Cimicifuga Rhizome Research Articles

The features of optimal nonhormonal therapy of vegetative disorders among women with postmenopause

Objectives: to evaluate the clinical effectiveness of the Vitae-Melatonin in the complex treatment of vegetative disorders in postmenopausal women.Materials and methods. The 64 postmenopausal women who complained of vegetative disorders were included in our prospective study. Patients were divided into clinical groups. The first group consisted of 31 women who were prescribed a herbal preparation of Cimicifuga racemosa extract – 30 mg/day for 3 months. The second group included 33 patients who received in addition to the herbal medicine Vitae-Melatonin 3 mg/day every evening 2 hours before bedtime for 1 month. The clinical effectiveness of the therapy was assessed 1, 2 and 3 months after the start of treatment based on the dynamics of psychological disorders, somatic symptoms, vasomotor and sexual disorders, sleep problems and satisfaction with the therapy.Results. The use of herbal medicine containing Cimicifuga rhizome extract alone or in combination with Vitae-Melatonin in postmenopausal women significantly reduced the manifestations of vegetative disorders, including psychological and dyssomnia in a month from the start of therapy. After 3 months from the start of therapy, the advantage of combined therapy involving Vitae-Melatonin compared to the monotherapy of Cimicifuga rhizome was marked by a significant reduction of psychological disorders, somatic symptoms, vasomotor disorders and sleep problems (р = 0.003, р = 0.01, р = 0.02 and p = 0.015, respectively). Patient satisfaction with the combined therapy of vegetative disorders during the menopause compared to monophytotherapy was probably higher (risk ratio 1.63, 95% confidence interval 1.09–2.44, p = 0.018). There was no significant difference between the two research groups regarding side effects during and after the use of the drugs (p > 0.05).Conclusions. The use of Vitae-Melatonin at a dose of 3 mg/day in addition to phytotherapy in postmenopausal women had a clear clinical effect, which was a significant reduction of vegetative disorders, both compared to the initial indicators and in comparison with monophytotherapy. Results of the study showed the safety of melatonin, as well as the willingness of participants to continue using melatonin after 3 months of the treatment.

Fibrous Roots of Cimicifuga Are at Risk of Hepatotoxicity

The cause of liver damage by using black cohosh preparation has been concerned but remains unclear. After a preliminary investigation, the black cohosh medicinal materials sold in the market were adulterated with Asian cohosh (Cimicifuga) without removing the fibrous roots. The safety of Cimicifuga rhizome and fibrous roots is unknown and has not been reported. Therefore, in this paper, the rhizome and fibrous roots of Cimicifuga dahurica (Turcz.) Maxim (C. dahurica) were completely separated, extracted with 70% ethanol, and freeze-dried to obtain crude rhizome extract (RC) and fibrous roots extract (FRC). UHPLC-Q-TOF-MS was used to identify 39 compounds in the rhizome and fibrous roots of Cimicifuga, mainly saponins and phenolic acids. In the L-02 cytotoxicity experiment, the IC50 of fibrous roots (1.26 mg/mL) was slightly lower than that of rhizomes (1.417 mg/mL). In the 90-day sub-chronic toxicity study, the FRC group significantly increased the level of white blood cells, ALP, ALT, AST, BILI and CHOL (p < 0.05); large area of granular degeneration and balloon degeneration occurred in liver tissue; and the expression of p-NF-kB in the nucleus increased in a dose-dependent manner. Overall, Fibrous roots of Cimicifuga are at risk of hepatotoxicity and should be strictly controlled and removed during the processing.

Suppression of Release of Matrix Metalloprotease-1 from Human Gingival Fibroblasts by Cimicifuga Rhizome Extract and a Novel Cimigenol Xyloside as an Active Constituent

Oral malodor has become a major oral problem and the need for self-medication has increased. Oral malodor is attributed to the various enzymes produced by periodontal bacteria and the treatment of periodontal disease is recognized as the major therapy for oral malodor. In our research program to investigate novel agents for alternative medicine, which are effective for oral malodor treatment, we focused on Cimicifuga rhizomes used in ancient Chinese medicine for the treatment of periodontal diseases. In order to evaluate the effectiveness of Cimicifuga rhizomes on periodontal disease, suppression of matrix metalloprotease-1 from human gingival fibroblasts was assayed. A 50% ethanol extract from Cimicifuga rhizomes showed 51.0% suppression at 10 μg/mL. Activity-guided purification of the active principle was led to the isolation of 7,8-didehydrocimigenol 3- O-β-D-xylopyranoside (1), 24- epi-24- O-acetyl-7,8-didehydrohydro-shengmanol 3- O-β-D-xylopyranoside (2) and a novel compound (3). Compound 3 was elucidated as 24,25-epoxy-7,8-didehydrohydroshengmanol 3- O-β-D-xylopyranoside by spectral analysis. Compounds 1 and 3 suppressed matrix metalloprotease-1 release at 50 nM. From these results, the extract from Cimicifuga rhizome may be a novel agent for oral malodor therapy as an alternative medicine.

