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Bupleurum

Background & General Info

Bupleurum is a genus belong to the Apiaceae or parsley family and comprises a number of annual and perennial shrubs and herbs. Bupleurum chinense and Bupleurum scorzonerifolium are extensively distributed in the grasslands, stream banks, forest margins, sunny slopes, and roadsides of China, Japan, and Korea. ^[1]Bupleurum falcatum is endemic to Europe and Western Asia.

Bupleurum - Botany

Bupleurum chinense is an herbaceous perennial plant characterized by erect, tufted stems and alternately arranged leaves with broadly linear-lanceolate leaf blades and acuminate apex. Its roots are conical and taupe. The five-petal, bright yellow flowers are borne from axillary and terminal compound umbels, with the plant blossoming from July to September. During the months of August to October, the plant bears oblong, brown fruits that are approximately 3 mm in length. ^[1]Bupleurum falcatum is a perennial that can grow up to a meter tall. Its lanceolate basal leaves have broad upper lamina, whereas its linear to lanceolate middle and upper leaves are gradually shorter and falcate. ^[2]

Bupleurum scorzonerifolium is another herbaceous perennial plant. Its primary features consist of usually glabrous stems; reddish brown roots; and linear or linear-lanceolate leaves with acuminate apex. Its yellow flowers comprise five petals as well and its fruits are ellipsoid and dark brown. ^[1]

Bupleurum - History & Traditional Use

The dried roots of Bupleurum falcatum are traditionally used in folk medicine as an anti-inflammatory and antioxidative remedy. ^[3] In traditional oriental medicine, they are also broadly used as remedy to psychosomatic disorders. ^[4]

Scarcely known in the West, Bupleurum Chinense is a very important herb in Chinese herbalism. It is considered to release toxins from the liver but not used on its own because it does not eliminate the toxins from the body. Detoxification is a multi-stage process.

In Asian countries such as China, Japan, and Korea, Radix Bupleuri, which refers to the dried roots of Bupleurum chinense and Bupleurum scorzonerifolium, has been traditionally used as medicine for more than 2000 years for influenza, fever, inflammation, malaria, menstrual disorders, and hepatitis. ^[5] Ancient Chinese medical literatures mentioned its ability to normalize the exterior and interior metabolisms, diffuse “evil heat” from the surface, soothe the liver, and promote yang and qi (“life force”). ^[6]

Bupleurum - Herbal Uses

A number of scientific studies have been conducted on many species of genus Bupleurum, which generated massive data about their extracts’ biological activities. ^[5] Triterpene saponins isolated from Bupleurum species have been shown to exhibit immunomodulatory, anti-inflammatory, and antiviral activities, and several saikosaponins from Bupleurum display very potent anti-inflammatory, hepatoprotective, and immunomodulatory actions both in vivo and in vitro. ^[5]

Bupleurum - Constituents / Active Components

Chemical profiling of genus Bupleurum characterized numerous groups of secondary metabolites with important biological activities, including triterpene saponins (especially saikosaponins), lignans, essential oils, and polysaccharides. ^[5] Gas chromatography–mass spectrometry (GC–MS) analysis by Shi et al. (2010) on the essential oil from Bupleurum longiradiatum roots identified 51 compounds, including thymol (7.0%), butylidene phthalide (6.8%), 5-indolol (5.6%), heptanal (5.3%), 4-hydroxy-2-methylacetophenone (5.3%), 4,5-diethyl-octane (5.3%), bormeol (5.1%), and hexanoic acid (5.1%). ^[7] A 2013 Iranian study also screened the chemical composition of water-distilled essential oils from the aerial parts of Bupleurum falcatum and Bupleurum gerardi. α-Pinene (29.4%) and spathulenol (27.7%) were identified as the major compounds of Bupleurum falcatum essential oil, whereas higher amounts of undecane (62.9%) and germacrene D (11.1%) were isolated from Bupleurum gerardi essential oil. ^[8]

Bupleurum - Medicinal / Scientific Research

Anticancer:

A 2015 Chinese study confirmed the anticancer, apoptotic, and antioxidant properties of extract from Bupleurum chinense roots against human epithelial ovarian cancer cells (HO-8910) in vitro and further explained that such anticancer property was mediated by induction of apoptosis, DNA fragmentation, and disruption of mitochondrial membrane potential. In the MTT assay, Bupleurum chinense root extract exerted potent and dose-dependent cytotoxic effects against the cancer cells and stimulated apoptosis, as evidenced by cell shrinkage, chromatin condensation, and membrane blebbing. In the Annexin V/PI double staining assay, which was used to quantify percentage of apoptotic cells, there was a marked rise in the average proportion of total apoptotic cells, from 9.4% in control cells to 18.5, 28.2, and 50.5% in cells treated with the extract at doses of 20, 80, and 120 μg/mL, respectively. ^[9]

Antitumor components of Bupleurum, especially saikosaponins A and D, have been proven to be potent against human hepatoma cells as well as other human cell lines. In the study of Motoo and Sawabu (1994), 20 µg/mL of saikosaponin D and 50 µg/mL of saikosaponin A inhibited the cell growth of human PLC/PRF/5 hepatoma cells by 50%. Saikosaponin A in particular suppressed the growth and DNA synthesis of tested human hepatoma cell lines, human liver cells, and human pancreatic cancer cell line. ^[10]

