Vasicine alleviates 2,4-dinitrochlorobenzene-induced atopic dermatitis and passive cutaneous anaphylaxis in BALB/c mice.

Atopic dermatitis (AD), a type of skin inflammation, is associated with immune response mediated by T-helper 2 (Th2) cells, and mast cells. Vasicine is an alkaloid isolated from Adhatoda vasica, a popular Ayurvedic herbal medicine used for treating inflammatory conditions. In the present study, the anti-AD effects of vasicine were evaluated on 2,4-dinitrochlorobenzene-induced AD-like skin lesions in BALB/c mice. The potential anti-allergic effects of vasicine were also assessed using the passive cutaneous anaphylaxis (PCA) test. The results showed that the oral administration of vasicine improved the severity of AD-like lesional skin by decreasing histopathological changes and restoring epidermal thickness. Vasicine also inhibited the infiltration of mast cells in the skin and reduced the levels of pro-Th2 and Th2 cytokines as well as immunoglobulin E in the serum. Finally, vasicine inhibited the expression of pro-Th2 and Th2 cytokines in skin tissues, indicating the therapeutic potential of vasicine for AD.

Activity of Compound Agrimony Enteritis Capsules against invasive candidiasis: Exploring the differences between traditional Chinese medicine prescriptions and its main components in the treatment of diseases.

ETHNOPHARMACOLOGICAL RELEVANCE: Compound Agrimony Enteritis Capsules (FFXHC) is an ethnomedicine derived from Yi Nationality Herbal Medicine for the treatment of enteritis. We found that compared to berberine hydrochloride (BBR), a component of this medicine, FFXHC was more efficacious in the mouse model of IC mice in significantly alleviating lung and intestinal lesions. " Our study provides a novel perspective into the pharmacological mechanism of action of the ethnic compound FFXHC. AIM OF THE STUDY: To determine the underlying mechanism of the superiority of FFXHC over BBR in IC. MATERIALS AND METHODS: The susceptibility of Candida albicans to FFXHC was evaluated in vitro. The mouse model of IC was established and the survival rate, weight change, the number of organ colonies, and immune organ coefficient of the mice were determined, the effect of FFXHC on the immune function of mice, including changes in the number of immune cells, levels of the related inflammatory cytokines (INF-γ, TNF-α, MCP-1, IL-6, and IL-17A), and the antimicrobial peptide, LL-37 (CRAMP in mice), were determined. Mice feces were collected and changes in the intestinal microecology were studied. RESULTS: Our findings indicated that FFXHC was not active against Candida albicans and did not restore the sensitivity of the resistant strain in vitro; however, it had a therapeutic effect that improve survival rate on mice with IC. The number of lymphocytes and neutrophils of mice with IC treated with FFXHC increased significantly. The intestinal microecology of mice was restored and the abundance of the probiotic Bacteroides was increased, which further stimulated the production of the antimicrobial peptide, LL-37, which is required for acquired immunity. Furthermore, the levels of Th cell-related cytokines, including INF-γ, TNF-α, and IL-17A were significantly increased, whereas those of the proinflammatory cytokines, IL-6 and MCP-1, decreased. With the activation of acquired immunity, the immune function of mice was restored, the body weight and survival rate of mice improved considerably, the coefficients of the thymus and spleen increased, and the number of fungal colonies in the lung and kidney decreased. CONCLUSIONS: FFXHC could eliminate fungi by increasing the relative abundance of probiotics in Bacteroides and the number of neutrophils, thereby promoting the production of CRAMP and resulting in a fungicidal effect, leading to acquired immunity. Although BBR has an antifungal effect, we found that it was not as effective as FFXHC.

Synthesis of Scutellarein Derivatives with a Long Aliphatic Chain and Their Biological Evaluation against Human Cancer Cells.

Scutellarin is the major active flavonoid extracted from the traditional Chinese herbal medicine Erigeron breviscapus (Vant.) Hand-Mazz., which is widely used in China. Recently, accumulating evidence has highlighted the potential role of scutellarin and its main metabolite scutellarein in the treatment of cancer. To explore novel anticancer agents with high efficiency, a series of new scutellarein derivatives with a long aliphatic chain were synthesized, and the antiproliferative activities against Jurkat, HCT-116 and MDA-MB-231 cancer cell lines were assessed. Among them, compound 6a exhibited the strongest antiproliferative effects on Jurkat (IC50 = 1.80 µM), HCT-116 (IC50 = 11.50 µM) and MDA-MB-231 (IC50 = 53.91 µM). In particular, 6a even showed stronger antiproliferative effects than the positive control NaAsO2 on Jurkat and HCT-116 cell lines. The results showed that a proper long aliphatic chain enhanced the antiproliferative activity of scutellarein.

