Biphasic effects of baicalin, an active constituent of Scutellaria baicalensis Georgi, in the spontaneous sleep–wake regulation

Chang, Han-Han; Yi, Pei-Lu; Cheng, Chiung-Hsiang; Lu, Ching-Lan; Hsiao, Yi‐Tse; Tsai, Yao-Chen; Li, Chia‐Ling; Chang, Fang‐Chia

doi:10.1016/j.jep.2011.03.023

Cited by 32 publications

(14 citation statements)

References 29 publications

(52 reference statements)

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“…By contrast, baicalin increased both SWS and REMS during 8–10 hours of the dark (active) period when baicalin was administered at the beginning of the dark period, and this effect can be blocked by the GABA A receptor antagonist bicuculline. Taken together, these results demonstrated that baicalin exhibits biphasic effects on sleep-wake regulation (decreases in SWS during the light period and increases in SWS and REMS during the dark period) and the inhibition of IL-1 action together with enhancement of GABA A receptor activity may mediate the effects of baicalin during the light and dark periods, respectively [30]. Besides baicalein, wogonin (monoflavonoid, 5,7-dihydroxy-8-methoxyflavone), a benzodiazepine receptor ligand isolated from Scutellaria baicalensis Georgi had been tested by Kwok Min Hui et al .…”

Section: Resultsmentioning

confidence: 85%

“…Its main active components of anti-inflammatory are baicalin, baicalein, and wogonin [74]. It has been widely used in China and other Asian countries for its anti-inflammatory, anti-pyretic, anti-bacterial, anti-hypertensive, anti-allergic and sedating effects [30]. Recently, several studies have demonstrated the effectiveness of Scutellariae Radix in insomnia treatment, nevertheless, the clinical practice focus on the CNS regulation function of Scutellaria baicalensis is limited [30].…”

Section: Resultsmentioning

confidence: 99%

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Herbal Insomnia Medications that Target GABAergic Systems: A Review of the Psychopharmacological Evidence

Shi¹,

Dong²,

Zhao³

et al. 2014

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Insomnia is a common sleep disorder which is prevalent in women and the elderly. Current insomnia drugs mainly target the γ-aminobutyric acid (GABA) receptor, melatonin receptor, histamine receptor, orexin, and serotonin receptor. GABAA receptor modulators are ordinarily used to manage insomnia, but they are known to affect sleep maintenance, including residual effects, tolerance, and dependence. In an effort to discover new drugs that relieve insomnia symptoms while avoiding side effects, numerous studies focusing on the neurotransmitter GABA and herbal medicines have been conducted. Traditional herbal medicines, such as Piper methysticum and the seed of Zizyphus jujuba Mill var. spinosa, have been widely reported to improve sleep and other mental disorders. These herbal medicines have been applied for many years in folk medicine, and extracts of these medicines have been used to study their pharmacological actions and mechanisms. Although effective and relatively safe, natural plant products have some side effects, such as hepatotoxicity and skin reactions effects of Piper methysticum. In addition, there are insufficient evidences to certify the safety of most traditional herbal medicine. In this review, we provide an overview of the current state of knowledge regarding a variety of natural plant products that are commonly used to treat insomnia to facilitate future studies.

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Section: Resultsmentioning

confidence: 85%

Section: Resultsmentioning

confidence: 99%

Herbal Insomnia Medications that Target GABAergic Systems: A Review of the Psychopharmacological Evidence

Shi¹,

Dong²,

Zhao³

et al. 2014

View full text Add to dashboard Cite

show abstract

“…Scutellaria baicalensis has documented clinical safety (103,104). There are reports of sedation and it has been shown to be active on the GABA receptor sites (105,106). A medical food combination of purified Scutellaria baicalensis and the bark of Acacia catechu containing concentrated baicalin and catechin (Limbrel TM , Move Free Advanced TM ) caused reversible liver damage in at least 35 cases, with a calculated estimated incidence of approximately 1 in 10,000 (107).…”

Section: Discussionmentioning

confidence: 99%

Evaluation of Natural and Botanical Medicines for Activity Against Growing and Non-growing Forms of B. burgdorferi

Feng

Leone

Schweig³

et al. 2020

Front. Med.

