The prerequisites and clinical outcomes of ipsilateral C7 nerve root transfer to the upper trunk for adult C5-C6 brachial plexus injuries.

PURPOSE: Although ipsilateral C7 nerve transfer is used for the treatment of C5-C6 brachial plexus injuries, accurately evaluating the functional quality of the donor nerve (ipsilateral C7 nerve root) is difficult, especially when the C7 nerve root is slightly injured. The purpose of this study was to determine the indicators to evaluate the quality of the ipsilateral C7 nerve and assess the clinical outcomes of this procedure. METHODS: This study employed the following three indicators to assess the quality of the ipsilateral C7 nerve: (1) the muscle strength and electrophysiological status of the latissimus dorsi, triceps brachii, and extensor digitorum communis; (2) the sensibility of the radial three digits, especially the index finger; and (3) the intraoperative appearance, feel and electrophysiological status of the ipsilateral C7 nerve root. Transfer of the ipsilateral C7 nerve root to the upper trunk was implemented only when the following three tests were conducted, the criteria were met, and the clinical outcomes were assessed in eight patients with C5-C6 brachial plexus injuries. RESULTS: Patients were followed-up for an average of 90 ± 42 months. At the final follow-up, all eight patients achieved recovery of elbow flexion, with five and three patients scoring M4 and M3, respectively, according to the Medical Research Council scoring. The shoulder abduction range of motor recovery averaged 86 ± 47° (range, 30°-170°), whereas the shoulder external rotation averaged 51 ± 26° (range, 15°-90°). CONCLUSION: Ipsilateral C7 nerve transfer is a reliable and effective option for the functional reconstruction of the shoulder and elbow after C5-C6 brachial plexus injuries when the three prerequisites are met.

[Common diseases and drug use characteristics of Chinese herbal medicines and suggestions].

Based on the data of 56 kinds of diseases and drug use in 100 kinds of cultivated Chinese herbal medicines, this paper used frequency analysis method to count the types of diseases and their drug use characteristics, and systematically analyzed the status of drug registration and monitoring standards for disease prevention and control of Chinese herbal medicines. The results showed that 14 diseases such as root rot, powdery mildew, and drooping disease were common in the production of Chinese herbal medicines. Among the 99 pesticides reported, 67.68% were chemically synthesized, 23.23% were biological pesticides, and 9.09% were mineral pesticides. Among the reported pesticides, 92.93% of them were low toxic, with relative safety. However, 70% of the production drugs were not registered in Chinese herbal medicines, and the phenomenon of overdose was serious. The current pesticide residue monitoring standards does not match well with production drugs in China. Although the matching degree between Maximum Residue Limit of Pesticide in Food Safety National Standard(GB 2763-2021) and production drugs is more than 50%, there are few varieties of Chinese herbal medicines covered. The matching degree between Chinese Pharmacopoeia(2020 edition), Green Industry Standard of Medicinal Plants and Preparations(WM/T2-2004), and production drugs is only 1.28%. It is suggested to speed up the research and registration of Chinese herbal medicine production and further improve the pesticide residue limit standard combined with the actual production, so as to promote the high-quality development of Chinese herbal medicine industry.

Two pairs of epimers and three undescribed diterpenoids from Pseudocaryopteris paniculata.

A phytochemical investigation on the petroleum ether partition of the whole plant of Pseudocaryopteris paniculata, yield seven new compounds: one phytanes diterpenoid (2Z,6E,10E) 14-keto-2,6,10-trimethyl pentadeca-2,6,10-trien-1-carboxylic acid (1), five clerodane diterpenoids: paniculatins A-E (2, 3a/3b, 4a/4b), one abietane diterpenoid: ent-uncinatone (5), together with 12 known compounds. Their structures were elucidated on the basis of 1D and 2D Nuclear Magnetic Resonance （NMR_, Infrared Radiation (IR), and mass spectroscopic data. Compound 2, 5, and 11 showed weak selective cytotoxic activity of 11 human cancer cell lines.

Combined Nerve and Tendon Transfers for C7-T1 Brachial Plexus Avulsion Injury.