Antibacterial Activity Of Shin’iseihaito (Xinyiqingfeitang) And its Components Against Methicillin-Resistant Staphylococcus aureus

Objective: Shin’iseihaito (xinyiqingfeitang in Chinese, SSHT), a formula in traditional Japanese Kampo medicine and Chinese medicine comprising nine crude drugs, Gypsum, Ophiopogon Tuber, Scutellaria Root (SR, root of Scutellaria baicalensis), Gardenia Fruit, Anemarrhena Rhizome, Lilium Bulb, Magnolia Flower, Loquat Leaf, and Cimicifuga Rhizome (CR, rhizome of Cimicifuga heracleifolia), is commonly used to treat sinusitis associated with purulent nasal discharge and reddish nasal mucosa. We evaluated anti-bacterial activity of SSHT extract on methicillin-resistant Staphylococcus aureus (MRSA), one cause of bacterial sinusitis. Materials and Methods: Sterile paper disks impregnated with SSHT extract, the combination of crude drugs composing SSHT according to the traditional pharmacological theory, or each component were placed on Mueller-Hinton agar plates inoculated with several strains of MRSA isolated from the patients. The diameter of inhibitory zone was measured after 18–24 h incubation. Results: SSHT extract showed antibacterial activity against 128/190 (66.8%) MRSA clinical isolates. The effect of the extract of SSHT without heat-clearing drugs (SSHT–HC) or without exterior-releasing drugs (SSHT–ER) were significantly lower than that of SSHT extract. Each water extract of SR, Loquat Leaf, Magnolia Flower and CR showed significant anti-MRSA activity, and SR extract exhibited the largest inhibitory zone. Conclusions: SSHT has antibacterial activity against MRSA clinical isolates, and SR mainly contributes to the antibacterial activity of SSHT against MRSA clinical isolates.

Evaluation of the Botanical Origin of Black Cohosh Products by Genetic and Chemical Analyses

Despite the increasing sales of black cohosh (the dried rhizome and root of Cimicifuga racemosa L.) in the world herbal market, these products have continuous adulteration issues. The botanical authenticity of the black cohosh products is the first important step for ensuring their quality, safety and efficacy. In this study, we genetically identified the botanical sources of 10 black cohosh products and 5 Cimicifuga Rhizome crude drugs of Japanese Pharmacopoeia grade, and analyzed the metabolic profiling of 25 black cohosh products using liquid chromatography-tandem mass spectrometry (LC-MS/MS). Consequently, we found that C. dahurica and possibly C. foetida are misused as sources of the black cohosh products and in some cases, the extracts of black cohosh were adulterated with the plant materials of C. dahurica. We demonstrated that these three species can be distinguished by three marker compounds in a specific mass range. These results must be helpful in establishing regulations for the safe use of the black cohosh products.

Medicinal herbal extracts of Sophorae radix Acanthopanacis cortex Sanguisorbae radix and Torilis fructus inhibit coronavirus replication in vitro

Cimicifuga rhizome, Meliae cortex, Coptidis rhizome and Phellodendron cortex have been previously shown to exhibit anti-coronavirus activity. Here, an additional 19 traditional medicinal herbal extracts were evaluated for antiviral activities in vitro. A plaque assay was used to evaluate the effects of 19 extracts, and the concentration of extract required to inhibit 50% of the replication (EC(50)) of mouse hepatitis virus (MHV) A59 strain (MHV-A59) was determined. The 50% cytotoxic concentration (CC(50)) of each extract was also determined. Northern and western blot analyses were conducted to evaluate antiviral activity on viral entry, viral RNA and protein expression, and release in MHV-infected DBT cells. Sophorae radix, Acanthopanacis cortex and Torilis fructus reduced intracellular viral RNA levels with comparable reductions in viral proteins and MHV-A59 production. The extracts also reduced the replication of the John Howard Mueller strain of MHV, porcine epidemic diarrhoea virus and vesicular stomatitis virus in vitro. Sanguisorbae radix reduced coronavirus production, partly as a result of decreased protein synthesis, but without a significant reduction in intracellular viral RNA levels. The EC(50) values of the four extracts ranged from 0.8 to 3.7 microg/ml, whereas the CC(50) values ranged from 156.5 to 556.8 microg/ml. Acanthopanacis cortex and Torilis fructus might exert their antiviral activities in MHV-A59-infected cells by inducing cyclooxygenase-2 expression via the activation of extracellular signal-related kinase (ERK) and p38 or ERK alone, respectively. Sophorae radix, Acanthopanacis cortex, Sanguisorbae radix and Torilis fructus might be considered as promising novel anti-coronavirus drug candidates.

