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Dihuang powder (DHP) has been used in the traditional Chinese medicine for the treatment of diarrhea in some regions of China. But up to now, the anti-diarrheal activity of DHP haven't been performed with modern pharmacological technology. This study aims to investigate the quality control, the potential toxicity and anti-diarrheal activity of Dihuang powder in mice. High performance liquid chromatography (HPLC) and thin layer chromatography (TLC) were used to detect five active compounds in DHP for quality control, and the acute toxicity and sub-acute toxicity for 28-day oral administration of DHP were then evaluated. The anti-diarrheal activity was investigated using mouse model. Results showed that the levels of quercetin and berberine in DHP were 0.054 and 0.632 mg/g, respectively, and atractylodin, matrine, and patehouli aleohal were also detected in DHP. At the given doses, DHP was safe in terms of acute and sub-acute toxicity. Meanwhile, DHP exhibited strong anti-diarrheal effects as well as decreased gastrointestinal motility and the secretions induced by Sennae and castor oil in a dose-dependent manner. It could decrease the content of IL-1β, IL-6, and TNF-α in the small intestine, and improve the histopathological changes of small intestine and large intestine induced by Sennae. The antinociceptive and anti-inflammatory activities in vivo also were presented. Based on all of the results, we thought that DHP has anti-diarrheal activity, and could be used to treat diarrhea as well as alleviate the pain and inflammation induced by diarrhea. This study provides a theoretical basis for the clinical use of DHP and may assist in the development of new drugs for the treatment of diarrhea. The mechanism of the anti-diarrheal activity should be investigated in the future.
As important secondary plant metabolites, naphthoquinones exhibit a wide range of biological activities. However, their potential as sustainable alternatives to synthetic acaricides has not been studied. This study for the first time investigates the acaricidal activity of naphthoquinones against Psoroptes cuniculi in vitro. Furthermore, the in vivo activity, the skin irritation effects, the cytotoxicity and the inhibitory activities against mite acetylcholinesterase (AChE) and glutathione S-transferase (GST) of the two compounds that displayed the best insecticidal activity in vitro were evaluated. Among fourteen naphthoquinones and their analogs, juglone and plumbagin were observed to possess the strongest acaricidal activities against P. cuniculi with LC50 values of 20.53 ppm and 17.96 ppm, respectively, at 24 h. After three treatments, these two chemicals completely cured naturally infested rabbits in vivo within 15 days, and no skin irritation was found in any of the treated rabbits. Compared to plumbagin, juglone presented no or weak cytotoxicity against HL-7702 cells. Moreover, these two chemicals significantly inhibited AChE and GST activity. These results indicate that juglone has promising toxicity against P. cuniculi, is safe for both humans and animals at certain doses, and could be used as a potential alternative bio-acaricide for controlling the development of psoroptic mange in agricultural applications.
Seven phenolic compounds, <b>1</b> - <b>7</b>, including a new organic acid gallate, mucic acid 1-ethyl 6-methyl ester 2-<i>O</i>-gallate (<b>7</b>), were isolated from the MeOH extract of the fruits of <i>Phyllanthus emblica</i> L. (Euphorbiaceae). The structures were elucidated on the basis of extensive spectroscopic analysis and comparison with literature data. Upon evaluated for their antioxidant abilities by 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2′-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS), and ferric reducing antioxidant power (FRAP) assays. The inhibitory activities against melanogenesis in B16 melanoma cells induced by <i>α</i>-MSH, as well as cytotoxic activities against four human cancer cell lines were also evaluated. All phenolic compounds, <b>1</b> - <b>7</b>, exhibited potent antioxidant abilities (DPPH:<i> IC</i><sub>50</sub> 5.6 - 12.9 μm; ABTS: 0.87 - 8.43 μm <i>Trolox</i>/μm; FRAP: 1.01 - 5.79 μm Fe<sup>2+</sup>/μm, respectively). Besides, <b>5</b> - <b>7</b>, also exhibited moderate inhibitory activities against melanogenesis (80.7 - 86.8% melanin content), even with no or low toxicity to the cells (93.5 - 101.6% cell viability) at a high concentration of 100 μm. Compounds <b>1</b> - <b>3</b> exhibited cytotoxic activity against one or more cell lines (<i>IC</i><sub>50</sub> 13.9 - 68.4%), and compound <b>1</b> with high tumor selectivity for A549 (<i>SI</i> 3.2).
Addicted drugs like nicotine affect autonomic nervous system that results in arrhythmia and other cardiovascular diseases. Notable effects of Zen meditation on autonomic nervous system have been reported during the past decade. Holistic Detox Association (HDA) in Taiwan offered Zen-meditation program to drug addicts as the core scheme among a variety of drug addiction treatments. This paper reports the results of quantifying the cardiorespiratory interactions and autonomic nervous system function to evaluate the on-site effect of Zen meditation on drug rehab. Methods and schemes for quantifying time-domain heart rate variability were employed to electrocardiograph and respiratory signals. Peak-valley method was developed to quantify the respiratory sinus arrhythmia (RSA) behavior. Poincaré Plot Analysis was adopted to evaluate the cardiorespiratory functioning. Among 18 voluntary drug addicts during the 10-minute Zen meditation session, about two-third subjects have significant improvement in autonomic nervous system function characterized by heart rate variability (SDNN, RMSSD and pNN50). Group average of RSA increases from 33.43 ms(Rest) to 69.14 ms(AR Zen meditation). Poincaré-plot analysis reveals the improvement of SD1, SD2 and SD2/SD1 by respectively 14.7%, 19.8% and 8.8%. The group averages of all the parameters exhibit significantly positive changes in the 10-minute session of abdominal-respiration Zen meditation. Even the subject with heart transplant showed the improvement of all the quantitative indicators during the AR Zen meditation.