BACKGROUND: In patients with C7-T1 brachial plexus avulsions, complete loss of hand function is commonly seen. However, the reconstruction of hand function is difficult. OBJECTIVE: To report the outcomes of hand function recovery after combined nerve and tendon transfers in C7-T1 brachial plexus injury. METHODS: From 2012 to 2019, 8 patients with C7-T1 brachial plexus injury underwent combined nerve and tendon transfers for hand function restoration, which included the following: (1) the pronator teres motor branch to the anterior interosseous nerve and brachialis motor branch to the flexor digitorum superficialis branch for finger flexion, (2) the supinator motor branch to the posterior interosseous nerve for finger extension, (3) the brachioradialis tendon transfer for thumb opposition, and (4) the radial branch of the superficial radial nerve to the sensory branch of the ulnar nerve for sensory reconstruction. Patients were evaluated for functional improvement of finger flexion, finger extension, thumb opposition, and sensory recovery. RESULTS: No clinical donor deficits were observed. Seven of eight patients recovered finger and thumb flexion (4 patients scored British Medical Research Council grade M4 and 3 scored M3). The average grip strength was 3.4 kg. All patients regained finger extension (4 scored M4 and 4 scored M3), thumb opposition, and protective sensation on the ulnar hand. Patients were able to use their reconstructed hands in daily lives. CONCLUSION: Combined nerve and tendon transfers are reliable and effective. This strategy could be an option for hand function reconstruction after C7-T1 brachial plexus injury.

Acylated iridoid glucosides from Pseudocaryopteris paniculata (C.B.Clarke) P.D.Cantino.

Phytochemical investigation of the ethyl acetate fraction of Pseudocaryopteris paniculata C.B.Clarke P.D.Cantino resulted in the identification of 26 undescribed iridoid glucosides (paniculosides A-Z), along with 7 known iridoid glucosides. Their structures were elucidated via two-dimensional nuclear-magnetic-resonance (2D-NMR) spectroscopy, high-resolution electrospray ionization mass spectroscopy (HR-ESI-MS), and chemical-hydrolysis methods. All isolated substances were analyzed for their cytoprotective effects against t-BHP-induced toxicity in HepG2 cells. Among the tested compounds, paniculoside A, paniculoside I, paniculoside T, and paniculoside U exhibited moderate cytoprotective activities with IC50 values in the range of 11.72-34.22 µM against t-BHP-induced toxicity.

Cytotoxic Diterpenoids from Caryopteris aureoglandulosa.

Seven new (1-7) and 11 known diterpenoids were isolated and identified from Caryopteris aureoglandulosa. These diterpenoids were structurally determined by HRESIMS and NMR spectroscopic analyses, single-crystal X-ray diffraction, and ECD data. Structurally, aureoglandulosin A (1) is a highly oxygenated abietane diterpenoid with an unprecedented 7/6/6/5-ring system. Aureoglandulosins B (2) and C (3) represent naturally occurring new diterpenoids with an unusual 6/6/6/5-ring system. Additionally, the configurations of two known abietane diterpenoids 11 and 12 were determined by X-ray crystallographic data analysis for the first time. A plausible biosynthetic pathway for compounds 1-3 is proposed. The cytotoxicity of all isolates was evaluated, and compounds 1 and 11 exhibited significant cytotoxic activity against some cell lines with IC50 values in the range 1.6-8.2 µM.

The impact of social capital on physical activity and nutrition in China: the mediating effect of health literacy.