Induction of mast cell degranulation by triterpenoidal saponins isolated from Cimicifuga Rhizome

Induction of mast cell degranulation by triterpenoidal saponins isolated from Cimicifuga Rhizome

Two New 15‐Deoxycimigenol‐Type and Three New 24‐epi‐Cimigenol‐Type Glycosides from Cimicifuga Rhizome

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Three New 15,16-Seco-cycloartane Glycosides from Cimicifuga Rhizome

Three new 15,16-seco-cycloartane glycosides, which were constructed by a C-C bond cleavage in the D ring, have been isolated from Cimicifuga Rhizome for the first time. Their structures were determined by the use of 2D NMR techniques and chemical evidence.

Two New 15-Deoxycimigenol-Type and Three New 24-epi-Cimigenol-Type Glycosides from Cimicifuga Rhizome

Two new 15-deoxycimigenol-type (1, 2) and three new 24-epi-cimigenol-type glycosides (3-5) were isolated from Cimicifuga Rhizome, and the structures were elucidated on the basis of spectroscopic data including 2D NMR spectra and chemical evidence. The two new 15-deoxycimigenol-type glycosides were the first cimigenol-type glycosides lacking a hydroxyl group at C-15.

Two New Tetranor‐cycloartane Glycosides from Cimicifuga Rhizome.

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Three cycloartane glycosides from Cimicifuga rhizome and their immunosuppressive activities in mouse allogeneic mixed lymphocyte reaction.

One known (1) and two new cycloartane triglycosides, 20S,22R,23S,24R-16beta,23;22,25-diepoxy-cycloartane-3beta,23,24-triol 3-O-beta-D-glucopyranosyl-(1-->2)-beta-D-glucopyranosyl-(1-->2)-beta-D-xylopyranoside (2) and 20S,22R,23S,24R-16beta,23;22,25-diepoxy-cycloartane-3beta,23,24-triol 3-O-(6-O-trans-isoferuloyl-beta-D-glucopyranosyl)-(1-->2)-beta-D-glucopyranosyl-(1-->2)-beta-D-xylopyranoside (3), were isolated from a commercial Cimicifuga Rhizome. Their structures were determined by two dimensional (2D) NMR spectroscopic analysis and chemical evidence. These compounds suppressed the proliferation of lymphocytes in mouse allogeneic mixed lymphocyte reaction.

Two new tetranor-cycloartane glycosides from cimicifuga rhizome.

Two new tetranor-cycloartane glycosides (1, 2) were isolated from Cimicifuga Rhizome. Their structures were determined by spectroscopic analysis. These compounds suggested the existence of a biogenetic pathway into C-23 lactone-type cycloartane glycosides.

Two new 15,16-seco-cycloartane glycosides from Cimicifuga rhizome.

Two new 15,16-seco-cycloartane glycosides (1, 2) were isolated from Cimicifuga Rhizome. Their structures were determined by spectroscopic analysis.

Vasoactive effects of cimicifugic acids C and D, and fukinolic acid in cimicifuga rhizome.

Vasoactive effects of cimicifugic acids A-E, fukinolic acid and fukiic acid isolated from Cimicifuga plants were investigated using rat aortic strips. Cimicifugic acid D and fukinolic acid at 3x10(-4) M caused a sustained, slowly developing relaxation of aortic strips precontracted with norepinephrine (NE) in preparations with or without endothelium. Cimicifugic acid C inversely caused a weak contraction. Cimicifugic acids A, B and E and fukiic acid showed no vasoactivity at 3x10(-4) M. Cimicifugic acids A-E and fukinolic acid are esters between cinnamic acids and the hydroxyl group of benzyltartaric acids. For the manifestation of vasoactivity in the rat aorta, it is concluded that in the cinnamic acid moiety, a caffeoyl group might be necessary for the relaxation activity, and the p-coumaroyl group causes contraction. Concentration response curves for the Ca2+-induced contracture of depolarized aortic strips with isotonic high K+ were not affected by cimicifugic acid D or fukinolic acid. The Ca2+-induced contraction of aortic strips, preincubated with 10(-6) M NE in the presence of 10(-6) M nicardipine and 0.01 mM EGTA in Ca2+-free solution, were inhibited by cimicifugic acid D and fukinolic acid. These results indicated that the inhibition by cimicifugic acid D and fukinolic acid of the NE-induced contraction of rat aorta are attributable to the suppression of Ca2+ influx from the extracellular space enhanced by NE.