Kudinoside-D, a triterpenoid saponin derived from Ilex kudingcha suppresses adipogenesis through modulation of the AMPK pathway in 3T3-L1 adipocytes.

The leaves of Ilex Kudingcha, locally named "Kudingcha" in China, has been traditionally applied for treating obesity. Studies have demonstrated that the ethanol extract of Ilex kudingcha have anti-adipogenic effects. However, the constituent which was responsible for its anti-obesity and its underlying molecular mechanism has not yet been elucidated. This research explored the anti-obesity effect of kudinoside-D which was a main natural component of triterpenoid saponin from the ethanol extract of Ilex kudingcha, on lipid accumulation and the potential mechanism of action of adipogenesis in 3T3-L1 adipocytes. The adipocytes were treated with various concentrations of kudinoside D (0 to 40µM) during differentiation. The image-based Oil Red O staining analyses revealed that KD-D, dose dependently reduced cytoplasmic lipid droplet in 3T3-L1 adipocytes with the IC50 is 59.49µM. Meanwhile, major adipogenic transcription factor peroxisome proliferator-activated receptor γ (PPARγ), CCAAT/enhancer binding protein-α (C/EBPα) and sterol regulatory element-binding protein 1c (SREBP-1c) were significantly repressed as well as their target genes. The phosphorylation of AMP-activated protein kinase (AMPK) and its downstream target phosphorylated-acetyl CoA carboxylase (ACC) expression were also increased. In addition, the inhibitory effects of KD-D on the expressions of PPARγ and C/EBPα were weakened when cells were cotreated with AMPK inhibitor Compound C. These results indicated KD-D exerts anti-adipogenic effects through modulation of adipogenic transcription factors via AMPK signaling pathway. And the current findings demonstrated that KD-D was a potential therapeutic candidate for alleviating obesity and hyperlipidemia.

Simultaneous Qualitation and Quantitation of Chlorogenic Acids in Kuding Tea Using Ultra-High-Performance Liquid Chromatography-Diode Array Detection Coupled with Linear Ion Trap-Orbitrap Mass Spectrometer.

Kuding tea, the leaves of Ilex Kudingcha C.J. Tseng, has been applied for treating obesity, hypertension, cardiovascular disease, hyperlipidemia, and so on. The chlorogenic acids (CGAs) in Kuding tea have shown excellent antioxidative, antiobesity, anti-atherosclerotic and anticancer activities. Nevertheless, the chemical profiles of CGAs in Kuding tea have not been comprehensively studied yet, which hinders further quality control. In the present study, a sensitive ultra-high-performance liquid chromatography-diode array detection coupled with a linear ion trap-Orbitrap (UHPLC-DAD-LTQ-Orbitrap) method was established to screen and identify CGAs in Kuding tea. Six CGA standards were first analyzed in negative ion mode with a CID-MS/MS experiment and then the diagnostic product ions (DPIs) were summarized. According to the retention behavior in the RP-ODS column, accurate mass measurement, DPIs and relevant bibliography data, a total of 68 CGA candidates attributed to 12 categories were unambiguously or preliminarily screened and characterized within 18 min of chromatographic time. This was the first systematic report on the distribution of CGAs in Kuding tea. Meanwhile, the contents of 6 major CGAs in Kuding tea were also determined by the UHPLC-DAD method. All the results indicated that the established analytical method could be employed as an effective technique for the comprehensive and systematic characterization of CGAs and quality control of the botanic extracts or Chinese medicinal formulas that contain various CGAs.

Roemerine Improves the Survival Rate of Septicemic BALB/c Mice by Increasing the Cell Membrane Permeability of Staphylococcus aureus.

Staphylococcus aureus is one of the most frequently occurring hospital- and community-associated pathogenic bacteria featuring high morbidity and mortality. The occurrence of methicillin-resistant S. aureus (MRSA) has increased persistently over the years. Therefore, developing novel anti-MRSA drugs to circumvent drug resistance of S. aureus is highly important. Roemerine, an aporphine alkaloid, has previously been reported to exhibit antibacterial activity. The present study aimed to investigate whether roemerine can maintain these activities against S.aureus in vivo and further explore the underlying mechanism. We found that roemerine is effective in vitro against four S. aureus strains as well as in vivo against MRSA insepticemic BALB/c mice. Furthermore, roemerine was found to increase cell membrane permeability in a concentration-dependent manner. These findings suggest that roemerine may be developed as a promising compound for treating S. aureus, especially methicillin-resistant strains of these bacteria.