BACKGROUND: Physical activity and good nutrition are important behavioral factors in promoting health and preventing disease. It is important to understand the factors affecting physical activity and nutrition. The purpose of this study was to explore whether social capital has an effect on physical activity and nutrition, and whether health literacy plays a mediating role between social capital and physical activity as well as nutrition. METHODS: This cross-sectional study was performed in a certain district of Shanghai in March and April 2017. Data was collected using a self-reported questionnaire, which included questions on sociodemographic characteristics, social capital, health literacy and health-promoting lifestyle profile-II. Health-promoting lifestyle profile-II measures the behaviours or habits of physical activity and healthy nutrition. An explore factor analysis of the principal components with varimax rotation was carried out on the social capital scale. Descriptive statistics was used to summarize the sociodemographic of participants. Mediation analysis was performed using the bootstrapping tests to examine whether health literacy mediate the relationship between social capital and physical activity as well as nutrition. RESULTS: The explore factor analysis results showed that social capital has five dimensions, namely social participation, social support, social network, control over life and feelings about the community. There is a positive correlation between social capital, health literacy, physical activity and nutrition. The correlation coefficient varied from 0.135 to 0.594. Mediation analysis demonstrated health literacy played a partial mediating effect between social capital and physical activity as well as nutrition. In the relationship between physical activity and social capital, the indirect effect of health literacy accounted for 8.20 to 12.65% of the total effect. In the relationship between nutrition and social capital, the mediation effect of health literacy accounted for 4.93 to 12.71% of the total effect. CONCLUSION: Social capital can promote physical activity and nutrition by disseminating health information. Enhancing the social capital of residents will help increase physical activity and develop healthy eating habits. Attention should also be paid to the improvement of residents' health literacy.

Gender differences in vascular reactivity of mesenteric arterioles in portal hypertensive and non-portal hypertensive rats.

BACKGROUND: Portal hypertension (PHT) is primarily caused by an increase in resistance to portal outflow and secondarily by an increase in splanchnic blood flow. Vascular hyporeactivity both in systemic circulation and in the mesenteric artery plays a role in the hyperdynamic circulatory syndrome. AIM: To explore gender differences and the role of endogenous sex hormones in PHT and vascular reactivity of mesenteric arterioles in rats. METHODS: Cirrhosis and PHT were established by subcutaneous injection of carbon tetrachloride (CCl4) in both male and female integral and castrated rats (ovariectomized [OVX] in female rats, orchiectomy [ORX] in male rats). The third-order branch of the mensenteric artery was divided and used to measure vascular reactivity to vasoconstrictors. RESULTS: No significant difference in portal pressure was observed between integral and castrated male PHT rats (15.2 ± 2.1 mmHg vs 16.7 ± 2.7 mmHg, P > 0.05). The portal pressure in integral female PHT rats was lower than that in OVX female PHT rats (12.7 ± 2.7 mmHg vs 16.5 ± 2.4 mmHg, P < 0.05). In PHT rats, the concentration response curves of the mesenteric arterioles to norepinephrine were shifted to the right, and the maximal responses (Emax) values were decreased and effective concentrations causing half maximum responses (EC50) values were increased, compared to those of non-PHT rats, both in male and female rats. Compared to non-PHT integral male rats, the sensitivity of the mesenteric arterioles of non-PHT ORX male rats to norepinephrine was decreased (P > 0.05). However, there was no difference between integral and ORX male rats with PHT. In integral female PHT rats, the concentration response curves were shifted to the left (P < 0.05), and the Emax values were increased and EC50 values were decreased compared to OVX female PHT rats. CONCLUSION: Clear gender differences were observed in mesenteric vascular reactivity in CCl4-induced cirrhotic and PHT rats. Conservation of estrogen can retain the sensitivity of the mesenteric arterioles to vasoconstrictors and has a protective effect on splanchnic vascular function in PHT.

[Study on commodity specification and grade standard and quality evaluation of Dipsaci Radix].

Through the records of herbal and market investigations,the samples collected from different market and origin were analyzed,and the appearance character indexes were determined in order to revise the commodity specification and grade standard of Dipsaci Radix combined with production practice. This is also to analyze association of the appearance with quality different of intrinsic components. The investigation results indicated the root's long and thick was better,and atrovirens of fracture surface,there are most of the market is dominated by the ungraded goods. Through principal component analysis,variance analysis and cluster analysis,combining with the feasibility of actual operation and herbal record,the length,middle diameter and phloem color were filtrated and the specification was divided into 2 ranks: the selection and ungraded goods,and the grade was divided into 2 ranks for the selection goods: big,small selected goods. Moreover,there were no significant correlation between the appearance and the intrinsic quality index of Dipsaci Radix,the content of extractum were significantly positive correlation with the moisture,but had extremely negative correlation with the total ash. Multiple comparisons indicated that the content of the moisture,extractum and asperosaponin VI of the selected goods were higher than the ungraded goods,while the total ash content were lower,and they hasn't significant difference. The commodity specification and grade standard of Dipsaci Radix as a basis provide commodity specification and grade standard of communities and standardizing market trade order.