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Lyme disease is the most common vector-borne disease in the US and Europe. Although the current recommended Lyme antibiotic treatment is effective for the majority of Lyme disease patients, about 10-20% of patients continue to suffer from persisting symptoms. There have been various anecdotal reports on the use of herbal extracts for treating patients with persisting symptoms with varying degree of improvements. However, it is unclear whether the effect of the herb products is due to their direct antimicrobial activity or their effect on host immune system. In the present study, we investigated the antimicrobial effects of 12 commonly used botanical medicines and three other natural antimicrobial agents for potential anti-Borrelia burgdorferi activity in vitro. Among them, 7 natural product extracts at 1% were found to have good activity against the stationary phase B. burgdorferi culture compared to the control antibiotics doxycycline and cefuroxime. These active botanicals include Cryptolepis sanguinolenta, Juglans nigra (Black walnut), Polygonum cuspidatum (Japanese knotweed), Artemisia annua (Sweet wormwood), Uncaria tomentosa (Cat's claw), Cistus incanus, and Scutellaria baicalensis (Chinese skullcap). In contrast, Stevia rebaudiana, Andrographis paniculata, Grapefruit seed extract, colloidal silver, monolaurin, and antimicrobial peptide LL37 had little or no activity against stationary phase B. burgdorferi. The minimum inhibitory concentration (MIC) values of Artemisia annua, Juglans nigra, and Uncaria tomentosa were quite high for growing B. burgdorferi, despite their strong activity against the non-growing stationary phase B. burgdorferi. On the other hand, the top two active herbs, Cryptolepis sanguinolenta and Polygonum cuspidatum, showed strong activity against both growing B. burgdorferi (MIC = 0.03-0.06% and 0.25-0.5%, respectively) and non-growing stationary phase B. burgdorferi. In subculture studies, only 1% Cryptolepis sanguinolenta extract caused complete eradication, while doxycycline and cefuroxime and other active herbs could not eradicate B. burgdorferi stationary phase cells as many spirochetes were visible after 21-day subculture. Further studies are needed to identify the active constituents of the effective botanicals and evaluate their combinations for more effective eradication of B. burgdorferi in vitro and in vivo. The implications of these findings for improving treatment of persistent Lyme disease are discussed.

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“…Scutelaria baicalensis has been used safely in clinical use (142–144), and has a long historical record of safety. There are reports of sedation and it has been shown to be active on the GABA receptor sites (though this is frequently used to help anxiety and sleep)(145) (145–147). A medical food combination of purified Scutellaria baicalensis and the bark of Acacia catechu containing baicalin and catechin, concentrated and standardized to greater than 90% purity (Limbrel ™, Move Free Advanced ™) caused reversible liver damage in at least 35 cases, with a calculated estimated incidence of approximately 1 in 10,000 (148, 149).…”

Section: Discussionmentioning

confidence: 99%

Evaluation of Natural and Botanical Medicines for Activity against Growing and Non-growing Forms ofB. burgdorferi

Feng

Leone²,

Schweig³

et al. 2019

Preprint

View full text Add to dashboard Cite

Lyme disease is the most common vector-borne disease in the US. Although the current recommended Lyme antibiotic treatment can cure the majority of Lyme disease patients, about 10-20% patients continue to suffer from persisting symptoms. There have been various anecdotal reports on the use of herbal extracts for treating patients with persisting symptoms with varying degree of improvements. However, it is unclear whether the effect of the herb products is due to their direct antimicrobial activity or their effect on host immune system. In the present study, we investigated the antimicrobial effects of 12 commonly used botanical medicines and 3 other natural antimicrobial agents for potential anti-Borrelia burgdorferi activity in vitro. Primary criteria for selecting compounds for the present study included agents that had shown significant anti-borrelial effects in previous studies, have favorable safety profiles, and can be absorbed systemically. Among them, 9 natural product extracts at 1% were found to have good activity against the stationary phase B. burgdorferi culture compared to the control antibiotics doxycycline and cefuroxime. These active herbs include Cryptolepis sanguinolenta, Juglans nigra (Black walnut), Polygonum cuspidatum (Japanese knotweed), Artemesia annua (Sweet wormwood), Uncaria tomentosa (Cat’s claw), Cistus incanus, and Scutellaria baicalensis (Chinese skullcap). In contrast, Stevia rebaudiana, Andrographis paniculata, Grapefruit seed extract, colloidal silver, monolaurin, and antimicrobial peptide LL37 had little or no activity against stationary phase B. burgdorferi. The minimum inhibitory concentration (MIC) values of Artemesia annua, Juglans nigra, and Uncaria tomentosa were quite high for growing B. burgdorferi, despite their strong activity against the non-growing stationary phase B. burgdorferi cells. On the other hand, the top two active herbs, Cryptolepis sanguinolenta and Polygonum cuspidatum, showed strong activity against both growing B. burgdorferi (MIC=0.03%-0.06% and 0.25%-0.5% respectively) and non-growing stationary phase B. burgdorferi. In subculture studies, only 1% Cryptolepis sanguinolenta extract caused complete eradication, while current Lyme antibiotics doxycycline and cefuroxime and other active herbs including Polygonum cuspidatum, Artemesia annua, Juglans nigra and Uncaria tomentosa could not eradicate B. burgdorferi stationary phase cells as many spirochetes were visible after 21-day subculture. Further studies are needed to identify the active ingredients of the effective herbs and evaluate their combinations for more effective eradication of B. burgdorferi in vitro and in vivo. The implications of these findings for more effective treatment of persistent Lyme disease are discussed.

show abstract

Biphasic effects of baicalin, an active constituent of Scutellaria baicalensis Georgi, in the spontaneous sleep–wake regulation

Cited by 32 publications

References 29 publications

Herbal Insomnia Medications that Target GABAergic Systems: A Review of the Psychopharmacological Evidence

Herbal Insomnia Medications that Target GABAergic Systems: A Review of the Psychopharmacological Evidence

Evaluation of Natural and Botanical Medicines for Activity Against Growing and Non-growing Forms of B. burgdorferi

Evaluation of Natural and Botanical Medicines for Activity against Growing and Non-growing Forms ofB. burgdorferi

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