Potent Activities of Roemerine against Candida albicans and the Underlying Mechanisms.

Roemerine (RM) is an aporphine alkaloid isolated from the fresh rattan stem of Fibraurea recisa, and it has been demonstrated to have certain antifungal activity. This study aimed to investigate the antifungal activity of RM and the underlying mechanisms in Candida albicans (C. albicans). The in vitro antifungal activity of RM was evaluated by a series of experiments, including the XTT reduction assay, confocal laser scanning microscopy assay, scanning electron microscope assay. Results showed that 1 µg/mL RM inhibited biofilm formation significantly (p < 0.01) both in Spider medium and Lee's medium. In addition, RM could inhibit yeast-to-hyphae transition of C. albicans in a dose-dependent manner. The biofilm-specific and hypha-specific genes such as YWP1, SAP5, SAP6, HWP1, ECE1 were up-regulated and EFG1 was down-regulated after 8 µg/mL RM treatment. Furthermore, the toxicity of RM was investigated using C. elegans worms, three cancer cells and one normal cell. The date showed that RM had no significant toxicity. In conclusion, RM could inhibited the formation of C. albicans biofilm in vitro, but it had no fungicidal effect on planktonic C. albicans cells, and the anti-biofilm mechanism may be related to the cAMP pathway.

Limonoids from the fruits of Cipadessa cinerascens.

A new limonoid, 3-de(2-methylbutanoyl)-3-propanoylcipadesin (1), along with 10 known limonoids and 1 known triterpenoid, was isolated from the fruits of Cipadessa cinerascens. Their structures were elucidated on the basis of spectroscopic analysis. All compounds were evaluated for their antimicrobial activities, and compounds 6 and 12 showed weak antimicrobial activities against MRSA 82(#) and MRSA 92(#).

[Akaloids from roots of Stephania dentifolia].

Eight alkaloids were isolated from the thin sulfuric acid extracts of the fresh roots of Stephania dentifolia by aluminum oxide, silica and Sephadex LH-20 column chromatography methods. Based on the spectroscopic analysis and chemical evidence, the structures of these alkaloids were identified as sinoacutine (1), sinomenine (2), cephamonine (3), tetrahydropalmatine (4), capaurine (5), stepharanine (6), (+)-stepharine (7) and palmatine (8). All compounds were obtained from this plant for the first time.

[Chemical constituents of Aconitum brachypodum from Dong-Chuan area].

Aconitum brachypodum is traditionally known to be toxic chinese medicie, but its chemical constituents is not enough studied to date. To further elucidate the chemical constituents of A. brachypodum, 80% ethanol extract of A. brachypodum collected from Dong-Chuan area was investigated, which led to isolation of seventeen compounds. By spectroscopic methods, their structures were determined as hypaconitine (1), mesaconitine (2), talatisamine (3), neoline (4), fuziline (5), aconine (6), bullatine A (7), lepeine (8), songrine (9), isocorydine (10), beta-sitosterol (11), daucosterol (12), stearic acid (13), triacontanol (14), palmitic acid (15), benzoic acid (16), and inosine (17), respectively. All compounds except for compounds 1 and 7 were isolated from A. brachypodum for the first time.

[Studies on the chemical constituents of the leaves of Polygonum multiflorum].

OBJECTIVE: To study the chemical constituents of the leaves of Polygonum multiflorum. METHODS: The chemical constituents were extracted with water and separated by manifold chromatography technique, and their structures were determined by spectral analysis. RESULTS: Eleven compounds were isolated and identified as physcion (I), emodin (II), noreugenin (III), apigenin (IV), hyperoside (V), rutin (VI), vitexin (VII), 2,3,5 ,4'-tetrahydroxy-stibene-2-O-beta-D-glucoside (VIII), beta-amyrin (IX), beta-sitosterol (X), daucosterol( XI). CONCLUSION: Among these compounds, I - IV, VI - XI are isolated from the leaves of Polygonum multiflorum for the first time.

[Flavonoids in leaves of Alstonia scholaris].

OBJECTIVE: To investigate the flavonoids in leaves of Alstonia scholaris, an ethno-remedy of Dai People in Yunnan. METHOD: The chemical constituents were isolated and purified by column chromatography. Their structures were elucidated on the basis of spectroscopic evidences and physicochemical properties. RESULT: Eight flavonoids were isolated and identified as kaempferol (1), quercetin (2), isorhamnetin (3), kaempferol-3-0-beta-D-galactopyranoside (4), quercetin-3-0-beta-D-galactopyranoside (5), isorhamnetin-3-0-beta-D-galactopyranoside (6), kaempferol-3-0-beta-D-xylopyranosyl-( 2-1)-0-beta-D-galactopyranoside (7) ,quercetin-3-0-beta-D-xylopyranosyl-( 2-1)-0-beta-D-galactopyranoside (8). CONCLUSION: Flavonoids 1-7 were isolated from A. scholaris for the first time.