[Research on grade standard and quality evaluation of Pinelliae Rhizoma for merchandise specification].

The study aims at investigating the grade standard and the quality characteristic of Pinelliae Rhizoma for commodity specification, which provides the reference for its grade standard formulation. 42 Pinelliae Rhizoma simples were collected from 5 medicinal materials markets and 2 producing areas. Based on the previous herbalogical study and market investigation, we combined with the data analysis to select the grading indicators using SPSS software for descriptive statistical analysis, analysis of variance, K-cluster analysis and correlation analysis. According to the actual production condition, we developed the grading standards of Pinelliae Rhizoma. Moreover, we compared the internal indicators(water, total ash, leachate and guanosine) of Pinelliae Rhizoma at various grade levels, and analyzed the correlation between appearance traits and internal indicators. The herbalogical study and market research found that the Pinelliae Rhizoma was better in large, solid and white. The results from descriptive and variance analysis showed that the appearance of Pinelliae Rhizoma was significantly different in weight per grain and grain number of 500 g. Referring to the 2015 Chinese Pharmacopoeia and the production practice, we use the length, weight per grain and grain number of 500 g as the classification index of Pinelliae Rhizoma. The results from correlation analysis showed that there was no significant correlation between the appearance of Pinelliae Rhizoma and the intrinsic quality index. In addition, we found there was no significant difference in the content of the intrinsic index except for the total ash and the extract. The current study established the classification index of the product specification and grade standard of Pinelliae Rhizoma with length, weight per grain and grain number of 500 g as the index, which can provide the basis for the classification of the product specification and grade of Pinelliae Rhizoma market.

[Study on commodity specification and grade standard and quality evaluation of Galla Chinensis].

This paper is aimed to study the commodity specification and grade standard of Galla Chinensis,for standardizing market order and guide the market circulation,and provide a basis for standardization of Galla Chinensis. With 33 samples of Galla Chinensis from market as the object of the research,the herbal textual research and market research were carried out. Then the grading indicator were selected by the descriptive statistics,principal component analysis and cluster analysis,combining with production practice,the commodity specification and grade standard of Galla Chinensis were set out. The data of moisture,ash,gallic acid as the internal index were used to analyze the relationship between the quality difference between grades and the appearance characters and the intrinsic composition. Herbal textual research and market research found that the high quality of Galla Chinensis characterized with large,complete,wall thick,grayish brown characteristics,and Galla Chinensis could be divided into gallnuts and horned gall. Through principal component analysis and cluster analysis,combining actual production and herbal record,screening,the length,diameter,single weight,the number of 500 g were determined as 4 grading indicators,the commodity specification was divided into two: gallnuts and horned gall,the grades was divided into two: selected goods and mixed goods. The result of correlation analysis showed there was no significant correlation between the internal index and the appearance characters of Galla Chinensis. The result of multiple comparison showed that the ash content of the selected goods was smaller than that of the mixed goods,but it did not reach significant. The content of gallic acid of the selected goods and the mixed goods of gallnuts were higher than selected goods of horned gall,and higher than mixed goods of horned galls. Using the length,diameter,single weight,the number of 500 g as the appearance characters index. Combining with the herbal textual research and market research,we have divided two specifications and two grades for the commodity specification and grade standard of Galla Chinensis,which can provide a basis for industry standards and national standards.

Phenylethanoid glycosides from the Schnabelia nepetifolia (Benth.) P.D.Cantino promote the proliferation of osteoblasts.

