Three butylphthalide derivatives from the Rhizome of Ligusticum chuanxiong / 药学学报

Three butylphthalide derivatives were isolated from the Rhizome of Ligusticum chuanxiong using a series of isolation and purification approaches including macroporous resin, ODS-A column, Sephadex LH-20 and preparative HPLC. These structures were elucidated based on extensive spectroscopic data (UV, IR, HR-ESI-MS and NMR) and identified as (3Z,3aE)-(6R,7R,2'S)-6-hydroxy-7-(2-carboxyl-2-hydroxyethylthio)-3-(2-hydroxybutylidene)-4,5,6,7-tetrahydro-phthalide (1), (3Z,3aZ)-3-butylidene-6,7-dihydroxy-4,5,6,7-tetrahydro-phthalide 7-O-α-D-glucopyranosyl-(1→2)-β-D-fructo-furanoside (2) and 3-(3-β-D-glucopyranosyloxy-butylidene)-7-hydroxy-phthalide (3).

Two new flavanone glucosides identified in Glycyrrhiza uralensis / 药学学报

Two flavanone glucosides were isolated from the 80% ethanol extract of Glycyrrhiza uralensis using various chromatographic techniques, including macroporous adsorbent resin, RP-C18, Sephadex LH-20, MCI and preparative HPLC. On the basis of chemical properties and spectra data, these compounds were identified as (2S)-liquiritigenin-4'-O-β-D-glucopyranosyl-(1→6)-O-β-D-glucopyranoside (1), (2R)-liquiritigenin-4'-O-β-D-glucopyranosyl-(1→6)-O-β-D-glucopyranoside (2), respectively. Compounds 1 and 2 are new compounds, and their aglycones are enantiomers.

A new neolignan from the fruits of Arctium lappa L / 药学学报

In our study of the chemical constituents of the dried mature fruits of Arctium lappa L., ten compounds were isolated by various chromatography methods and preparative HPLC. Their structures were elucidated as (7R,8R)-4,7,9,9'-tetrahydroxy-3,3'-dimethoxy-8-4'-oxyneolign-7'-ene-9'-O-β-D-glucopyranoside (1), (7R,8R)-4,7,9,9'-tetrahydroxy-3,3'-dimethoxy-8-O-4'-neolignan-9'-O-β-D-glucopyranoside (2), (7R,8R)- 4,7,9,9'-tertahydroxy-3,3'-dimethoxy-8-4'-oxyneolignan (3), (7S,8R)-dihydrodehydrodiconiferylalcohol-4-O-β- D-glucopyranoside (4), (7S,8R,7'R,8'R)-pinoresinol-4,4'-di-O-β-D-glucopyranoside (5), (8S,7'S,8'R)-4,4',9'- trihydroxy-3,3'-dimethoxy-7',9-epoxylignan-7-oxo-4'-O-β-D-glucopyranoside (6), 2-methoxy-4-hydroxyphenol- 1-O-β-D-xylopyranosyl-(1→6)-O-β-D-glucopyranoside (7), 3-methoxy-4-hydroxyphenol-1-O-β-D-xylopyranosyl- (1→6)-O-β-D-glucopyranoside (8), 4-hydroxy-3-methoxybenzylalcohol-4-O-β-D-xylopyranosyl-(1→6)-O-β-D- glucopyranoside (9) and 2-phenethyl β-primeveroside (10) by their spectroscopic data (IR, UV, CD, MS, HR-ESI-MS, and 1D and 2D NMR) and comparison to literature data. Compound 1 is a new 8-O-4'-neolignan. Compounds 2-10 were isolated from the dried mature fruits of Arctium lappa L. for the first time.

