Sichuan Lovage (Ligusticum chuanxiong Hort.): A Comprehensive Reference
1. Identity and Botanical Description
1.1 Botanical and Scientific Names
Sichuan lovage rhizome (Chuanxiong in Chinese transliteration) is derived from the dried rhizome of Ligusticum chuanxiong Hort. (family: Apiaceae) and has a long history of medicinal uses. The plant is also referenced under several synonymous or historically used scientific designations, including Ligusticum wallichii Franch. and, in newer taxonomic nomenclature, Conioselinum anthriscoides "Chuanxiong." Despite older sources assigning "chuanxiong" as a synonym of L. striatum = L. wallichii, morphological, karyotypic, and DNA barcode evidence all point to "chuanxiong" being a cultivated form of L. sinense.
In Chinese, the herb is written 川芎 (Chuān Xiōng), meaning "Sichuan lovage." Chuanxiong Rhizoma (CX) is the dried root rhizomes of the plant Ligusticum chuanxiong Hort. of the family Umbelliferae. Other common designations include Rhizoma Chuanxiong, Rhizoma Ligustici Chuanxiong, Szechwan Lovage Rhizome, and Chuanxiong Rhizoma.
1.2 Plant Morphology
Ligusticum chuanxiong Hort. is a perennial herbaceous plant in the Apiaceae (Umbelliferae) family, growing 40–70 cm tall. The stems are upright, cylindrical, and hollow, with conspicuous swollen nodes. It is a perennial plant with hermaphrodite flowers that are pollinated by insects. Authentic Sichuan Chuan Xiong can be distinguished by its fist-like knotted shape with prominent node rings, strong characteristic aroma, and the distinctive wavy cambium ring on cross-section.
1.3 Geographic Origin and Cultivation
L. chuanxiong, the dried rhizome of Ligusticum chuanxiong Hort (family Umbelliferae), is mainly cultivated in Sichuan Province, China, and was first recorded in "Shen Nong's Canon of Materia Medica." Ancient medical practitioners discovered that the therapeutic efficacy of SLR cultivated in Sichuan Province in China was better than that of SLR cultivated in other areas; Sichuan therefore became a genuine cultivating area for SLR. It is widely cultivated in China, Korea, and Japan, and the young leaves of this plant are eaten as vegetables and the rhizomes and roots are known to expand blood vessels and activate blood circulation in traditional Asian medicine.
1.4 Pharmacopeial Status
CX is documented in the Chinese Pharmacopoeia from 1963 to 2020 editions. The 2020 edition of the Chinese Pharmacopoeia lists 245 Chinese patent medicines containing CX, which accounts for 16.8% of the listed Chinese patent medicines. CX is also one of the Chinese herbal medicines with a relatively long history of export in China, and has been widely exported to many countries and regions, and has been listed in the pharmacopoeias of Japan, South Korea, Thailand, Brazil, and even European countries. It has significant clinical efficacy in relation to human diseases of the cardiocerebrovascular system, nervous system, respiratory system, digestive system, urinary system, etc. Apart from China, SLR is also used in Singapore, Malaysia, the European Union, and the United States of America.
1.5 Related Species and Substitutes
Japanese Cnidium officinale (known as "Japanese Chuan Xiong" or 日本川芎) is used in Japanese Kampo medicine but differs in chemical profile. Because there is no chuanxiong plant in Japan, local Kampo practitioners substitute it with Conioselinum officinale (Makino) K.Ohashi & H.Ohashi (= L. officinale Makino). Gao Ben (藁本, Ligusticum sinense or L. jeholense) is a related species in the same genus that enters the Bladder channel and primarily treats vertex headache, and is sometimes mistakenly sold as Chuan Xiong. Chuanxiong is considered more valuable than gaoben, and adulteration using gaoben is not uncommon.
1.6 Common Preparations and Dosage Forms
When Chinese proprietary medicines are applied to the clinical treatment of diseases, they can be made into various dosage forms according to their physical and chemical properties and clinical needs, such as decoctions, pills, powders, tablets, granules, plasters, solutions, syrups, tinctures. Nine dosage forms have been reported in the literature, including powders, pills, concentrated pills, drip pills, tablets, granules, bagged tea, oral liquid, and soft capsules.