An investigation of the n-BuOH fraction of Schnabelia nepetifolia (Benth.) P.D.Cantino led to the isolation and identification of 12 undescribed phenylethanoid glycosides (nepetifosides A-L) and one undescribed phenylmethanoid glycoside (nepetifoside M), together with 23 known compounds. The structures of these compounds were determined by spectroscopic analyses including two-dimensional nuclear-magnetic-resonance (2D-NMR) spectroscopy and chemical-hydrolysis methods. Nepetifoside F exhibited strong activity that significantly increased osteoblast proliferation at three concentrations of 0.1, 1, and 10 µM. Moreover, nepetifoside C and nepetifoside D exhibited moderate activities in promoting the proliferation of osteoblasts at medium and high concentrations of 1 µM and 10 µM, respectively.

Four new sesquiterpenoids with anti-inflammatory activity from the stems of Jasminum officinale.

Four new sesquiterpenoids，including three nor-cinalbicane type sesquiterpenoids, named Jasminol A, G, H (1-3) and one eremophilene-type sesquiterpenoid, named Jasminol B (4) together with nine known compounds (5-13) were isolated from the stems of Jasminum officinale L. The structures of new compound were elucidated on the base of IR, HR-ESI-MS, 1D NMR, 2D NMR and DEPT analysis, and the absolute configurations were determined by single-crystal X-ray diffraction analysis. In addition, the anti-inflammatory activity of isolated compounds was evaluated using lipopolysaccharide (LPS)-induced murine macrophage RAW264.7, and compounds 1-4 exhibited a moderate inhibition of LPS-induced nitric oxide (NO) production in RAW264.7 cells with IC50 values of 20.56 ±â€¯1.31, 30.12 ±â€¯0.89, 30.35 ±â€¯2.72 and 31.60 ±â€¯1.69 µM, respectively, and CC50 values >200 uM.

Caryopincaolide M, a rearranged abietane diterpenoid with new skeleton and a new iridoid from Caryopteris incana.

Caryopincaolide M (1), a new rearranged abietane diterpenoid with an unusual pent-4-enoic acid group on a 6/6/5 tricyclic ring system, and 7-epi-8-dehydroxypatriscabrol (3), a new iridoid, together with 17 known compounds, have been isolated from the whole plant of Caryopteris incana (Thunb.) Miq. Their structures were elucidated on the basis of 1-D and 2-D NMR, IR, and mass spectroscopic data. Compounds 1-5 were evaluated for their inhibitory activities against enzyme α-glucosidase, and the results showed that only 1 has moderate inhibitory activity against enzyme α-glucosidase with IC50 at 528.3 ± 12.37 mg/L.

Surgical treatment for severe cubital tunnel syndrome with absent sensory nerve conduction.

For severe cubital tunnel syndrome, patients with absent sensory nerve action potential tend to have more severe nerve damage than those without. Thus, it is speculated that such patients generally have a poor prognosis. How absent sensory nerve action potential affects surgical outcomes remains uncertain owing to a scarcity of reports and conflicting results. This retrospective study recruited one hundred and fourteen cases (88 patients with absent sensory nerve action potential and 26 patients with present sensory nerve action potential) undergoing either subcutaneous transposition or in situ decompression. The minimum follow-up was set at 2 years. Primary outcome measures of overall hand function included their McGowan grade, modified Bishop score, and Disabilities of the Arm, Shoulder, and Hand Questionnaire (DASH) score. For patients with absent sensory nerve action potential, 71 cases (80.7%) achieved at least one McGowan grade improvement, 76 hands (86.4%) got good or excellent results according to the Bishop score, and the average DASH score improved 49.5 points preoperatively to 13.1 points postoperatively. When compared with the present sensory nerve action potential group, they showed higher postoperative McGowan grades and DASH scores, but there was no statistical difference between the modified Bishop scores of the two groups. Following in situ decompression or subcutaneous transposition, great improvement in hand function was achieved for severe cubital tunnel syndrome patients with absent sensory nerve action potential. The functional outcomes after surgery for severe cubital tunnel syndrome are worse in patients with absent sensory nerve action potential than those without. This study was approved by the Ethical Committee of Huashan Hospital, Fudan University, China (approval No. 2017142).

