Budesonide-liposomes inclusion complex in thermosensitive gel alleviates DSS-induced ulcerative colitis in mice.

PURPOSE: A novel formulation for Ulcerative Colitis (UC) treatment by rectal administration with budesonide liposomes (Bud Lip) and thermosensitive gel (Gel) was developed for future clinical use. To evaluate the anti-inflammatory activity and colon mucosal protection of this novel formulation compared with the other three in mice. METHODS: Bud Lip was prepared by reverse evaporation method and then dispersed in solutions with PL407 and PL188 by a cold method. Male mice were induced to UC by dextran sulfate sodium (DSS) and were treated for 14 days by rectal administration, as follows: Bud enema (a conventional suspension formulation); Bud Lip; Bud Gel; Bud Lip-Gel; saline. And a negative control without colitis was also used. Disease activity index (DAI), and macroscopic and microscopic damage scores in colon tissues were used to evaluate the effect of therapy. The levels of IL-6 and IL-10 in serum and the concentrations of TNF-α and IL-10 and myeloperoxidase (MPO) activity in colon tissue were also introduced. RESULTS: In UC mice model, Bud Lip-Gel showed inflammation was alleviated significantly, and the treatment was highly associated with lower DAI, less macroscopic and microscopic colonic damage and downregulation of pro-inflammatory cytokines TNF-α, IL-6 and MPO. Bud Lip-Gel had advantages over Bud, Bud Lip, Bud Gel in the treatment of active UC. CONCLUSION: Novel Bud liposomes complex in thermosensitive Gel effectively mitigated symptoms, alleviated macroscopic and microscopic colon damage, and reduced inflammatory reaction in UC mice, which might be a potential strategy for UC treatment.

Electroacupuncture improves follicular development and metabolism and regulates the expression of adiponectin, AMPK and ACC in an obese rat model of polycystic ovary syndrome.

BACKGROUND: Polycystic ovary syndrome (PCOS) is a common endocrine disorder characterized by hyperandrogenism and follicular arrest. Electroacupuncture (EA) has been shown to be effective at improving hyperandrogenism and follicular arrest in PCOS; however, its mechanism of action remains to be deciphered. OBJECTIVE: In this study, we investigated whether EA improved follicular development in an obese rat model of PCOS and regulated the expression of adiponectin, AMP-activated protein kinase (AMPK) and acetyl-CoA carboxylase (ACC). METHODS: EA was administered at CV3, CV4 and ST40. Changes in body weight, paraovarian fat, estrus cycle, ovarian morphology, levels of related hormones, and glucose and lipid metabolism were evaluated. In addition, protein and mRNA expression of adiponectin, AMPK and ACC was measured. RESULTS: The body weight and paraovarian fat of rats in the EA group were reduced, while estrus cyclicity and ovarian morphology improved. Levels of free fatty acids, triglycerides, total cholesterol and low-density lipoprotein cholesterol were significantly reduced in the EA group, as well as blood glucose levels. Furthermore, levels of testosterone and luteinizing hormone were reduced in the EA group, while estradiol levels were increased. Protein and mRNA expression of adiponectin, AMPKα1 and liver kinase B1 (LKB1) was found to be increased in the EA group, while protein and mRNA expression of ACC were significantly reduced.Conclusion: Our findings suggest that EA improved follicular development and metabolism and regulated expression levels of adiponectin, AMPKα1, LKB1 and ACC in our obese rat model of PCOS.

Effectiveness of herb-partitioned moxibustion combined with electroacupuncture on polycystic ovary syndrome in patients with symptom pattern of kidney deficiency and phlegm-dampne.

OBJECTIVE: To observe the effect of herb-partitioned moxibustion combined with electroacupuncture on polycystic ovary syndrome (PCOS) in patients with symptom pattern of kidney deficiency and phlegm-dampness. METHODS: Totally 62 PCOS patients who met the inclusion criteria were randomly divided into intervention group and control group. In the intervention group, acupoints were subjected to (43 ± 1) ℃ herb-partitioned moxibustion and electroacupuncture treatment. In the control group, acupoints were subjected to (37 ± 1) ℃ herb-partitioned moxibustion and sham electroacupuncture treatment. Treatment was provided 3 times per week for 12 weeks, and the treatment was stopped during menstruation. After the treatment, the clinical efficacy, the Traditional Chinese Medicine (TCM) symptom pattern score, basal body temperature (BBT) levels, menstrual cycle, and related sex hormone levels of the two groups were evaluated. RESULTS: Sixty patients were eventually included in the study (30 in the intervention group and 30 in the control group). There were not obvious between-group differences in the baseline efficacy parameters (all P > 0.05). (a) After treatment, the two groups have improved in terms of clinical efficacy, TCM symptom pattern score, menstrual cycle and, BBT (P < 0.01, < 0.05), and the intervention group was better than the control group (P < 0.01, < 0.05). (b) In the intervention group, the estradiol (E2) and P450 aromatase (P450arom) levels were increased (all P < 0.05), the testosterone (T) level was decreased (P < 0.05), and the luteotropic hormone (LH) and anti-Müllerian hormone (AMH) levels were significantly decreased (P < 0.01). In the control group, E2 level was increased (P < 0.05), and LH level was decreased (P < 0.05). After treatment, the T, LH, and AMH levels of the intervention group were decreased compared with those of the control group (all P < 0.05), and the P450arom level was increased (P < 0.05). CONCLUSIONS: Herb-partitioned moxibustion combined with electroacupuncture can effectively improve the related clinical symptoms of PCOS patients with kidney deficiency and phlegm-dampness. Herb-partitioned moxibustion combined with electroacupuncture may inhibit the overexpression of AMH to increase the expression level of P450arom in ovarian granulosa cells, thereby reconstructing the dependence of follicular development on FSH, and finally improving abnormal follicular development and hyperandrogenism in PCOS patients with kidney deficiency and phlegmdampness. TRIAL REGISTRATION NUMBER: ChiCTR1900024182.