Antifungal alkaloids from the fresh rattan stem of Fibraurea recisa Pierre.

AIM OF THE STUDY: The rattan stem of Fibraurea recisa Pierre. is known as an ethno-remedy commonly used for the treatment of various skin diseases by the minority Yao, Zhuang and Miao in Yunnan Province of China. The present study was designated to evaluate its antifungal activity, and to root out the antifungal substances from this ethical herb. MATERIALS AND METHODS: The in vitro antifungal assay was performed by agar diffusion test for extracts and fractions. Then, the active fractions were submitted to column chromatography on silica gel and LH-20 to isolate their compounds. And the antifungal activity of pure compounds has been examined by checkerboard microdilution test. Nine Candida strains and one Cryptococcus strain were used for the bioassay. RESULTS: The MeOH extract exhibited significant antifungal activity, and the alkaloidal fractions were deduced as main active component. Subsequent studies led to the identification of a new alkaloid fibrecisine (1) and 21 known alkaloids including berberines, tetrahydroberberines and aporphine derivatives. The bioassay result indicated that the berberines showed more potent activity than aporphine derivatives against the test Candida strains, while tetrahydroberberines showed very weak activity against Cryptococcus neoformans. CONCLUSION: The new alkaloid fibrecisine (1) was identified as 1,2-methylenedioxy-8-hydroxy-6a(R)-aporphine by detailed spectral analysis. The rattan stem of Fibraurea recisa Pierre. is an effective antifungal herb, and its major active component is alkaloidal compounds. Bioassay tests revealed that the water-soluble berberines are the most important antifungal substances. The study provides preliminary scientific validation for the traditional medicinal use of this ethno-remedy.

[Studies on chemical constituents of Peucedanum delavayi].

OBJECTIVE: To study the chemical constituents of the radix and rhizome of Peucedanum delavayi. METHODS: The chemical constituents had been separated by manifold chromato-graphy methods, and their structures were determined by spectral analysis. RESULTS: Fifteen compounds were isolated and identified as Umbelliferone(I), Coumurayin(II), Mexoticin(III), Marmesin (IV), Ammijin(V), Delton (VI), Selinidin(VII), Anomalin(VII), Isopteryxin(IX), Ferulic acid(X), Falcarindiol(XI), Stearic acid(XII), beta-sitosterol(X III), Daucosterol(XIV) and d-Mannitol(XV). CONCLUSION: All these compounds are isolated from Peucedanum delavayi for the first time.

[Studies on chemical constituents from rattan of Polygonum multiflorum].

OBJECTIVE: To study on the chemical constituents from rattan of Polygonum multiflorum. METHODS: The chemical constituents were extracted with alcohol and were separated with manifold chromatography technique. Their structures were determined by spectral analysis. RESULTS: Thirteen compounds were isolated and identified as Chrysophanol(I), Physcion(II), Emodin(III), Aloeemodin(IV), Rhein(V), Physcion-8-O-beta-D-glucoside(VI), Emodin-8-O-beta-D-glucoside (VII),2,3,5,4'-Tetrahydroxy-stibene-2-O-beta-D-glucoside(VIII), Noreugenin(IX), Apigenin(X), Daucosterol(XI), beta-Sitosterol(XII), Stearic acid(XIII). CONCLUSION: Among these, compounds I, IV-VI, VIII-XI, XIII are isolated from rattan of Polygonum multiflorum for the first time.

[Studies on the chemical constituents of the aerial parts of Seseli mairei].

OBJECTIVE: To study the chemical constituents of the aerial parts of Seseli mairei Wolf. METHODS: The chemical constituents have been separated with manifold chromatography methods, and their structures were determined hy spectral analysis. RESULTS: Thirteen compounds were isolated and identified as sphondin (I), hergapten (II), isopimpinellin (III), umbelliferone (IV), chrysosptertin B (V), apiin (VI), rutin (VII), quercetin (VIII), ferulic acid (IX), falcarindiol (X), docosanol (XI), beta-sitosterol (XII), daucosterol (X III). CONCLUSION: All these compounds were isolated from the aerial parts of Seseli mairei Wolf. for the first time.