-density lipoprotein (LDL) oxidation. They increased the lag time of conjugated dienes formation and inhibited the generation of thiobarbituric acid reactive substances (TBARS) in a dose-dependent manner. These results suggested that Dipsacus asper due to its antioxidant constituents, 1-6, may have a role to play in preventing the development and progression of atherosclerotic disease. “The antioxidant activity of caffeoyl quinic acid from the roots of Dipsacus asper.” 809011

7) Radix Paeonia Lactiflora

Function of the herb:

•  It is used to nourish the blood

a) Paeonia lactiflora and Astragalus membranaceus are two popular traditional Chinese medicines, commonly used in Chinese herb prescription to treat liver disease. The extract prepared from the roots of Paeonia lactiflora and Astragalus membranaceus (PAE) demonstrated more excellent hepato-protective activity than the single herbs used individually as indicated in our preliminary studies. The present study was carried out to investigate the effects of PAE on liver fibrosis in rats induced by carbon tetrachloride (CCl₄) and to explore its possible mechanisms. Liver fibrosis was induced in male Sprague–Dawley rats by injection with 50% CCl₄ subcutaneously twice a week for 8 weeks. At the same time, PAE (40, 80 and 160 mg/kg) was administered intragastrically. Upon pathological examination, the PAE-treated rats significantly reduced the liver damage and the symptoms of liver fibrosis. Administration of PAE decreased CCl₄-induced elevation of serum transaminase activities, hyaluronic acid, laminin and procollagen type III levels, and contents of hydroxyproline in liver tissue by approximately 30–60%. It also restored the decrease in SOD and GSH-Px activites and inhibited the formation of lipid peroxidative products during CCl₄ treatment. Moreover, PAE (80, 160 mg/kg, ig) decreased the elevation of TGF-β1 by 47.7% and 53.1%, respectively. In the primary cultured hepatic stellate cells (HSCs), PAE also significantly decreased [³H] thymidine incorporation in cells stimulated with platelet-derived growth factor-B subunit homodimer (PDGF-BB) and suppressed [³H] proline incorporation. These results suggested that PAE significantly inhibited the progression of hepatic fibrosis induced by CCl₄, and the inhibitory effect of PAE on hepatic fibrosis might be associated with its ability to scavenge free radicals, decrease the level of TGF-β1 and inhibit collagen synthesis and proliferation in HSCs. “Effects and mechanisms of extract from Paeonia lactiflora and Astragalus membranaceus on liver fibrosis induced by carbon tetrachloride in rat.”   514523

b) This study examined the effect of Paeoniae Radix (PR) on endothelial function and the activity of superoxide dismutase (SOD) of erythrocytes in rats administered a high-fat diet. Administration of the extract of PR increased the endothelium-dependent relaxation and the activities of SOD compared with high the cholesterol diet group significantly. Hypercholesterolaemia induced an increase of endothelial superoxide anion and endothelial dysfunction. Paeoniae Radix is suggested to have a protective effect on endothelial cells and their function. “Effect of extract prepared from the roots of Paeonia lactiflora on endothelium-dependent relaxation and antioxidant enzyme activity in rats administered high-fat diet.” 479767

(The endothelium is the thin layer of cells that line the interior surface of blood vessels. Endothelial cells line the entire circulatory system, from the heart to the smallest capillary. These cells reduce turbulence of the flow of blood allowing the fluid to be pumped farther.)

c) Paeoniae Radix is a crude drug that is used in Asia and Europe to improve blood flow. We studied its vasodilator effect and mechanisms of action in vitro. The extract from Paeoniae Radix (PRE) relaxed prostaglandin F2a-precontracted aortic ring preparations of isolated rat aorta that contained endothelium. Relaxation by PRE did not occur in specimens without endothelium, and was inhibited by pretreatment with 10^-4 M N^G-nitro-1-arginine methyl ester. Paeoniflorin and paeonol, the main active components of Paeoniae Radix, lacked a vasodilator effect. The effect of the component gallotannin was examined after treating PRE with tannase, but the product lacked a vasodilator effect. Pentagalloylglucose, hexagalloylglucose, heptagalloylglucose, and octagalloylglucose were extracted from PRE ; they relaxed aortic rings with endothelium, but failed to relax aortic rings without endothelium. We conclude that PRE exhibits an endothelium-dependent vasodilator effect on isolated rat aorta. “Endothelium-dependent vasodilator effect of extract prepared from the roots of Paeonia lactiflora on isolated rat aorta.” 436439

d) Research showed that the herb:

1)   Lower cholesterol levels. “Zhang Y. The effects of nifedipine, diltiazem, and Paeonia lactiflora Pall. on atherogenesis in rabbits. Chung Hua Hsin Hsueh Kuan Ping Tsa Chih 1991;19:100–3”

2)   Improve liver function  and help prevent liver damage from chemical toxins such as carbon tetrachloride. “Qi XG. Protective mechanism of Salvia miltiorrhiza and Paeonia lactiflora for experimental liver damage. Chung Hsi I Chieh Ho Tsa Chih 1991;11:69, 102–4”

3)   Inhibit blood platelet aggregation. “Liu J. Effect of Paeonia obovata 801 on metabolism of thromboxane B2 and arachidonic acid and on platelet aggregation in patients with coronary heart disease and cerebral thrombosis. Chung Hua I Hsueh Tsa Chih (Chin Med J) 1983;63:477–81.”

e) Clinical research by western scientists confirmed the validity of the historical use of the drug, Radix Paeonia Lactiflora for improving liver functions by preventing liver damage and micro-circulation disorders. "Acute liver damage from D-galactosamine was initiated in rats that were then treated with Paeonia lactiflora and Salvia miltiorrhiza. Parameters measured in this study were changes in ALT, bilirubin, levels of plasma fibronectin and pathological histology. The results showed that both herbs increased plasma fibronectin and improved the reticuloendothelial system function. Aggregation of albumin, collagen fragments and immune complexes were markedly reduced. Liver immune damage and micro-circulation disorders were avoided, justifying the important role of Paeonia lactiflora and Salvia miltiorrhiza in protecting hepatocytes". 102-41991