Thermopsis Lanceolata R.Br Extract; Cytisine HPLC98% Powder 485-35-8

Cytisine (also known as cytisinicline; CAS No. 485-35-8) is a compound found in plants of the genus Thermopsis within the legume family (Leguminosae). It is a natural alkaloid extracted from leguminous plants._[1-3] This plant contains various alkaloids, among which the relative content of quercetin is the highest, accounting for about half of the total alkaloid content. Chrysophylline has high medicinal value and is an important raw material for the pharmaceutical industry. Jinquehua alkaloid is a partial agonist of α4β2 nicotinic acetylcholine receptors, which is the basis for its various pharmacological effects, especially its smoking cessation effect.

Cytisine is primarily derived from the leguminous plant Thermopsis lanceolata R. Br., which is used as a medicinal herb and is commonly known as "Shepherd's Beans"(Muma beans). It is also known as the yellow-flowered bitter bean, wild cassia seed, spear-leaved wild cassia seed, or bitter bean.

Shepherd beans grow on riverbank grasslands, dunes, roadsides, and field edges. It is distributed in northeast, north, and northwest China, as well as Inner Mongolia, Hebei, Shanxi, Shaanxi, Ningxia, Gansu, Qinghai, Xinjiang, Sichuan, Xizang, and other provinces and regions.

The whole grass of Muma beans contains alkaloids ranging from 0.5% to 3%, of which the content of genistein accounts for about half of the total alkaloids. The alkaloid content in the seeds is relatively high, reaching up to 5%._[5] Its main alkaloid components are cytisine, in addition to berberine, sophocarpine, stinky bean alkaloid, methyl quercetin, eagle claw bean alkaloid, arginine, lupine, rhododendron alkaloid, and huanghua amine. The leaves still contain a small amount of flavonoids._[6] 

The extraction of cytisine utilizes multiple techniques designed to achieve high yield and purity. The conventional extraction process includes: raw material → drying → crushing → alcohol reflux extraction → separation by macroporous resin → separation by silica gel chromatography → recrystallization → drying → production.

• Traditional extraction and crystallization method: using muma beans as raw material, after crushing, soaking and extracting with ethanol, filtering and combining the filtrate, and concentrating to obtain the extract; adjust the pH of the extract with sulfuric acid and extract it with chloroform to remove organic impurities; Adjust the pH of the water layer with sodium hydroxide to make the alkaloid free, and then extract the total alkaloids with chloroform; Dissolve and cool the total alkaloids in acetone to obtain crude crystals; The crude crystals were repeatedly dissolved in ethyl acetate and acetone, cooled and recrystallized to obtain high-purity cytisine.

Featuring simple steps and easy operation, this method offers high efficiency, rapid crystallization, high yield, and product purity over 98%.

• Macroporous resin purification method: This method uses horse pea seeds as raw materials, crushed to 40-60 mesh, and extracted with supercritical CO₂ fluid (conditions: pressure 21-22 MPa, temperature 40-45 ° C, CO₂ flow rate 30-35 kg/h, extraction time 3-5 hours) to obtain crude cytisine.
  Dissolve the analyte in an acidified aqueous solution (pH 1–3) and filter. Adjust the pH to 7.5–8.5, adsorb onto a macroporous resin column, and rinse with water until the effluent runs neutral. Then elute the target compounds using 60–90% ethanol. The eluent is concentrated under reduced pressure to obtain a liquid extract. Finally, acetone is added and heated to reflux to dissolve the crystals 2-3 times. The crystals are filtered and dried at low temperature to obtain cytisine. This method has high extraction efficiency, requires fewer toxic reagents, and is more environmentally friendly._[10]

According to records, shepherd's bean is a toxic plant, and its main active ingredient is cytisine. Recent studies indicate that cytisine alkaloids exhibit multiple pharmacological effects, such as anti-arrhythmic, anti-ulcer, antimicrobial, and white blood cell-enhancing activities, with particularly potent anti-cancer properties._[6] 

• Core application: Smoking cessation assistance

The most well-known and extensively researched application of cytisine is smoking cessation assistance.

