Gooderoside A from Anoectochilus elatus attenuates acute and chronic pains by inhibiting NO/cGMP and IRAK4/IRAK1/TAK1 signaling pathways.

ETHNOPHARMACOLOGICAL RELEVANCE: Anoectochilus elatus Lindl. was traditionally used for pain treatment and Gooderoside A (GA) was regarded as its principal constituent. AIM OF THE STUDY: To investigate whether GA can be responsible for the antinociceptive activity of A. elatus and explore its underlying mechanism. MATERIALS AND METHODS: Acetic acid-induced abdominal writhing and tail flick tests were employed to evaluate the antinociceptive activity of ethanolic extract of A. elatus (EEA) and GA. Formalin test was used to ascertain the antinociceptive pattern of GA. Entobarbital sodium induced sleep test was adopted to exclude its hypnotic effect, while open-field test was performed to rule out its motor impairment effect. Chronic constriction injury (CCI)-induced neuropathic pain in rats was developed to evaluate its efficacy on neuropathic pain, and BV-2 cells were used to explore the underlying mechanism. RESULTS: EEA and GA, significantly inhibited chemical and thermal nociception. GA suppressed nociception in formalin test in both phase I and II, whereas methylene blue and L-NAME partially reversed its efficacy. GA located inner and slightly blocked sodium channel current, and did not show any hypnotic effect or motor impairment effect. Crucially, GA markedly attenuated chronic neuropathic pain in rats, inhibited the phosphorylation of IRAK4, IRAK1 and TAK1, and suppressed MAPKs pathway in BV-2 cells. CONCLUSION: GA relieved acute and chronic pains in vivo. The mechanism of action involves the blocking of NO/cGMP and IRAK4/IRAK1/TAK1 pathways. These results suggested GA may be a promising candidate for antinociceptive drug development.

Total lignans from Vitex negundo seeds attenuate osteoarthritis and their main component vitedoin A alleviates osteoclast differentiation by suppressing ERK/NFATc1 signaling.

The seeds of Vitex negundo have been used for inflammation-related disease treatment in traditional medicine. This study focused on the anti-osteoarthritis (OA) effects of the total lignans of V. negundo seeds (TOV) in monosodium iodoacetate-induced osteoarthritis rats and its pharmacokinetic properties, as well as the effects and potential mechanism of its main components VN1 (6-hydroxy-4-(4-hydroxy-3-methoxy-phenyl)-3-hydro-xymethyl-7-methoxy-3,4-dihydro-2-naphthaldehydeb) and VN2 (vitedoin A) on receptor activator of NF-κB ligand (RANKL)-induced osteoclast differentiation in bone marrow macrophages (BMMs). TOV significantly attenuated osteoarthritis, leading to an increase in pain thresholds, improvement of knee articular cartilages and chondrocytes loss, and decreased total joint scores and serum levels of TNF-α, interleukin-1ß (IL-1ß), and prostaglandin E2 (PGE2) in osteoarthritis rats. The half-time (T1/2 ) was 2.82 h and 1.33 h, and the bioavailability was 15.34%-21.89% and 16.29%-22.11%, for VN1 and VN2, respectively. VN2, rather than VN1, remarkably inhibited tartrate-resistant acid phosphatase (TRAP) activity, reduced the number of TRAP-positive multinuclear cells, diminished the formation of actin ring, and decreased mRNA levels of cathepsin K (CTSK), TRAP, nuclear factor of activated T cell 1 (NFATc1), and osteoclast-associated receptor, as well as downregulated protein levels of p-ERK (phosphorylated extracellular signal-regulated kinase), TRAP, CTSK and NFATc1 in BMMs. These findings suggest TOV has promising therapeutic potential for OA treatment and VN2, in particular, attenuates osteoclast differentiation by suppressing ERK/NFATc1 signaling and actin ring, mainly accounting for the anti-OA efficacy of TOV.

A comparison review of Hehuan flowers and Hehuan bark on the traditional applications, phytochemistry and pharmacological effects.