ChemInform Abstract: Studies on the Chinese Crude Drug “Shoma.” Part 10. Three New Trinor‐9, 19‐cyclolanostanol Xylosides, Cimicifugosides H‐3, H‐4, and H‐6, from Cimicifuga Rhizome and Transformation of Cimicifugoside H‐1 into Cimicifugosides H‐2, H‐3, and H‐4.

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Studies on the Chinese crude drug "shoma." IX. Three novel cyclolanostanol xylosides, cimicifugosides H-1, H-2 and H-5, from cimicifuga rhizome.

Three new cyclolanostanol xylosides were isolated from a batch of commercial Cimicifuga Rhizome, cimicifugoside H-1 (1), C35H52O9, mp 260-262 degrees C, [alpha]D -43.5 degrees, cimicifugoside H-2 (2), C35H54O10, mp 227-229 degrees C, [alpha]D -38.8 degrees, and cimicifugoside H-5 (3), C35H52O10, mp 262-264 degrees C, [alpha]D -22.9 degrees, together with known glycosides, actein and 27-deoxyactein. Their structures were determined on the basis of chemical and spectrometric evidence including an X-ray crystallographic analysis. The structure of cimicifugoside H-1 (1) was established as (20R,24R)-24,25-epoxy-11 beta-hydroxy-3-beta-(beta-D- xylopyranosyloxy)-9,19-cyclolanost-7-ene-16,23-dione. Cimicifugoside H-5 (3) is the 15-hydroxylated derivative of 1. Since 1 changed into cimicifugoside H-2 (2) on treatment with p-toluenesulfonic acid, 2 has a 24R,25-diol structure derived from 1 by opening its epoxy ring.

Studies on the Chinese Crude Drug "Shoma". X. Three New Trinor-9,19-cyclolanostanol Xylosides, Cimicifugosides H-3, H-4 and H-6, from Cimicifuga Rhizome and Transformation of Cimicifugoside H-1 into Cimicifugosides H-2, H-3 and H-4.

Three trinor-triterpenol glycosides were isolated from a batch of commercial Cimicifuga Rhizome : cimicifugoside H-3 (1), C32H48O9, mp 249-251 °C, [α]D -22.3°, cimicifugoside H-4 (2), C32H48O9, mp 265-267 °C, [α]D -75.0°, and cimicifugoside H-6 (3), C32H O10, mp 275-276 °C, [α]D -64.3°, On the basis of chemical and spectral data, the structure of 1 was proposed to be 11β, 24-dihydroxy-3β-(β-D-xylopyranosyloxy)-25, 26, 27-trinor-9, 19-cyclolanost-7-ene-16, 23-dione. Cimicifugoside H-4 (2), 11β, 16α, 24α-trihydroxy-3β-(β-D-xylopyranosyloxy)-25, 26, 27-trinor-9, 19 : 16, 24-dicyclolanost-7-en-23-one, seems to be generated from intramolecular aldol condensation between C-16 and C-24 of 1. Cimicifugoside H-6 (3) is the 15α-hydroxy derivative of 2. Cimicifugoside H-2 (5), which has already been obtained from cimicifugoside H-1 (4) under an acidic condition, was found to give 1, 2 and an α-hydroxy enone (2a) under an alkaline condition.

Three Novel Cyclolanostanol Xylosides from Cimicifuga Rhizome.

Three novel xylosides, cimicifugosides H-1(1), -3(2) and -4(3), were isolated from a commercial Cimicifuga Rhizome. Their structures were determined on the basis of chemical and spectrometric evidence including an X-ray crystallographic analysis. The xyloside 1 is 3-O-xyloside of (20R, 24R)-24, 25-epoxy-3β, 11β-dihydroxy-9, 19-cyclolanost-7-ene-16, 23-dione, while 2 and 3 are 3-O-xylosides of 25, 26, 27-trinor-derivatives from the genin of 1.