Prescription of Jingdan Yimin for treatment of metabolic syndrome / 中国中药杂志

Based on the theory of traditional Chinese medicine, modern methods for drug investigation such as molecular targets in vitro and effects in vivo were used to study the prescription of Jingdan Yimin(JD), including selection of raw materials, composition, proportion, and effective dose of the compounds for treatment of metabolic syndrome. The IRF mice models, characterized by insulin resistance and hypercholesterolemia, were induced by high fat diet. The insulin sensitivity was estimated with insulin tolerance test(ITT) and glucose tolerance test(GTT); the levels of blood glucose and total cholesterol(TC), and the activities of α-glucosidase, protein tyrosine phosphatase 1B(PTP1B), and fructose phosphate amide transferase(GFAT)were measured with biochemical methods, respectively. The sample H13(h) extracted from Rhodiola crenulata, Y12(y) from Cordyceps militaris, and D(d) from Rheum palmatum were selected according to the inhibition activity on both PTP1B and α-glucosidase in vitro, regulation on hypercholesterolemia in IRF mice, and effects on GFAT activity, respectively; their synergistic effects on the treatment of metabolic syndrome were determined in IRF mice; composition proportion of h∶y∶d was measured in accordance with the results of L8(27) orthogonal experiments targeting on the inhibition of both PTP1B and α-glucosidase; finally, the effective dose was assessed based on the effects on IGT and hypercholesterolemia, respectively, in IRF mice. In conclusion, the prescription JD is composed by R. crenulata, C. militaris, and R. palmatum with the rate of 20∶1∶1, and its effective oral dose is 200 mg•kg⁻¹ for treatment of metabolic syndrome; its main mechanism is to inhibit the targets PTP1B and α-glucosidase. Monarch drug, R. crenulata, can clear away the lung-heat, tonify Qi, resolve stasis and nourish the heart. Adjuvant drug, C. militaris, can tonify the lung Qi and the kidney essence, strengthen waist and knee, accompanied with R. crenulata to enhance the function of invigorating lung and kidney. Assistant drug, rhubarb, can clear heat, detoxify, and remove blood stasis. These three herbs are compatible to show the effects of tonifying Qi, nourishing essence, clearing heat, reducing phlegm and resolving masses for the treatment of metabolic syndrome.

Investigation of a compound, compatibility of Rhodiola crenulata, Cordyceps militaris, and Rheum palmatum, on metabolic syndrome treatment II - improving obesity / 中国中药杂志

To investigate the effect of compound FF16, compatibility of Rhodiola crenulata, Cordyceps militaris, and Rheum palmatum, on obesity, both the insulin resistant obese IRF mouse model induced by high fat diet and the spontaneous type 2 diabetes KKAy obese mouse model were used. The results showed that the body weights and the energy uptake were markedly reduced by compound FF16 in both IRF mice in dose-dependent manner and KKAy mice, respectively. Meanwhile, with the administration of FF16, the hypercholesterolemia and the hypertriglyceridemia were improved significantly in KKAy mice; and the levels of serum cholesterol and fatty index were decreased obviously, and the value of serum HDL-C was increased significantly in IRF mice, respectively. Moreover, the activity of a-glycosidase was inhibited by compound FF16 in vitro. In conclusion, FF16 could improve the obesity by inhibiting alpha-glycosidase activity.

Investigation of a compound, compatibility of Rhodiola crenulata, Cordyceps militaris, and Rheum palmatum on metabolic syndrome treatment III--controlling blood glucose / 中国中药杂志

Base on the improvement of compound FF16, compatibility of Rhodiola crenulata, Cordyceps militaris, and Rheum palmatum, on both insulin resistance and obesity, its effects on type 2 diabetes (T2DM ) was investigated here. The results showed that the levels of fasting and no-fasting blood glucose were controlled in the spontaneous type 2 diabetes KKAy mice; the impaired glucose tolerance (IGT)was improved by decreasing significantly the values of the glucose peaks and the area under the blood glucose-time curve (AUC ) after glucose-loading in glucose tolerance test (OGTT) in both high-fat-diet-induced pre-diabetes IRF mice and KKAy mice, respectively. The pancreatic histopathological analysis showed that the increased islet amount, the enlarged islet area, and the lipid accumulation in the pancreas were reversed by FF16 treatment in both IRF mice and KKAy mice. In the palmitate-induced RINm5f cell model, FF16 could effectively reduce the apoptosis and enhance the glucose-stimulated insulin secretion, respectively. In conclusion, FF16 could improve the T2DM by protecting the pancreatic beta-cells.