Various dosage forms of this herb and herb pairs on the market such as capsules, pellets, oral decoctions, and granules are mainly indicated for a blood stasis type of headache. The root and rhizomes are used for herbal remedies. In addition to its medicinal uses, Ligusticum can be combined with certain foods and beverages as a flavor component, and to add fragrance to some soaps and cosmetics.
2. Traditional and Historical Use
2.1 Earliest Historical Records
The earliest name for SLR was "Xiongqiong," recorded in The Classic of Mountains and Seas compiled in China during the Pre-Qin Dynasty (estimated from 476 BC to 221 BC), which stated that "the grasses were many peonies and Xiongqiong." In Shennong's Herbal Classic, compiled during the Eastern Han Dynasty (more than 2,000 years ago), SLR was recorded under the name of "Xiongqiong," which was classified into the top-grade herb category.
CX is listed as a superior herb in the book "Shennong Bencao Jing." It has a pungent and warm nature and belongs to the liver, gallbladder, and pericardium meridians.
2.2 Traditional Chinese Medicine (TCM) Framework
L. chuanxiong promotes blood circulation, circulates "Qi," dispels wind, and relieves pain, and it is commonly used for the treatment of gynecological pain, cardiovascular diseases, and cerebrovascular diseases clinically. Nicknamed the "Qi herb within the Blood," it uniquely combines the ability to move both blood and Qi, making it a cornerstone of many classical formulas for women's health and pain management. It has been used for over two thousand years and remains one of the most commonly prescribed herbs in modern clinical practice.
In TCM theory, CX facilitates blood circulation (活血通络 huo xue tong luo), dispels wind-cold (祛风散寒 qu feng san han), and exhibits properties such as invigorating blood (活血 huo xue), promoting qi flow (行气 xing qi), expelling wind (祛风 qu feng), and alleviating pain (止痛 zhi tong).
The rhizome is warm in property and pungent in flavor, with functions of promoting the circulation of the blood and Qi, expelling wind, and alleviating pain. Therefore, L. chuanxiong has long been used as a traditional Chinese medicine for the treatment of headache, rheumatic arthralgia, menstrual disorders, swelling pain due to traumatic injury, and coronary heart diseases.
2.3 Traditional Uses by Condition
In China, LCH is often used to treat gynecological diseases, such as dysmenorrhea, amenorrhea, dystocia, and lochia, and it is also applied to treat ischemic diseases, such as dizziness, headache, and migraine. CX can be used alone or in combination with other Chinese botanical drugs to treat various conditions, including stroke, angina pectoris, bruises, swelling, and menstrual irregularities.
CX and Cyperi Rhizoma (Xiangfu) have been used alone or in combination to treat migraine dating back to the Eastern Jin Dynasty (AD 317) of China. CX was first documented for migraine in the treatise of Handbook of Prescriptions for Emergencies published in the Eastern Jin Dynasty (AD 317 CE) of China.
The herb pair of CX with Gastrodiae Rhizoma, first recorded in "Xuan Ming Lun Fang" in the Jin Dynasty, has been widely used to promote blood circulation, balance the liver and extinguish wind, eliminate pathogens, and dredge the collaterals to stop pain with thousands of years' clinical experience.
2.4 Classical Formula Contexts
Warm, acrid, and entering the Liver, Gallbladder, and Pericardium channels, it simultaneously moves Blood and Qi to relieve pain across the head, chest, abdomen, and limbs — classically prescribed in Chuan Xiong Cha Tiao San for Wind headaches, Xue Fu Zhu Yu Tang for chest pain and Blood stasis, and the Si Wu Tang family for irregular menstruation.
CX is an important component of various Chinese patent medicine formulations, including Chuanxiong Cha Pills, Weichang An Pills, and Xuebijing Injection. The "Suxiao Jiuxin pills," with CX as one of the main ingredients, occupies a pivotal position in the market of cardio-cerebral and cerebrovascular medicines.
2.5 Use in Japanese and Korean Medicine
It has been used in Japanese, Korean, and other traditional medicine for over 2,000 years. In traditional Asian medicine, Ligusticum chuanxiong Hort. is mainly used for improving blood circulation or for analgesic and anti-inflammatory purposes, but it also has a long history of use for pain disorders in the head and face, such as headache. Ligusticum is considered one of the 50 fundamental herbs in Traditional Chinese Medicine.
