Ergot is a name in traditional Chinese medicine. It refers to the sclerotia of the fungi Claviceps purpurea (Fr.) Tul. and Claviceps microcephala (Wallr.) Tul., both belonging to the Clavicipitaceae family. It has the effects of uterine contraction, hemostasis, and pain relief. It is primarily used to treat postpartum hemorrhage and migraines.
Ergot
Ergot is a name in traditional Chinese medicine. It refers to the sclerotia of the fungi Claviceps purpurea (Fr.) Tul. and Claviceps microcephala (Wallr.) Tul., both belonging to the Clavicipitaceae family. It has the effects of uterine contraction, hemostasis, and pain relief. It is primarily used to treat postpartum hemorrhage and migraines.
Chinese Name : 麦角
Aliases : Black Rye, Purple Ergot
Nature, Flavor & Meridian Tropism : Pungent and slightly bitter in taste; neutral in nature
Benefits & Efficacy
Benefits
Induces uterine contractions to stop bleeding and relieves pain.
Indications
Postpartum hemorrhage and migraines.
Usage and Dosage
Oral use: Prepare as a fluid extract; take 0.5–2 mL 3–4 times daily; for high doses, take 4 mL once daily, up to 12 mL per day; or use as tablets or injections.
Precautions
Contraindicated for pregnant women, women in labor, and when the placenta has not been fully expelled. Use with caution in patients with liver disease or peripheral vascular disease. This product is toxic; accidental ingestion often causes thirst, vomiting, diarrhea, cold extremities, pallor, and visual and auditory disturbances; in severe cases, hallucinations, convulsions, and even coma or death may occur.
Chemical Constituents
It contains alkaloids, which can be divided into three categories. The first category consists of ergot alkaloids, which are amide derivatives of ergot acid. The main compounds include ergonovine, ergotamine, ergobutine, ergobutrine, ergonine, ergopentamine, ergometrine, α-ergocryptine,β-ergocryptine, ergocornine, o-12′-methyl-α-ergocryptine, o-12′-methyl-ergocornine, ergobin, ergamine, ergocline, and ergostine, among others.The second class consists of the corresponding ergot-isotoxin alkaloids, which are amide derivatives of isergic acid. The main members include ergotisone, ergotisogen, ergotibutine, ergotinine, ergotisopotine, ergotisoxine, α-ergotisocryptine, β-ergotisocryptine, ergotikonine, o-12′-methyl-α-ergotocrypthamine, o-12′-methyl-ergotocornine, ergobin, ergotamine, and ergocrine, among others.The third category consists of ergot alkaloids from Ergotum species, including ergotamine, 6,7-dihydroergotamine, ergotamine, setotergotamine, isosetotergotamine, ergotamine from Ergotum, ribergotamine, and naked ergotamine. In addition, it contains ergosterol, ergothioneine, rye ketone acids A, B, C, and D, golden ergonic acid, 4,5-dimethyloctanoic acid, ergopigments AD, BD, CD, DD, AC, BC, and CC, ergot-jade red alkaloid, ergot xanthophyll, as well as sugars, fatty oils, and other compounds.
Pharmacological Actions
1. Uterine stimulant effect: Ergot alkaloids such as ergamine and ergotamine have a stimulating effect on the uterus. This effect is most pronounced in the pregnant uterus. The action is strong and long-lasting. Among these, ergotamine is the most potent, followed by ergamine. Ergotamine acts directly on uterine smooth muscle; at high doses, it can cause tonic contractions of the uterine muscles, compressing the blood vessels within the uterine muscle at the site of placental implantation to stop bleeding.Uterine sensitivity to ergot increases during the third trimester of pregnancy. Ergot tincture is primarily used for postpartum hemorrhage and uterine involution, and its effects are relatively mild. 2. Effects on the Nervous System: Large doses of ergotamine and other ergot alkaloids can block α-adrenergic receptors, reversing the pressor effect of epinephrine; however, they do not block the release of sympathetic neurotransmitters.Small doses of ergot can stimulate the medullary centers (resulting in vagal-induced bradycardia, increased respiration, convulsions, etc.), while large doses can cause medullary paralysis and death. Ergotamine can also potentiate the sedative and hypnotic effects of barbiturates, morphine, and methadone. 3. Effects on the Cardiovascular System: In in vitro studies, ergotamine causes contraction of peripheral vascular smooth muscle; in whole animals, it can lead to elevated blood pressure due to vasoconstriction and induce compensatory bradycardia. High doses of ergotamine can damage vascular endothelial cells, leading to gangrene. Ergot toxin has a weaker effect on blood vessels than ergotamine, while ergonovine has virtually no effect on blood pressure and does not damage vascular endothelial cells.The mechanism by which ergotamine treats migraines primarily involves its direct vasoconstrictive effect on smooth muscle, causing dilated extracranial arteries to constrict, or it may be related to the activation of serotonin (5-HT) receptors in the arterial wall, thereby restoring normal tone and pulsation to the cerebral arteries and alleviating headache. 4. Pharmacokinetics: ① Ergotamine: Rapid and complete absorption occurs after oral or intramuscular administration; uterine contractions begin approximately 6–15 minutes after oral administration, with effects lasting 3 hours; intravenous administration takes effect immediately. This drug is metabolized in the liver and excreted in the urine via the kidneys. ② Ergotamine: Oral absorption is approximately 60% but irregular; co-administration with caffeine can enhance the absorption of ergotamine and strengthen its vasoconstrictive effects.Oral administration generally takes effect within 1–2 hours. Peak blood concentrations are reached in 0.5–3 hours. The half-life (t₁/₂) is approximately 2 hours. It is primarily metabolized in the liver. Approximately 90% of metabolites are excreted in bile. A small amount of the unchanged drug is excreted in urine and feces.