Anti-inflammatory:

Initial studies on the genus Bupleurum had paid particular attention only on the traditional uses of several Bupleurum species as treatment of inflammatory disorders and infectious diseases. ^[5] An early study in 1975 confirmed the anti-inflammatory property of saikosaponins A and D isolated from Bupleurum falcatum roots using female albino rats. ^[11] In the study of Bermejo Benito et al. (1998), saikosaponins isolated from Bupleurum rigidum displayed potent in vivo anti-inflammatory activity on experimental mouse ear edema and showed a substantial effect on cellular systems that generate cyclooxygenase and lipoxygenase metabolites. ^[12]

Hepatoprotective:

In an early animal study, pretreatment of saikosaponin D extracted from Bupleurum falcatum roots had been shown to remarkably protect the liver against carbon tetrachloride-induced injury in rats, preventing acute damage and significantly inhibiting lipid peroxidation. Saikosaponin D also minimized the severity of cirrhosis caused by constant injection of carbon tetrachloride in treated rats. ^[13]

Depression And Anxiety:

Administration of Bupleurum falcatum extract had been shown to significantly alleviate depression and anxiety-like behaviors, perhaps via central adrenergic mechanisms. By employing the forced swimming test and elevated plus maze test in rats that had been exposed to repeated restraint stress, Lee et al. (2012) investigated the effect of Bupleurum falcatum extract on the rodents’ behavioral responses. Intraperitoneal pretreatment of rodents with Bupleurum falcatum extract at daily doses of 20, 50, or 100 mg/kg for 15 days resulted in a significant reduction in immobility in the forced swimming test and augmented open-arm exploration in the elevated plus maze test. Additionally, findings from the immunohistochemical examination revealed that the extract prevented any increase in the expression of tyrosine hydroxylase in the locus coeruleus (a nucleus located in the brain stem) of treated rats that underwent restraint stress. ^[14]

Memory Impairment:

Lee et al.’s (2009) research results revealed the protective property of Bupleurum falcatum against neuronal and cognitive impairments caused by repeated immobilization stress in rats and its potential utility in mitigating stress-induced memory impairment. In this study, 14-day oral treatment of Bupleurum falcatum at a dose of 150, 300, or 600 mg/kg in rats before their exposure to repeated immobilization stress resulted in noteworthy enhancement in escape latency (time required to find the platform) in the Morris water maze test and triggered an anxiolytic-like effect in the elevated plus maze behavioral test. Moreover, Bupleurum falcatum treatment significantly lessened the loss in cholinergic immunoreactivity due to repeated immobilization stress in the hippocampus. ^[4]

Hyperthyroidism:

Being a source of antioxidants, Bupleurum falcatum has been considered as a medicinal plant that can be of value against numerous endocrine diseases. Findings from the study of Kim et al. (2012) indicated the benefits of water extract derived from Bupleurum falcatum in ameliorating hyperthyroidism and its associated organ damage. In a rat model wherein hyperthyroidism was elicited by using L-thyroxine, oral treatment of Bupleurum falcatum water extract at doses of 300, 150, and 75 mg/kg for 15 days led to a dose-dependent reversal of hyperthyroidism and its effects, stabilizing L-thyroxine-induced liver oxidative stresses and decreasing alterations in liver and epididymal fats. ^[3]

Peptic Ulcers:

Oral administration of BR-2, an antiulcer polysaccharide fraction from Bupleurum falcatum, in rats had been demonstrated in a 2002 study to be effective in promoting healing of acetic acid-induced chronic ulcers. ^[15]

Allergic Asthma:

Saikosaponin A, which is isolated from Bupleurum falcatum extract, had been demonstrated by Park et al. (2002) to dose-dependently hamper the passive cutaneous anaphylaxis reaction in rats at an intravenous dose greater than 1 mg/kg and hence to display an inhibitory activity against allergic asthma. Maximum inhibition of nearly 60% was achieved at a dose of 10 mg/kg. At doses of 3 and 10 mg/kg, this active compound prevented the bronchoconstriction associated with asthma in sensitized guinea pigs. However, it only weakly inhibited the histamine-induced tracheal contraction in guinea pigs, as well as the histamine release in mast cells of experimental rats. ^[16]

Bupleurum - Contraindications, Interactions, And Safety

The herbal use of Bupleurum is generally considered safe, with no contraindications having been concretely established. However, long-term use of the herb in clinical applications has been reported to cause liver toxicity, which is manifested by transaminase lifts, hepatitis, and jaundice. ^[6] A 2016 review of reports on adverse events resulting from the use of complementary and alternative medicine within the period of 2009 to 2014 found 11 hepatotoxicity cases (31.4%) associated with Radix Bupleuri use out of the 57 reports eligible for analysis. ^[17] Liver functions nonetheless return to normal after some time. ^[6] Side effects include mild lethargy, sedation, and drowsiness, as well as flatulence and bowel movements in large doses. ^[18]

Article researched and created by Dan Ablir for herbshealthhappiness.com.
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