3. Key Constituents and Active Compounds
3.1 Major Chemical Classes
To date, more than 263 bioactive substances have been isolated from different parts of LCH (rhizomes, fibrous roots, and aboveground parts), including volatile oils, organic acids, phenolic acids, phthalates, alkaloids, polysaccharides, ceramides, cerebrosides, and terpenoids.
Over 100 metabolites have been isolated and identified from CX, classified into nine major classes. Key bioactive compounds include senkyunolide A, ligustilide, tetramethylpyrazine (TMP), and ligusticum CX polysaccharides (LCP).
3.2 Phthalides (Lactones)
The main constituents of CR include phthalides and phenolic acids. Phthalides include Z-ligustilide, senkyunolide A, senkyunolide I, senkyunolide H, and butylphthalide.
Z-ligustilide is the most abundant and pharmacologically prominent phthalide. The effects of Z-ligustilide are vasodilatation and neuroprotection. Pharmacokinetic studies have shown that Z-ligustilide has poor oral bioavailability in rats due to severe first-pass metabolic reactions. New evidence suggests that Z-ligustilide has a wide range of pharmacological properties, including anticancer, anti-inflammatory, anti-oxidant, as well as neuroprotective activities. Z-ligustilide, a major component of CR, can significantly decrease the infarct volume and mitigate neurological dysfunction in rats with middle cerebral artery occlusion (MCAO).
Senkyunolides: Senkyunolide A, senkyunolide I, and senkyunolide H can inhibit the formation of thrombi, increase cerebral blood flow, and reduce cerebral vascular resistance.
Among compounds absorbed into rat plasma after oral administration of Rhizoma Chuanxiong decoction, 13 compounds were absorbed into rat plasma in prototype and identified as ferulic acid, senkyunolide J, senkyunolide I, senkyunolide D, senkyunolide F, senkyunolide M, senkyunolide Q, senkyunolide A, E-butylidenephthalide, E-ligustilide, neocnidilide, Z-ligustilide, and levistolide A.
3.3 Alkaloids — Tetramethylpyrazine (TMP / Ligustrazine)
Tetramethylpyrazine (TMP) is one of the main active ingredients extracted from the Chinese herbal medicine Ligusticum striatum DC. (Chuan Xiong). Many in vivo and in vitro studies have demonstrated that TMP has a certain role in the treatment of CNS diseases through inhibiting calcium ion overload and glutamate excitotoxicity, anti-oxidative/nitrification stress, mitigating inflammatory response, anti-apoptosis, protecting the integrity of the blood-brain barrier (BBB), and facilitating synaptic plasticity.
Tetramethylpyrazine (ligustrazine, TMP) is a natural compound isolated from Chinese herbal medicine Ligusticum wallichii (Chuan Xiong), which has been extensively used for medicinal purposes for more than 2,000 years. TMP was first isolated in 1957 and has been increasingly studied for its action on myocardial and cerebral infarction since the 1970s.
Several studies have shown that TMP can exhibit multiple biopharmacological activities such as inhibition of platelet aggregation, oxidative stress, inflammation, apoptosis, and so forth.
3.4 Phenolic Acids — Ferulic Acid
Ferulic acid has shown antioxidant properties through its interaction with 1,1-diphenyl-2-picryl-hydrazyl radical, acting as a key antioxidant metabolite in CX. Due to its abundance, ferulic acid is frequently used as a quality control marker for CX. According to the 2020 edition of the Chinese Pharmacopoeia, the ferulic acid content in dried CX should not be less than 0.01%.
The organic acids of chuanxiong rhizome include ferulic acid, sedanonic acid, folic acid, vanillic acid, caffeic acid, and protocatechuic acid.
3.5 Volatile Oil Fraction
The active components in Sichuan lovage rhizome include volatile oils, alkaloids, and organic acids. The volatile oils include ligustilide, sabinene, limonene, and senkyunolide A–S; the alkaloids include tetramethylpyrazine, perlolyrine, wallichilide, 3-butylidene-7-hydroxyphthalide, and (3S)-3-butyl-4-hydroxyphthalide.
3.6 Other Alkaloids and Polysaccharides
Alkaloids are among the most important metabolites of CX; only a limited number of alkaloids have been isolated from CX, including organic amines, pyrazines, pyrimidines, purines, pyridines, carbolines, and scopolamine types. Ligusticum CX polysaccharides (LCP) have also been identified as pharmacologically relevant, contributing to the herb's immunomodulatory and antioxidant profile.