[Genetic diversity and quality analysis of Rehmannia glutinosa in different germplasm].

The study aims at evaluating genetic diversity and medicinal quality of cultivated germplasm in Rehmannia glutinosa, and providing theoretical guidance for screening excellent germplasm. The genetic diversity of 21 species of R. glutinosa were analyzed by SRAP molecular markers, and the catalpol and verbascoside was determined by HPLC. The mass fraction of catalpol and verbascoside in R. glutinosa germplasm were respectively in the range of 2.393%-6.519% and 0.063%-0.478%, the germplasm 14, 16, 15 and 20 germplasm, witch catalpol and verbascoside content was higher. A total of 57 bands were produced by 10 primer, among which 40 polymorphic bands were polymorphic bands, and the percentage of polymorphic loci was 8.77%-54.39%, the Nei's genetic diversity index (H) was 0.374 1, Shannon's polymorphism information index (I) was 0.546 6. Gst and gene flow Nm were 0.608 8 and 0.321 3, respectively. Based on the genetic uniformity, 21 species of germplasm were grouped into 2 categories. The genetic diversity level of R. glutinosa was medium low. The comprehensive consideration of the genetic diversity and the content inculde catalpol and verbascoside, germplasm 7 and germplasm 18 could be used as the preferred materials for the cultivation of reticulum. Germplasm 15 and 16 can be used as the preservation and breeding object of rhubarb germplasm.

The associations of comorbidities and consumption of fruit and vegetable with quality of life among stomach cancer survivors.

BACKGROUND: Stomach cancer survivors (SCS) often carry the dual burden of the cancer itself and other comorbidities; meanwhile, they are highly motivated to seek health advice about lifestyles to improve their health and quality of life (QOL). The associations of the comorbidity and the consumption of vegetable and fruit with QOL remain even less clear among the SCS. This study aimed to investigate the associations of comorbidities and consumption of fruit and vegetable with QOL among SCS. METHODS: A cross-sectional study was conducted among 969 SCS between April and July 2015 in Shanghai, People's Republic of China. Data were collected using a self-reported questionnaire, which included questions on sociodemographic characteristics, comorbidities and fruit and vegetable consumption, and a simplified Chinese version of the European Organization for Research and Treatment quality of life version 3 (EORTC QLQ-C30) questionnaire. In order to mitigate the bias caused by confounding factors, multiple linear regression models were employed to calculate the adjusted means of QOL scores. RESULTS: The proportion of participants without any comorbidity was only 23.3%, and the most common comorbidity among SCS was digestive diseases (49.8%). Participants with comorbidity generally reported lower scores for global health and functioning subscales and higher scores for symptom in EORTC QLQ-C30 compared to participants without comorbidity, indicating poorer QOL. Higher scores in most functioning subscales and lower scores in some symptoms subscales were found in participants (38.7%) who ate more than 250 g vegetables every day, compared to participants with less vegetable consumption, and in participants (58.1%) who ate fruit every day, compared to participants who didn't eat fruit every day indicating better QOL. CONCLUSIONS: The comorbidities are common health problems among SCS and have significantly negative influence on QOL, and participants with comorbidities generally reported lower QOL scores. The enough vegetables and fruit consumption are positively associated with QOL of SCS. These findings suggested that a multidisciplinary team approach and a variety of delivery systems are needed to address the medical, psychosocial, and lifestyle components for enriching patient-centered care among SCS.

[Effect of propofol and operative trauma on neurodevelopment and cognitive function of developing brain in rats].