Quantitative LC-MS/MS analysis of seven ginsenosides and three aconitum alkaloids in Shen-Fu decoction.

BACKGROUND: Shen-Fu decoction is a traditional Chinese medicine prescription with a 3:2 ratio of Radix Ginseng and Fuzi (Radix Aconiti lateralis praeparata). Ginsenosides and alkaloids are considered to be the main active components of Shen-Fu decoction. However, no analytical methods have been used to quantitatively analyse both components in Shen-Fu decoction simultaneously. RESULTS: We successfully developed a rapid resolution liquid chromatography coupled with tandem mass spectrometry (RRLC-MS/MS) method for the simultaneous analysis of seven ginsenosides and three aconitum alkaloids in Shen-Fu decoction, the decoction of Radix ginseng and Fuzi (Radix Aconiti lateralis praeparata). Chromatogrpahic separation by RPLC was achieved using a reversed-phase column and a water/acetonitrile mobile phase, containing 0.05% formic acid and using a gradient system. The method was optimized to allow for simultaneous analysis of all analytes in 11minutes without the need for baseline resolution of the components. Furthermore, the separation demonstrated good linearity (r > 0.9882), repeatability (RSD < 7.01%), intra- and inter-day precisions (RSD < 5.06%) and high yields of recovery (91.13-111.97%) for ten major constituents, namely ginsenoside-Re, Rg1, Rb1, Rc, Rb2, Rd, Rf, aconitine, hypacoitine and mesaconitine. CONCLUSIONS: The developed method could be used as a rapid and reliable approach for assessment of the quantity of the major constituents in Shen-Fu decoction.

[Effect of electroacupuncture at "Zusanli" (ST 36) and "Sanyinjiao" (SP 6) on collagen-induced arthritis and secretory function of knee-joint synoviocytes in rats].

OBJECTIVE: To observe the effect of electroacupuncture (EA) of "Zusanli" (ST 36) and "Sanyinjiao" (SP 6) on collagen-induced arthritis (CIA) and its underlying mechanism in regulating the secretory function of knee-joint synovial cells in CIA rats. METHODS: Thirty-six Wistar rats were equally randomized into control, model and EA groups. CIA model (rheumatoid arthritis) was duplicated by intradermal injection of Bovine type II collagen into the back of the anesthetized rats. EA (2 Hz, 2 mA) was applied to "Zusanli" (ST 36) and "Sanyinjiao" (SP 6) for 30 min, once a day for 30 days. The paw volume was measured by using a Plethysmometer and hot water tail-flick tests (50 degrees C) were conducted for detecting the rats' pain threshold (PT) before and after the treatment. The contents of PGE2, IL-1beta and TNF-alpha in supernatant of the cultured joint synoviocytes were detected by enzyme linked immunosorbent assay (ELISA). RESULTS: In comparison with control group, the swelled paw volume, the declined PT, PGE2, TNF-alpha and IL-1beta contents in knee-joint synoviocyte supernatant were significantly higher in model group (P < 0.05). Compared with model group, PT increased obviously (P < 0.05); paw volume, supernatant PGE2, TNF-alpha and IL-1beta contents decreased obviously (P < 0.05) in EA group. CONCLUSION: EA of ST 36 and SP 6 has a pronounced therapeutic effect in relieving knee joint pain and inflammation in CIA rats, which may be related to its effect in regulating the secretory function of the knee-joint synoviocytes.

[Effects of transcutaneous electric acupoint stimulation on plasma SOD and MDA in rats with sports fatigue].

OBJECTIVE: To observe the effect of transcutaneous electric acupoint stimulation (TEAS) on plasma superoxide dismutase (SOD) and malondialdehyde (MDA) in rats with sports fatigue so as to explore its mechanisms in resisting exercise-induced fatigue. METHODS: Twenty-seven male adult SD rats were randomly divided into control group (n 9), model group (n=9) and TEAS group (n=9). Sports fatigue model was established by using treadmill method, i.e. forcing the rat to run 10 min at a speed of 10 m/min, 15 m/min, 20 m/min, 24 m/min and 28 m/min, once daily for 6 days. TEAS (continuous waves, 2 Hz, 5 mA) was applied to unilateral "Zusanli" (ST 36) for 30 min, once per day for 7 days. The exhausted exercise time from starting running to exhaustion was recorded on the 7th day and the lactate levels, SOD activity and MDA contents in plasma were measured by lactate oxidase method, xanthine oxidase method and thiobarbituric acid method respectively. RESULTS: The duration of exhausted exercise in model group and TEAS group were (56.00 +/- 12.27) min and (70.88 +/- 13.74) min respectively, displaying significant increase in exercise tolerance after TEAS (P<0.05). The lactate level and MDA content in model group were markedly higher than those in control group (P<0.05); while compared with model group, lactate and MDA contents in TEAS group were significantly lower (P<0.05), and plasma SOD activity in TEAS group was significantly higher (P<0.01). No significant differences were found in plasma lactate content between control and TEAS groups and in SOD activity between model group and control group (P>0.05). SOD/MDA of model group was significantly lower than those of control group and TEAS group (P<0.05, 0.01). CONCLUSION: TEAS at "Zusanli"(ST 36) can effectively postpone exercise-induced fatigue by reducing accumulation of blood lactate, improving anti-oxidative ability and relieving lipid peroxidation in the rat.