4. Established Mechanisms of Action
4.1 Antiplatelet and Anticoagulant Activity
CX demonstrates significant pharmacological effects in treating cardio-cerebrovascular diseases (CCVDs), such as atherosclerosis, myocardial and cerebral ischemia-reperfusion injury, and hypertension. Its therapeutic mechanisms include antiplatelet activity, endothelial cell protection, anti-inflammatory, antioxidant, and anti-apoptotic properties.
Research confirms potent anti-platelet aggregation effects, cerebrovascular and coronary vasodilatory activity, anti-inflammatory properties, analgesic effects, and neuroprotective actions. Ligustilide is the principal smooth muscle relaxant responsible for its effects on blood vessels and the uterus.
4.2 Vasodilation and Cardiovascular Mechanisms
Chuanxiong has been long used in China to treat cardiovascular diseases (CVDs) including coronary heart disease, hypertension, arrhythmia, heart failure, dilated cardiomyopathy, dyslipidemia, and myocarditis. The benefits of Chuanxiong are attributed to its vasodilating, anti-inflammatory, anticoagulant, free radical-scavenging, and microcirculatory effects.
Tetramethylpyrazine (TMP), a pharmacologically active component isolated from the rhizome of Rhizoma Chuanxiong, has been clinically used in China and Southeast Asian countries for the prevention and treatment of cardiovascular diseases (CVDs) for about fifty years. The pharmacological effects of TMP on the cardiovascular system have attracted great interest. Emerging experimental studies and clinical trials have demonstrated that TMP prevents atherosclerosis as well as ischemia-reperfusion injury. The cardioprotective effects of TMP are mainly related to its antioxidant, anti-inflammatory, or calcium-homeostasis effects.
4.3 Neuroprotective Mechanisms
TMP treats CNS diseases through inhibiting calcium ion overload and glutamate excitotoxicity, anti-oxidative/nitrification stress, mitigating inflammatory response, anti-apoptosis, protecting the integrity of the blood-brain barrier (BBB), and facilitating synaptic plasticity. TMP exerts roles and mechanisms of action on ischemic cerebrovascular disease, spinal cord injury, Parkinson's disease, Alzheimer's disease, cognitive impairments, migraine, and depression.
Certain active metabolites reverse tau hyperphosphorylation and promote its degradation through the lysosomal pathway, thereby mitigating tau-mediated intracellular transport impairment, axonal and synaptic damage, and neuronal death. The primary active metabolites identified in this process include neocnidilide, ferulic acid, Z-ligustilide, and butylidene phthalide, which have demonstrated neuroprotective effects against Alzheimer's disease (AD).
4.4 Anti-inflammatory Mechanisms
Modern pharmacological studies have shown that LCH has analgesic, anti-inflammatory, antioxidant, antitumor, anti-coagulation, anti-depression, anti-aging, anti-atherosclerosis, and improving cardiac function effects. TMP has been shown to decrease the levels of inflammatory factors including TNF-α, IL-1β, and IL-6 in preclinical studies, according to the Frontiers in Pharmacology 2025 review of CX chemistry and pharmacology.
4.5 Nitric Oxide Pathway
Most studies on CR have focused on the L-arginine–nitric oxide (NO) pathway. CR was evaluated for its effects and mechanisms of action in coronary artery disease (CAD), with NO₃⁻, NO₂⁻, and NO levels examined in the nitrate-nitrite-NO pathway. Nitric oxide (NO) is an important signaling molecule that plays an important role in treating coronary artery disease via the NO pathway, thereby regulating endothelial cell function. NO also plays significant roles in relaxing blood vessels, regulating blood pressure, and maintaining the balance of the intravascular environment.
5. Scientific Evidence by Area of Use
5.1 Cardiovascular Disease
CX demonstrates significant pharmacological effects in treating CCVDs, such as atherosclerosis, myocardial and cerebral ischemia-reperfusion injury, and hypertension. Its therapeutic mechanisms include antiplatelet activity, endothelial cell protection, anti-inflammatory, antioxidant, and anti-apoptotic properties. CX can be administered alone or in combination with other traditional Chinese medicines (TCMs) or chemical drugs, showing efficacy in cardiovascular, nervous system, digestive system disorders, as well as analgesia and anticancer activities.