ETHNOPHARMACOLOGICAL RELEVANCE: Albizia julibrissin Durazz is a well-known medicinal plant with the Chinese name Hehuan []. Hehuan bark and Hehuan flowers have long been recognized as traditional Chinese herbal medicine for treating anxiety, melancholy, insomnia, bruises, pulmonary abscess, fractures, carbuncle, amnesia, acute conjunctivitis, blurred vision, neonatal tetanus and stroke for thousands of years. They are recorded in Chinese Pharmacopoeia separately with different properties. Until now, new chemical constituents and pharmacological activities of Hehuan have been continuously studied and revealed. THE AIM OF THE REVIEW: This review aims to provide a comprehensive summary of traditional applications, phytochemistry, pharmacology effects, and toxicology of Hehuan bark and Hehuan flowers, and give critical assessment and point out the promising direction for further research on Hehuan. MATERIAL AND METHODS: A literature search was undertaken on Hehuan bark and Hehuan flowers by analyzing the information from scientific databases (SciFinder, Pubmed, Elsevier, Google Scholar, Web of Science, and Baidu Scholar). We also gathered the information of Hehuan from classic herbal literatures and conference papers on ethnopharmacology. RESULTS: According to Chinese and English documents, the medicinal history of Hehuan in China can be traced back to ad 25. Meanwhile, its medicinal history as a kind of herbal medicine can also be found in other Asian countries. So far about 140 compounds have been isolated from Hehuan bark and Hehuan flowers, including triterpenoids, flavonoids, lignans, phenolic acids, alkaloids, etc. Among them, flavonoids mainly exist in Hehuan flowers, while Hehuan bark contains lignans and saponins. The composition differences between the barks and flowers of Hehuan account for the different effects and applications. Modern pharmacological studies have indicated that crude extracts and pure compounds of Hehuan flowers and Hehuan bark have multiple pharmacological activities, such as antineoplastic, immunomodulatory, anti-inflammatory, anxiolytic, antidepressant, metabolic regulation, anti-insomnia, neuroprotective, hepatoprotective, sedative, and anti-osteolytic activities. CONCLUSIONS: Hehuan (Albizia julibrissin Durazz) is traditionally used to relieve depression, calm nerves, promote blood circulation and reduce swelling. Modern pharmacological studies have revealed that natural products from Hehuan bark and Hehuan flowers possess extensive pharmacological activities in treating cancer, enhancing immunity, regulating metabolism, improving mental state, etc. These properties make it great clinical application potential. Further research on natural pharmaceutical chemistry, pharmacology, toxicology, pharmacokinetics, and quality standards of Hehuan are still required to verify the efficacy and safety for future clinical applications.

Cardioprotective mechanisms of salvianic acid A sodium in rats with myocardial infarction based on proteome and transcriptome analysis.

Ischemic heart diseases (IHDs) cause great morbidity and mortality worldwide, necessitating effective treatment. Salvianic acid A sodium (SAAS) is an active compound derived from the well-known herbal medicine Danshen, which has been widely used for clinical treatment of cardiovascular diseases in China. This study aimed to confirm the cardioprotective effects of SAAS in rats with myocardial infarction and to investigate the underlying molecular mechanisms based on proteome and transcriptome profiling of myocardial tissue. The results showed that SAAS effectively protected against myocardial injury and improved cardiac function. The differentially expressed proteins and genes included important structural molecules, receptors, transcription factors, and cofactors. Functional enrichment analysis indicated that SAAS participated in the regulation of actin cytoskeleton, phagosome, focal adhesion, tight junction, apoptosis, MAPK signaling, and Wnt signaling pathways, which are closely related to cardiovascular diseases. SAAS may exert its cardioprotective effect by targeting multiple pathways at both the proteome and transcriptome levels. This study has provided not only new insights into the pathogenesis of myocardial infarction but also a road map of the cardioprotective molecular mechanisms of SAAS, which may provide pharmacological evidence to aid in its clinical application.

A combination of Yiqiqubai granule and 308-nm excimer laser in treatment of segmental vitiligo: a prospective study of 233 patients.

OBJECTIVE: To study the effect of Yiqiqubai granule combined with 308-nm excimer laser treatment for segmental vitiligo (SV). METHODS: A prospective research was performed in 233 patients with SV treated in Shanghai General Hospital from 11 February 2015 to 25 August 2016, they were divided into group A (n = 75), group B (n = 78) and group C (n = 80) according to the random number table. Group A was treated with Yiqiqubai granule, group B treated with 308-nm excimer laser and group C treated with combined treatments. The treatment time lasts for 6 months. The clinical efficacy, color-reverse rate and quality of life of the three groups were assessed. RESULTS: After treatment, the effective rate and markedly effective rate of group C (87.5%, 51.3%) were significantly higher than group A (74.7%, 42.7%) and group B (80.8%, 47.4%) (p < .05). Color-reverse rate of group C (66.5 ± 17.6%) was much higher than group A (47.2 ± 16.4%) and group B (49.9 ± 24.2%) (p < .05). Significant differences were found among three groups after treatment in terms of embarrassment, social and work (p < .05). CONCLUSIONS: The combination of 308-nm excimer laser and Yiqiqubai granule in the treatment of SV has good clinical effect.