To study the effect of Tibetan medicine Zuotai on the activity, protein and mRNA expression of CYP1A2 and NAT2, three different doses (1.2, 3.8 and 12 mg x kg(-1)) of Zuotai were administrated orally to rats once a day or once daily for twelve days, separately. Rats were administrated orally caffeine (CF) on the second day after Zuotai administration, and the urine concentration of CF metabolite 5-acetylamino-6-formylamino-3-methyl-uracil (AFMU), 1-methyluric acid (1U), 1-methylxanthine (1X), 1, 7-dimethylxanthine (17U) at 5 h after study drug administration was determined by RP-HPLC. The activity of CYP1A2 and NAT2 was evaluated by the ratio of metabolites (AFMU+1X+1U)/17U and the ratio of AFMU/(AFMU+1X+1U), respectively. The protein and mRNA expression of CYP1A2 and NAT2 were determined by ELISA and RT-PCR method, respectively. After single administration of Zuotai 3.8 mg x kg(-1) and repeated administration of Zuotai 3.8 and 12 mg x kg(-1), the activity of CYP1A2 and NAT2 decreased significantly compared with control group and there was no significant difference between other dose group and control group. The protein expression of CYP1A2 was significant lower than that in control group after repeated administration of Zuotai 12 mg x kg(-1), and the mRNA expression of CYP1A2 decreased significantly compared with that of control group after single administration of Zuotai 3.8 mg x kg(-1) and repeated admistration of Zuotai 12 mg x kg(-1), separately. The protein expression of NAT2 decreased significantly compared with that of control group after single and repeated administration of Zuotai 3.8 mg x kg(-1), respectively, and the mRNA expression of CYP1A2 decreased significantly compared with control group after single administration of Zuotai 3.8 mg x kg(-1). This study found that Tibetan medicine Zuotai had significant effect on the activity, protein and mRNA expression of CYP1A2 and NAT2.
The genus Adonis L. (Ranunculaceae), native to Europe and Asia, comprises 32 annual or perennial herbaceous species. Due to their cardiac-enhancing effects, Adonis spp. have long been used in European and Chinese folk medicine. These plants have been widely investigated since the late 19th century, when the cardiovascular activity of Adonis vernalis L. was noted in Europe. The present paper provides a review of the phytochemistry, biological activities and toxicology in order to highlight the future prospects of the genus. More than 120 chemical compounds have been isolated, with the most important components being cardiac glycosides as well as flavones, carotenoids, coumarins and other structural types. Plants of the genus, especially A. vernalis L. and A. amurensis Regel & Radde, their extracts and their active constituents possess broad pharmacological properties, including cardiovascular, antiangiogenic, antibacterial, antioxidant, anti-inflammatory and acaricidal activities, and exhibit both diuretic effects and effects on the central nervous system. However, most plants within the 32 species have not been comprehensively studied, and further clinical evaluation of their cardiovascular activity and toxicity should be conducted after addressing the problem of the rapidly decreasing resources. This review provides new insight into the genus and lays a solid foundation for further development of Adonis.
A new xanthone glycoside ( 1 ) has been isolated from Swertia franchetiana together with five known xanthone glycosides. Their structures were elucidated as 7- O -[β- d -xylopyranosyl-(1→2)-β- d -xylopyranosyl]-1,7,8-trihydroxy-3-methoxyxanthone ( 1 ), 7- O -[α- l -rhamnopyranosyl-(1→2)-β- d -xylopyranosyl]-1,7,8-trihydroxy-3-methoxyxanthone ( 2 ), 8- O- β- d -glucopyranosyl-1,3,5,8-tetrahydroxyxanthone ( 3 ), 1- O- β- d -glucopyranosyl-1-hydroxy-3,7,8-trimethoxyxanthone ( 4 ), 1- O -[β- d -xylopyranosyl-(1→6)-β- d -glucopyranosyl]-1-hydroxy-2,3,5-trimethoxyxanthone ( 5 ) and 1- O -[β- d -xylopyranosyl-(1→6)-β- d -glucopyranosyl]-1-hydroxy-3,5-dimethoxyxanthone ( 6 ) on the basis of spectroscopic evidence.
Two new iridoid glycosides designated as senburiside III (2) and senburiside IV (3), together with one known iridoid glycoside senburiside I (1) and three known secoiridoid glucosides swertiamarin (4), gentiopicroside (5) and sweroside (6), were isolated from the whole plant of Swertia franchetiana. The structures of the two new compounds were elucidated by spectroscopic methods.;