Researchers have explored pharmacological capabilities of TMP in various diseases, such as coronary heart disease, diabetes, cancers, and liver injury. Laboratory study verified the regulation ability of this agent in multiple molecular targets, such as anti-inflammation, antioxidant, antiplatelet, and anti-apoptosis. The evidence base for isolated TMP in cardiovascular contexts is primarily from experimental and animal studies, with some early clinical investigation. Since most studies are experimental, large-scale clinical trials are required to assess the efficacy of TMP in the treatment of cardiovascular disease.
An older observation using oral administration reported that oral administration of Ligusticum chuanxiong at an equivalent dosage of 30 times to patients for 90 days significantly lowered serum total cholesterol (TC) and triglyceride (TG) levels. However, this represents a single report and cannot be considered strong clinical evidence without replication in well-controlled trials.
DG-CX (the Angelica–Chuanxiong herb pair) is known to significantly reduce serum triglyceride, total cholesterol, and low-density lipoprotein-cholesterol levels, though this evidence derives largely from animal and network-pharmacology research rather than large-scale randomized controlled trials.
5.2 Cerebrovascular Disease and Ischemic Stroke
Chuanxiong Rhizome is the most widely used traditional Chinese medicine for treating stroke. Tetramethylpyrazine, a natural alkaloid extracted from CR, has been used extensively for the treatment of ischemic stroke.
Chuan Xiong is used clinically in China for ischaemic stroke and is one of the primary herbs in cardiovascular formulas. Clinical trials have demonstrated therapeutic potential for ischemic stroke (IS) when used in combination formulas such as Hedysarum multijugum–Chuanxiong rhizoma compound (HCC), a modification of the classical Buyang Huanwu decoction. However, much of the mechanistic evidence for CR in stroke comes from animal models of middle cerebral artery occlusion (MCAO) rather than large, independent randomized clinical trials. Current research mainly focuses on cell and animal experiments, where some active ingredients exhibit diverse pharmacological activities. However, further studies are needed to fully understand its specific mechanisms of action.
A 2024 preclinical study investigated the methanol extract of CR in a mouse model of bilateral carotid artery stenosis and found that despite the possibility that the plant is effective for diseases such as cerebral infarction and vascular dementia (VaD), the mechanism of action is not well understood. The study attempted to determine if the dried rhizomes of L. chuanxiong methanol extract has activity in a VaD mice model. Through network analysis, the study confirmed that CR is effective in cerebrovascular diseases. This remains animal-level evidence.
5.3 Migraine and Headache
Traditional Chinese medicine has been used to treat migraine for more than 2,000 years. CX is the central herb in this tradition: CR has been recorded in "Shen Nong's Herbal Classic" and "Compendium of Materia Medica" and described as "pungent and warm." In the Chinese Pharmacopoeia, CR can be used to promote the flow of qi and blood circulation, wind-expelling, and pain alleviation. It is often used to treat migraine, rheumatism, and irregular menstruation.
In modern medicine, the antimigraine effect of the Da Chuanxiong formula (CR combined with Gastrodiae Rhizoma) has been definitely confirmed. Various dosage forms of this herb pair on the market such as capsules, pellets, oral decoctions, and granules are mainly indicated for a blood stasis type of headache.
Chuanxiong Rhizoma (CR) is employed in traditional Chinese medicine (TCM) to treat various disorders. CR is effective for migraine, but its active compounds, drug targets, and exact molecular mechanism remain unclear. The majority of mechanistic evidence is from network pharmacology analysis, animal models, and systems pharmacology studies; high-quality randomized controlled trials specifically isolating CR (as a single herb) for migraine are lacking in the Western literature.
5.4 Pain and Anti-inflammatory Activity
Modern pharmacological studies have shown that LCH has analgesic, anti-inflammatory, antioxidant, antitumor, anti-coagulation, anti-depression, anti-aging, anti-atherosclerosis, and improving cardiac function effects. A 2024 network pharmacology study (PMC11129751) investigated LCH's potential in neuropathic pain, examining its capacity to regulate microglial M1 polarization. This study was experimental in nature, and human clinical data on CR for neuropathic pain specifically are not yet available in peer-reviewed literature.