Investigation of compound, compatibility of Rhodiola crenulata, Cordyceps militaris, and Rhum palmatum, on metabolic syndrome treatment VI--improving hyperglycemia-mediated renal damage / 中国中药杂志

This study is to investigate the effects of a Chinese prescription (FF), compatibility of Rhodiola crenulata, Cordyceps militaris and Rheum palmatum, on nephropathy in type 1 diabetic rats induced by streptozocin. According to fasting blood glucose level, diabetic rats were divided into three groups: model group, insulin-treated group and FF-treated group. Parameters for evaluating the glucose & lipid metabolism and the renal function were monitored dynamically. Levels of oxidative stress were detected ten weeks later. The results show that FF could significantly decrease the level of serum glucose and lipid profiles, improve the renal functions by decreasing blood urea nitrogen, urine albumin excretion and urease activity; FF could also affect on oxidative stress. In conclusion, Chinese prescription FF could ameliorate hyperglycemia-mediated renal damage in type 1 diabetic rats. These effects may be related to its regulation on the metabolism of glucose and lipid, the microcirculation disturbance and the oxidative stress.

Effect of safflor yellow injection on inhibiting lipopolysaccharide-induced pulmonary inflammatory injury in mice / 中国结合医学杂志

<p><b>OBJECTIVE</b>To observe the effect of Safflor Yellow (SY) Injection on acute lung injury (ALI) induced by lipopolysaccharide (LPS) in mice.</p><p><b>METHODS</b>Seventy-two mice were divided into six groups: control (saline + saline); LPS (LPS + saline); SY Injection [LPS + SY (10, 20 or 40 mg/kg, intravenously)] and anisodamine (AD) (LPS + AD). Thirty minutes after SY or AD administration, 15 mg/kg LPS was given intraperitoneally. All animals were sacrificed 4 h after LPS injection. Arterial blood gas and lung water content index (LWCI) were measured. Lung tissue myeloperoxidase (MPO) activity was assayed. mRNA expression of inflammatory cytokines was assayed by reverse-transcription polymerase chain reaction. Lung morphological and nuclear factor (NF)-κB p65-positive cell changes were observed by HE and immunohistochemical staining. p38 mitogen-activated protein kinase (MAPK) phosphorylation was observed by Western blotting.</p><p><b>RESULTS</b>After LPS administration, all animals displayed increased arterial carbon dioxide partial pressure (PaCO2) and decreased arterial oxygen partial pressure (PaO2), arterial oxygen saturation (SO2), HCO3 (-) concentration and pH, and increased LWCI, MPO activity, interleukin (IL)-1β, IL-6 and tumor necrosis factor (TNF)-α mRNA expression, NF-κB p65-positive staining and p38 MAPK activation compared with normal controls (all P<0.01). SY Injection significantly mitigated the LPS-induced increase in arterial PaCO and the decreases in arterial PaO2, SO2 and pH, and attenuated increases in LWCI and lung tissue MPO activity (all P<0.01). Moreover, SY Injection inhibited the increases in NF-κB p65 staining and in TNF-α, IL-1β and IL-6 mRNA expression (all P<0.01), and promoted the expression of the antiinflammatory cytokine IL-10 (P<0.05) following LPS injection. LPS-induced pulmonary p38 MAPK phosphorylation was suppressed by pretreatment with SY Injection (P<0.01).</p><p><b>CONCLUSION</b>SY Injection ameliorates inflammatory ALI induced by LPS in mice.</p>

Investigation of a compound, compatibility of Rhodiola crenulata, Cordyceps militaris, and Rhum palmatum, on metabolic syndrome treatment. IV--Improving liver lipid accumulation / 中国中药杂志