[Study on ultraviolet-screening effect of extracts from mangosteen (Garcinia mangostana Linn.) pericarp].

OBJECTIVE: To analyze the ultraviolet-screening of the n-butanol extracts of mangosteen pericarp and alpha-mangostin, compare the ultraviolet-screening effect of the extracts with rutin and ultramicro-titanium dioxide (TiO2). METHODS: The samples (n-butanol extract from mangosteen pericarp, alpha-mangostin, rutin and TiO2) were scanned at different wavelength and Pan-wavelength by ultraviolet spectrophotometry. RESULTS: The n-butanol extracts and alpha-mangostin had relatively satisfactory effects on ultraviolet-screening when the concentration was over 0.40 mg/ml and the effects on ultraviolet-screening was better than TiO2. CONCLUSION: The n-butanol extracts and alpha-mangostin had a positive ultraviolet-screening activity which was better than TiO2.

[Chemical constituents from the flower of Paulownia fortunei( seem. ) Hemsl].

OBJECTIVE: To study the chemical constituents of the flower of Paulownia fortunei (Seem.) Hemsl. METHODS: The constituents were isolated by column chromatography and their structures were elucidated through spectroscopic analysis. RESULTS: The compounds were identified as diplacone( I ) ,3 '-O-methyldiplacone ( II ) , mimulone ( ll) , ursolic acid( IV ), beta-sitosterol ( V ), daucosterol ( VI). CONCLUSION: All these compounds were obtained from the flower for the first time.

[Non-alkaloid constituents from a Tibetan medicine Meconopsis quintuplinervia].

OBJECTIVE: To study the chemical constituents of a Tibetan medicine Meconopsis quintuplinervia. METHOD: Column chromatographic techniques were applied to isolate constituents. A combination of IR, MS and NMR spectroscopy was used to identify structures of constituents. RESULT: Twelve compounds were isolated from the ethanolic extract and their structures were elucidated as quercetin 3-O-beta-D-glucopyranoside (I), quercetin 3-O-beta-D-galactopyranosyl-(1-->6)-glucopyranoside (II), kaempferol 3-O-beta-D-glucopyranosyl-(1-->2)-beta-D-glucopyranoside (III), isorhamnetin 3-0-beta-D-galactopyranosyl-(1-->6)-beta-D-glucopyranoside (IV), caffeic acid (V), protocatechuic acid (VI), p-hydroxycinnamic (VII), 2-(3,4-dihydroxyphenyl )-ethyl-O-beta-D-glucopyranoside (VIII), p-hydroxybenzoyl-beta-D-glucopyranoside (IX), 4-O-beta-D-glucopyranosyl-(Z)-p-coumaric acid (X), 5, 7-dihydroxy-4H-4-chromenone (XI), daucosterol (XII). CONCLUSION: Ten compounds were isolated from this genus for the first time except for XI and XII.

Acetylated flavonol diglucosides from Meconopsis quintuplinervia.

Four acetylated flavonol diglucosides, quercetin 3-O-[2'''-O-acetyl-beta-d-glucopyranosyl-(1-->6)-beta-d-glucopyranoside], quercetin 3-O-[2''',6'''-O-diacetyl-beta-d-glucopyranosyl-(1-->6)-beta-d-glucopyranoside], isorhamnetin 3-O-[2'''-O-acetyl-beta-d-glucopyranosyl-(1-->6)-beta-d-glucopyranoside], and quercetin 3-O-[2'''-O-acetyl-alpha-l-arabinopyranosyl-(1-->6)-beta-d-glucopyranoside], together with five known flavonol glycosides quercetin 3-O-beta-d-glucopyranoside, kaempferol 3-O-beta-d-glucopyranoside, quercetin 3-O-[beta-d-galactopyranosyl-(1-->6)-glucopyranoside], isorhamnetin 3-O-[beta-d-galactopyranosyl-(1-->6)-beta-d-glucopyranoside], and kaempferol 3-O-[beta-d-glucopyranosyl-(1-->2)-beta-d-glucopyranoside] have been isolated from Meconopsis quintuplinervia. Their structures were determined using chemical and spectroscopic methods including HRFABMS, (1)H-(1)H COSY, HSQC and HMBC experiments.

Studies on chemical constituents of Rheum glabricaule.