5.5 Gynecological Applications (Dysmenorrhea, Irregular Menstruation)
L. chuanxiong is commonly used for the treatment of gynecological pain, cardiovascular diseases, and cerebrovascular diseases clinically. In China, LCH is often used to treat gynecological diseases, such as dysmenorrhea, amenorrhea, dystocia, and lochia. The classical formula Si Wu Tang (Four Substance Decoction), which contains CX as a key ingredient, has been used for centuries in women's health conditions related to blood deficiency and stasis. The evidence for CX specifically in gynecological conditions consists largely of traditional use records and in vitro/animal pharmacological findings; dedicated human clinical trials isolating CX for dysmenorrhea are not robustly represented in the English-language peer-reviewed literature.
5.6 Neurodegenerative Disease (Alzheimer's and Parkinson's)
TMP, a widely used therapeutic agent for ischemia/reperfusion-induced brain injury, has been associated with only two tau-related targets, suggesting limited therapeutic relevance in tau pathology-based Alzheimer's disease (AD). However, compared to the control group, the TMP-related group exhibited significant improvements in learning and memory abilities in transgenic AD mice, along with reduced levels of Aβ and tau phosphorylation in the brain. This evidence is limited to animal models. Human clinical trials on CX or isolated TMP for Alzheimer's disease are not yet established.
TMP has been studied for its regulatory roles in ischemic cerebrovascular disease, spinal cord injury, Parkinson's disease, Alzheimer's disease, cognitive impairments, migraine, and depression. Available evidence for Parkinson's disease and depression remains largely preclinical.
5.7 Lipid Metabolism and Atherosclerosis
CX demonstrates significant pharmacological effects in treating CCVDs, such as atherosclerosis, myocardial and cerebral ischemia-reperfusion injury, and hypertension. Experimental studies indicate activity against atherosclerotic plaque formation and lipid dysregulation, but these results derive primarily from animal models and in vitro assays. DG-CX constitutes a classic pair of Chinese medicine that is widely used to treat hyperlipidemia, coronary heart disease, and atherosclerosis. However, only a few studies have conducted molecular docking and in vivo experiments to determine the therapeutic effects and mechanisms of DG-CX in atherosclerosis.
5.8 Overall Evidence Assessment
CX holds substantial clinical value for treating multi-system diseases, with extensive evidence supporting its use in CCVDs. Further research and clinical exploration of CX are warranted to fully harness its therapeutic potential.
It should be clearly stated that while CX is widely used clinically in China and other Asian countries, and while TMP and ferulic acid have been subjects of clinical investigation, most of the global peer-reviewed evidence base is preclinical (cell cultures, animal models) or consists of mechanistic network pharmacology studies. Current research mainly focuses on cell and animal experiments, where some active ingredients exhibit diverse pharmacological activities. However, further studies are needed to fully understand its specific mechanisms of action. In addition, there are multiple active ingredients in CX, but current research mainly focuses on the pharmacological effects of individual components, with little research on the interactions and synergistic effects between different components.
6. Body Systems and Health Areas of Association
SLR has significant clinical efficacy in relation to human diseases of the cardiocerebrovascular system, nervous system, respiratory system, digestive system, and urinary system. The following organ systems and health areas are the most prominently associated:
- Cardiovascular system: Coronary heart disease, hypertension, arrhythmia, atherosclerosis, heart failure.
- Cerebrovascular system: Ischemic stroke, cerebral ischemia-reperfusion injury, vascular dementia.
- Neurological system: Migraine, headache, neuropathic pain, Parkinson's disease, Alzheimer's disease, depression.
- Reproductive and gynecological system: Dysmenorrhea, amenorrhea, irregular menstruation, postpartum lochia.
- Musculoskeletal system: Rheumatic arthralgia, trauma-related swelling and pain.
- Hepatic system: Liver fibrosis (preclinical evidence).
CX can be administered alone or in combination with other traditional Chinese medicines or chemical drugs, showing efficacy in cardiovascular, nervous system, digestive system disorders, as well as analgesia and anticancer activities.
7. Dosage Forms and Reported Dosages
The standard dosage cited in traditional pharmacopeia practice is 3–9 g as a decoction for oral use. Up to 9 g is considered safe, with up to 3–6 g used to treat irregular menses. If overdosed, vomiting and dizziness can occur.
Nine dosage forms have been reported in the literature, including powders, pills, concentrated pills, drip pills, tablets, granules, bagged tea, oral liquid, and soft capsules. In clinical Chinese pharmacological research, standardized injectable preparations of TMP (ligustrazine) have been studied intravenously for acute ischemic stroke in Chinese hospitals. The therapeutic application of ligustrazine is constrained by inadequate water solubility, fast breakdown, and low bioavailability.