051 Mechanism of action:
Partial agonist: Cytisine can selectively bind with high affinity to α4 and β2 neuronal nicotinic acetylcholine receptors (nAChRs), partially mimicking the effects of nicotine, thereby helping to alleviate withdrawal symptoms during smoking cessation, such as anxiety, irritability, and craving for tobacco._[6] 
The results of the study indicate that "the smoking cessation effect of cytisine is superior to the currently widely used smoking cessation medication - placebo", and "genistein is cheaper compared to other smoking cessation therapies, and it may become an economically affordable treatment to promote smoking cessation worldwide". Research has shown that a smoking cessation preparation mainly composed of tartaric acid salt of cytisine has a one-year smoking cessation effectiveness rate of up to 22%, and has considerable development prospects in promoting smoking cessation._[7]

Numerous clinical trials and systematic reviews have demonstrated the efficacy of cytisine in supporting smoking cessation. A large-scale clinical trial (n=1200) showed that the 12-week smoking cessation success rate of smokers using genistein was 35%, significantly higher than the 15% success rate of the placebo group and the 20% success rate of the nicotine patch group. Compared with another commonly used smoking cessation drug, Varenicline, a randomized clinical trial involving 800 smokers showed that the success rate of smoking cessation with cytisine (25-day course) was 40%, which was comparable to Varenicline's (84-day course) success rate of 42%, with no statistically significant difference. This indicates that cytisine can achieve smoking cessation effects similar to varenicline in a shorter course of treatment._[8] 
The Cochrane systematic review indicates that cytisine is more effective than a placebo and may be as effective as varenicline. It is estimated that 18 to 23 out of every 100 people who quit smoking with cytisine may successfully quit.

052 Other potential applications and benefits:
Neuroprotection and cognitive improvement: It may have potential effects on improving cognitive function in Alzheimer's or Parkinson's disease by regulating the cholinergic system (still under research). Current research indicates that cytisine demonstrates pharmacological potential in several areas, including antiarrhythmic, antimicrobial, anti-ulcer, and leukocyte-enhancing effects , with antitumor activity warranting further attention.
Other traditional applications: In some countries (such as Russia), it is also used as an adjuvant therapy for bronchitis and hypotension (modern evidence is limited)._[9]

In clinical trials, cytisine has good tolerance. The most common adverse reactions include nausea, insomnia, abnormal dreams, and headaches, but they are usually mild in severity and alleviate over time. Serious adverse reactions are rare.

• Contraindicated population

①Pregnant and lactating women: It may affect fetal development or milk secretion.
②Cardiovascular disease patients, such as those with angina pectoris, arrhythmia (due to the possibility of elevated blood pressure and heart rate).
③Patients with mental illnesses, such as schizophrenia, may experience worsening symptoms.
④People who are allergic to genistein.

• Drug interactions

Avoid using in combination with the following medications:

①Other nicotine replacement therapies, such as nicotine patches, may excessively stimulate receptors and increase the risk of side effects.
②Antidepressants (such as SSRIs): They may increase the risk of neurological side effects.

Cytisine, a natural alkaloid, has gained prominence as an effective smoking cessation aid worldwide owing to its clear mechanism of action, clinically validated efficacy, favorable safety profile, and high cost-effectiveness. With the increasing awareness of health and the growing demand for smoking cessation, especially its potential advantages over varenicline and nicotine replacement therapy, the application prospects of genistein and its related products are highly promising.

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Tags: Cytisinicline; cytisine; Thermopsis lanceolata R.Br; Sophorine, Baptitoxine, Baphitoxine, manufacturers, suppliers, factory, wholesale, best, price, buy, for sale, bulk.

Reference:

[1]Institute of Botany, Chinese Academy of Sciences. Atlas of Chinese Higher Plants (Volume II) [M]. Beijing: Science Press, 1972
[2]Fu Kunjun, Zhang Zhenwan, He Shanbao, et al. Flora of China [M]. Beijing Science Press, 1993.42
[3]Li Yanghan. Chinese Weed Chronicles [M]. Beijing: China Agricultural Press, 1998
[4]Wuyong, Borijihan Geriletu. New Extraction Ways For Preparation Of Cytisine[J]. Journal of Inner Mongolia Normal University(Natural Science Edition), 2004, (02):186-187.
[5]Ye Run, Chen Yihui, Cai Jing, et al. Extracing Technology and Content Determination of High Purity Cytisine[J]. Ion Exchange and Adsorption, 2020, 36(02):163-172.DOI:10.16026/j.cnki.iea.2020020163.
[6]Zhang Yi. Extraction and Separation of Cytisine from Thermopsislanceolate in the Study on Production Process[D]. Northwest University, Xi'an, China, 2014.
[7]Coe JW, Brooks P R, Vetelino M G, et al1Varenicline: anA4B2nicotinic receptor partial agonist for smoking cessation[J]1J Med Chem, 2005,48(10): 3474-34771
[8]https://www.sohu.com/a/860949386_121869527
[9]https://m.chemsrc.com/Product/7564594.html
[10]https://m.tianyancha.com/zhuanli/b42ef47c100a4896859c3b5f84545a41