Relevant Discussions
1. *Pharmacology of Traditional Chinese Medicine*: “It is a uterine contractile agent. It is effective for uterine bleeding, postpartum atonic hemorrhage, and conditions such as uterine insufficiency and atrophy.”
2. *Manual of High-Altitude Chinese Herbal Medicine*: “Used to treat migraines.”
3. *Flora of Medicinal Plants of Hangzhou*: “It is an internal hemostatic agent.”
Applications
Notes
The sclerotia of Claviceps macrocephala Torl. (large-headed ergot) are also used medicinally and have the same effects as ergot. The sclerotia are black, hard, and horn-shaped. They commonly parasitize the spikes of Poaceae plants such as ice grass, broom grass, aloe, barley, wheat, and ryegrass. They are distributed in Xinjiang.
Processing & Preparation
Harvesting & Processing
Harvested in summer and fall when the wheat ears turn yellow and ripen. Dry in the shade or by artificial heat for later use.
Crude Drug Identification
Properties of Crude Drugs
1. Ergot: The sclerotium is long spindle-shaped, straight or slightly arched, with three blunt ridges; it measures 1–4 cm in length and 2–7 mm in width. The outer surface is grayish-purple to dark purple, with fine transverse cracks and longitudinal grooves.The texture is hard and brittle; it breaks easily. The fracture surface is flat and slightly bluntly triangular, with a thin layer of dark purple tissue along the edges. The interior ranges from pale brownish-white to pale red, and star-shaped dark patterns are sometimes visible in the central portion. It has a distinctive but faint odor; the taste is initially slightly sweet, followed by a pungent aftertaste.
2. Small-headed Ergot: The sclerotium is black, horn-shaped, approximately 6 mm long, and about 0.7 mm in diameter. All other characteristics are similar to those of common ergot.
In both cases, the best specimens are those that are dry, large and uniform in size, purplish-brown in color, and white at the fracture surface.
Botanical Information
Botanical Classification
Ergot fungus (Claviceps) and small-headed ergot (Claviceps minor) of the Clavicipitaceae family.
Morphological Characteristics
1. Ergot: The sclerotium is oblong-cylindrical, horn-shaped at both ends, hard, (10–30) mm × (2–7) mm, smooth, with longitudinal grooves, purplish-black externally, and pale purple or grayish-white internally. Each sclerotium produces 20–30 stroma, which have slender, curved stalks that are dark brown. The stroma are nearly spherical, 1–2 mm in diameter, and reddish-brown.All ascomata are embedded within the stroma, with their apertures slightly protruding from the stroma surface, measuring (200–250) μm × (150–175) μm. The asci are long cylindrical.(100–125) μm × (4–5) μm, containing 8 ascosporangia. The ascosporangia are filamentous, colorless, and measure (50–70) μm × 1 μm. 2. Small-headed Ergot: Extremely similar to Ergot, the main distinction being that the sclerotia are black and horn-shaped, and the resulting fruiting bodies have smaller heads, with a diameter of less than 0.8 mm.
Distribution Area
1. Ergot: Found in Northeast China, North China, Xinjiang, Jiangsu, Zhejiang, Sichuan, and other regions. 2. Small-headed ergot: Found in Northeast China, Inner Mongolia, and other regions.
Growth Habits
Ergot is a parasitic fungus that infects plants in the Poaceae, Cyperaceae, Caryophyllaceae, and Juncaceae families. Sclerotia grow during warm, humid summers, and hyphae thrive at temperatures of 24–26°C.
Cultivation Techniques
Ergot is primarily produced by inoculating host plants to obtain ergot (sclerotia); alternatively, mycelium can be fermented to yield sclerotia-like substances and their active components. While ergot can also be obtained through inoculation cultivation, this method is labor-intensive and yields low output; therefore, industrial-scale deep-bed fermentation technology is currently the predominant production method. (1) Strain Isolation: Pure ergot strains are isolated from wild sclerotia collected in the wild. Currently, the superior strain used in fermentation is the Ce3-3 strain of Ergotus erigonis, isolated from Erigonis erigonis. (2) Process Flow: Strain → Spore culture on slanted test tube media → Seed culture and fermentation → Filtration, followed by separation and extraction of ergotamine. (3) Cultivation Method: The spore culture medium consists of 10% sucrose, 0.1% aspartate, 0.03% MgSO₄·7H₂O, 0.1% KH₂PO₄, 2% agar, and distilled water, with a pH of 6.0–6.2. The medium is prepared as a slant, inoculated with the strain, and incubated at 24–26°C for 15–20 days. The seed medium consists of 6% sucrose, 1.2% glutamic acid, 0.03% MgSO₄·7H₂O, 0.1% KH₂PO₄, and tap water, adjusted to a pH of 5.2. Fill a 500-mL conical flask with 100 mL of the medium, inoculate with the slant culture, and incubate on a rotary shaker for 72 hours at 24–26°C. The fermentation medium consisted of 10% sucrose, 1.2% glutamic acid, 0.03% MgSO₄·7H₂O, 0.1% KH₂PO₄, 0.5% soybean oil, and tap water, adjusted to a pH of 7.5.Fill a 500-liter conical flask with 75 liters of fermentation medium, inoculate with 5% of the culture, and incubate on a rotary shaker at 24–26°C for 9 days. Assay method: Total ergot alkaloids were extracted using sodium carbonate and chloroform. Ergotamine was extracted and separated using the ion-exchange resin method.