OBJECTIVE: To study the chemical Constituents in the root of Rheum glabricaule. METHODS: Compounds were isolated by various column chromatographies with sillica gel. Their structures were identified by spectral analysis (MS, 1HNMR, 13 CNMR) and chemical evidences. RESULTS: Seven compounds were isolated from this plant, including n-hexacosnic acid (I), palmitic acid (II), daucosterol (III), chrysophanol-8-Me ether (IV), citreorosein (V), chrysophanol 8-O-beta-D-glucopyranoside (VI) and 2,5-dimethyl-7-methoxychromone (VII). CONCLUSION: All above compounds are obtained from this plant for the first time.

[Studies on chemical constituents from Salvia roborowskii Maxim].

OBJECTIVE: To study the chemical constituents from Salvia roborowskii Maxim. METHODS: Chromatography and spectroscopic analysis were employed to isolate and elucidate the chemical constituents in the plant. RESULTS: Three compounds were isolated and elucidated as 1 beta-hydroxy-lupeol (I), quercetin-3-O-beta-D-glucoside (II), rutin (III). CONCLUSION: I - III were isolated from this plant for the first time.

[Study on the chemical constituents of Buddleja purdomii].

OBJECTIVE: To study the chemical constituents of Buddleja purdomii W. W Smith. METHODS: The constituents were isolated and purified by various chromatographic methods and structurally identified by spectral analysis. RESULTS: 4 compounds were obtained as cryptomeridiol (I), aucubin (II), galactilol (III), daucosterol (IV). CONCLUSION: All these compounds are obtained from this plant for the first time.

[Study on the chemical constituent from Buddleja purdomii].

OBJECTIVE: To study the chemical constituents from Buddleja purdomii W. W. Smith. METHODS: The constituents were isolated and purified by various chromatographic methods and structurally identified by spectral analysis. RESULTS: 4 compounds were identified as vanillin (I), vanillic acid (II), acteoside (III), acteoside isomer (IV). CONCLUSION: All these compounds were obtained from this plant for the first time.

[Alkaloids from a Tibetan medicine Meconopsis quintuplinervia Regel].

AIM: To reinvestigate the chemical constituents of the ethanolic extract of Meconopsis quintuplinervia Regel which is a traditional Tibetan medicine used for treatments of hepatitis, tuberculosis etc.. METHODS: The compounds were enriched by column chromatography techniques over silica gel, macro porous resin and Sephadex LH-20 absorbents, and finally purified by reverse phase preparative HPLC methods with isocratic mobile phase systems of methanol-H2O-acetic acid (500:500:1) and acetonitrile-H2O-acetic acid (200:800:1). Structural determination of the pure compounds were based on extensive analyses of modern spectroscopic methods including IR, MS, HRMS, 1D- and 2D-NMR spectra. RESULTS: Three alkaloids were obtained and their structures were elucidated as norsanguinarine (I), O-methylflavinantine (II) and 6-methoxy-17-methyl-2, 3-[methylenebis (oxy)]-morphin-5-en-7-one (III). CONCLUSION: Norsanguinarine (I) was isolated from genus Meconopsis for the first time, and 6-methoxy-17-methyl-2,3-[methylenebis(oxy)]-morphin-5-en-7-one (III) is a new alkaloid named as meconoquintupline.

[Studies on chemical constituents of Choerospondias axillaris].

Ten compounds were isolated from the dry fruit of Choerospondias axillaris (Roxb.) Burtt et Hill. Their structures were elucidated as dihydroquercetin(1), quercetin(2), protocatechuic acid(3), gallic acid(4), 3,3'-di-o-methylellagic acid(5), beta-sitosterol(6), daucosterol (7), stearic acid(8), triacontanoic acid(9), octacosanol(10) by IR, EI-MS and NMR.

[Studies on chemical constituents of Salvia roborowskii Maxim].

OBJECTIVE: To study the chemical constituents from Salvia roborowskii Maxim. METHODS: Chromatography and spectroscopic analysis were employed to isolate and elucidate the chemical constituents in the plant. RESULTS: Six compounds were isolated and elucidated as lupeol (I), 11 beta-hydroxy-lupeol(II),3 beta-acetyl-11 beta-hydroxy-lupeol(III), ursolic acid (IV), beta-sitosterol(V), daucosterol (VI). CONCLUSION: I approximately VI were isolated from this plant for the first time.

[Studies on chemical constituents of Meconopsis quintuplinervia Regel].

Seven flavonoids were isolated from Meconopsis quintuplinervia Regel for the first time, and their structures were elucidated as quercetin (I), dihydroquercetin (II), luteolin (III), chrysoeriol (IV), apigenin (V), huazhongilexone (VI) and hydnocarpin (VII) by spectroscopic methods including IR, EIMS, 1D- and 2D-NMR techniques.