OBJECTIVE: To investigate the effect of propofol and operative trauma on the neurodevelopment and cognitive function of the developing brain and its mechanism. METHODS: A total of 104 postnatal day 13 Sprague-Dawley rats were randomly divided into 4 groups: control group (treated by 7.5 mL/kg saline and sham surgery), propofol group (treated by 75 mg/kg propofol), surgery group (with abdominal surgery under local anesthesia) and propofol+surgery group (with abdominal surgery under local anesthesia plus 75 mg/kg propofol anesthesia). Thirteen rats from each group were randomly selected for detecting the content of TNF-α in the hippocampus and the expression levels of caspase-3 and c-fos in the brain. Morris Water Maze test was used to detect the cognitive ability of the other rats at 60 days old, after which TNF-α content in the hippocampus and caspase-3 and c-fos expressions in the brain were detected. RESULTS: In 13 day-old rats, TNF-α level and caspase-3 and c-fos expressions differed significantly between the surgery group and the other 3 groups (P<0.05) and were similar among the control group, propofol group and propofol+surgery group (P>0.05). In 60-day-old rats, Morris water maze test results, TNF-α level or expressions of caspase-3 and c-fos showed no significant differences among the 4 groups. CONCLUSION: Abdominal surgery can induce inflammation in the hippocampus and neuroapoptosis in neonatal rats rather than adult rats. Single-dose propofol anesthesia does not significantly affect neurodevelopment of young rats, and can relieve central inflammatory reaction induced by surgical trauma.

Estrogen receptor ß selective agonist ameliorates liver cirrhosis in rats by inhibiting the activation and proliferation of hepatic stellate cells.

BACKGROUND AND AIM: The aim of this study is to explore the roles of estrogen receptor (ER) subtypes and corresponding agonists/antagonists on the development of cirrhosis and activation and proliferation of hepatic stellate cells (HSCs). METHODS: Carbon tetrachloride (CCl4 )-induced cirrhotic ovariectomized rats were administered non-selective ER agonist (ß-estradiol, E2), ER selective agonists (ERα agonist, propylpyrazoletriol; ERß agonist, diarylpropionitrile [DPN]; and G-protein-coupled ER [GPER] agonist, G1), or E2 + ER selective antagonists (ERα antagonist, MPP; ERß antagonist, PHTPP; and GPER antagonist, G15) for 12 weeks. The expression of the three ER subtypes in livers and HSCs and the effects of the drugs on hepatic fibrosis, isolated HSCs, and uteri were evaluated. RESULTS: Selective ER agonists/antagonists had various effects on CCl4 -induced cirrhosis. The cirrhotic rats in the CCl4  + E2, CCl4  + DPN, CCl4  + E2 + MPP, and CCl4  + E2 + G15 groups presented reduced fibrosis scores, compared with those in the CCl4 group. The cirrhotic rats in the E2 + PHTPP group presented increased fibrosis scores that similar to those in the CCl4 group. The ovariectomized rats had enlarged uteri with increased uterus indexes after E2 administration; however, the proliferative effects of E2 were partially blocked by MPP or G15, but not PHTPP. In the in vitro study, DPN attenuated the transformation of quiescent HSCs to activated phenotype, suppressed collagen I, and α-smooth muscle actin expression. DPN also suppressed platelet-derived growth factor-induced proliferation in cultured HSCs, which was reversed by PHTPP. CONCLUSIONS: The antifibrogenic effects of estrogen were mediated by ERß but not ERα or GPER. The ERß selective agonist exerted a fibrosuppressive effect by inhibiting the activation and proliferation of HSCs, but did not induce uterine hyperplasia.

A new highly oxygenated pregnane and two new 5-hydroxymethylfurfural derivatives from the water decoction of Poria cocos.

A new highly oxygenated pregnane steroid, pregn-7-ene-2ß,3α,15α,20-tetrol (1) and two new 5-hydroxymethylfurfural derivatives, (5-formylfuran-2-yl)methyl 2-hydroxypropanoate (2) and (5-formylfuran-2-yl)methyl 2-(4-hydroxyphenyl)acetate (3), together with four known compounds, were isolated from the water decoction of Poria cocos. Their structures were established on the basis of extensive spectroscopic analysis. Compound 1 showed moderate inhibitory activity and a known compound (3S,6S)-3-[(1R)-1-hydroxyethyl]-6-(phenylmethyl)-2,5-piperazinedione (5) showed weak inhibitory activity against α-glucosidase, respectively.