The Chuanxiong Chatiao formula (a classical multi-herb powder containing CX) has been studied in rabbits at doses of 9.85 g/kg in pharmacokinetic comparisons of powder and pill dosage forms, as reported in a 2022 PMC study (PMC9218571). These dosages are not directly translatable to human use recommendations.
Processing of the raw herb influences constituent profiles: Raw Chinese medicinal herbs and teas are subjected to extensive processing procedures prior to being used in clinical prescriptions or for the preparation of proprietary Chinese medicines. Assessing the effects of various processing methods and optimizing the processing parameters are important for producing the most effective herbs from raw herbal materials.
8. Safety Considerations and Interactions
8.1 Pregnancy and Uterine Stimulation
Chuan Xiong is contraindicated in pregnancy because blood-invigorating herbs can stimulate uterine contraction and threaten the pregnancy. Under normal circumstances, Chuanxiong should not be used for maintaining pregnancy. Due to its pharmacological properties, its unsupervised use during pregnancy may affect pregnancy safety. Self-administration must be strictly avoided.
Animal toxicity data on skeletal development show mixed results: For medicinals showing toxic effects at certain periods of administration during pregnancy, the toxicity should be particularly evident if the medicinals were taken throughout the entire pregnancy. However, skeletal anomalies reported for Chuanxiong Rhizoma given in certain periods did not arise when these medicinals were administered throughout the entire pregnancy. This suggests the timing of exposure may modulate embryotoxic risk, but the picture is not fully resolved and the contraindication in pregnancy is considered standard in Chinese medicine practice.
8.2 Bleeding Disorders and Anticoagulant Interactions
Chuan Xiong should also be used cautiously in patients with heavy menstrual bleeding, bleeding disorders, or recent surgery, and reviewed with a doctor if the patient takes warfarin or antiplatelet medication. Chuan Xiong may have anticoagulant effects and can affect clotting. Therefore, individuals with bleeding disorders or those taking anticoagulant medications should exercise caution.
A pharmacokinetic interaction study specifically examined CX combined with warfarin: In China, warfarin is usually prescribed with Chuanxiong Rhizoma for treating thromboembolism diseases. However, the reason for their combination is still being determined. The study explored the pharmacokinetic interactions of warfarin, Chuanxiong Rhizoma, and gut microbiota in the rat model of middle cerebral artery occlusion (MCAO). This interaction warrants attention given the antiplatelet and vasodilatory properties of CX constituents.
8.3 Gastrointestinal and Allergic Reactions
Some users have reported experiencing gastrointestinal discomfort, including nausea, vomiting, diarrhea, and abdominal pain. These symptoms are usually mild and transient but can be bothersome to some individuals. Allergic reactions to ligustrazine phosphate, although rare, can occur.
8.4 Yin-Deficiency Caution
Chuanxiong Rhizoma is warm and dry in nature; it should be used with caution in cases where yin-deficiency leads to hyperactivity of fire. Within the TCM framework, this refers to patients presenting with signs of internal heat arising from constitutional insufficiency — a traditional contraindication reflected in classical materia medica texts.
8.5 Bioavailability and Pharmacokinetic Limitations
Pharmacokinetic studies have shown that Z-ligustilide has poor oral bioavailability in rats due to severe first-pass metabolic reactions. The therapeutic application of ligustrazine is also constrained by inadequate water solubility, fast breakdown, and low bioavailability. These limitations partly explain why injectable pharmaceutical-grade TMP has been used in Chinese clinical settings when rapid action is required.
8.6 Quality Control and Adulteration Concerns
The current chemical markers in pharmacopeia or monography for the quality assessment of SLR are not well characterized or specifically characterized, nor do they fully reflect the medicinal efficacy of SLR, resulting in the quality of SLR not being effectively controlled. Chuanxiong is considered more valuable than gaoben, and adulteration using gaoben is not uncommon. Consumers and practitioners sourcing CX should be aware of the potential for substitution with related but chemically distinct species.
8.7 General Safety Profile
Ligusticum chuanxiong has been used in Japanese, Korean, and other traditional medicine for over 2,000 years. Currently, it is mostly cultivated and has high safety and low side effects. This characterization reflects its long traditional use history and published pharmacological safety data, though it is based predominantly on traditional experience and preclinical studies rather than systematic long-term human safety trials.
References
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