To investigate the effects of a compound (FF16), compatibility of Rhodiola crenulata, Cordyceps militaris, and Rhum palmatum, on non-alcoholic fatty liver disease in IRF mice induced by high fat diet H&E stain was processed to evaluate the lipid accumulation in liver, and the dynamic microcirculation observation system was applied to determine hepatic microcirculation of IRF mice. Western blot was performed to evaluate IRS-2, HSL and ppar-alpha expression in liver. The results demonstrate that FF16 significantly decreased the liver lipid index and improved liver steatosis in IRF mice. Furthermore, FF16 could ameliorate hepatic microcirculation disturbance in IRF mice through enhancing RBC velocity and shear rates by 62.5% and 49.7%, increasing sinusoids perfusion by 70.0%, inhibiting adhered leukocytes in IRF mice. The abnormal expressions of IRS-2 and HSL were both reversed by the administration of FF16. In conclusion, FF16 could improve non-alcoholic fatty liver disease in IRF mice by improving insulin sensitivity, regulating lipid metabolism and improving microcirculation disturbance.

Investigation of a compound, compatibility of Rhodiola crenulata, Cordyceps militaris, and Rheum palmatum, on metabolic syndrome treatment. V--Mechanisms on improving glucose metabolic disorders / 中国中药杂志

To investigate the mechanisms of a compound (FF16), compatibility of Rhodiola crenulata, Cordyceps militaris, and Rheum palmatum, on glucose metabolic disorders, the IRF mice charactered with insulin resistance and glucose metabolic disorders induced by high-fat diet in C57BL/6J mice were randomly divided into 3 groups; IRF, rosiglitazone (Rosi) and FF16. The glucose metabolism was evaluated by fasting blood glucose (FBG) levels and intraperitoneal glucose tolerance test (IPGTT). The insulin sensitivity was estimated by insulin tolerance test (ITT), fasting serum insulin levels and the index of HOMA-IR. The expressions of Akt and its phosphorylation levels, GSK3beta and its phosphorylation levels in liver were detected by Western Blot. The results showed that FF16 significantly improved the glucose metabolic disorders through reducing FBG by 15.1%, decreasing AUC values in glucose tolerance tests by 22.3%. FF16 significantly improved the insulin sensitivity through decreasing AUC values in insulin tolerance tests by 22.1%, reducing the levels of serum insulin by 42.9% and of HOMA-IR by 49.5%, comparing with model control, respectively. After the treatment with FF16, the levels of p-Akt and p-GSK3beta were increased by 116.4% and 24.9%, respectively, in the liver of IRF mice. In conclusion, compound FF16 could improve glucose metabolic disorders in IRF mice through enhancing the glyconeogenesis.

Chemical constituents from flowers of Carthamus tinctorius / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents from the flowers of Carthamus tinctorius.</p><p><b>METHOD</b>Compounds were isolated by chromatographic techniques. Their structures were elucidated by spectral methods.</p><p><b>RESULT</b>Ten compounds were identified as 7,8-dimethylpyrazino [2,3-g] quinazolin-2, 4-(1H, 3H) -dione (1), adenosine (2), adenine (3), uridine (4), thymine (5), uracil (6), roseoside (7), 4'-O-dihydrophaseic acid-beta-D-glucopyranoside methylester (8), 4-O-beta-D-glucopyranosyloxy-benzoic acid (9) and p-hydroxybenzoic acid (10).</p><p><b>CONCLUSION</b>Compounds 1 and 8 were isolated from natural plants for the first time, and compounds 7, 9 and 10 were isolated from this plant for the first time.</p>

Studies on chemical constituents from roots of Cudrania cochinchinensis / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents from the roots of Cudrania cochinchinensis.</p><p><b>METHOD</b>The chemical constituents of C. cochinchinensis were isolated and purified by silica gel, polyamide column chromatography, Their structures were identified on the basis of spectroscopic data.</p><p><b>RESULT</b>Six compounds were isolated and identified. Their structures were established as 3, 5, 7, 4"-tetrahydroxyflavanone-7-O-(6"-acetyl)-glucoside (1), 3, 5, 7, 4'-tetra hydroxyflavanone-7-O-glucoside (2), 2', 4', 5, 7-tetrahydroxy-6-prenyldihydroflavanone (3), 5, 7, 4'-trihysdroxy-6-prenylisoflavanone (4), 1, 3, 5, 6-tetrahydroxyxanthone (5), stilbene-2, 4, 3', 5'-tetraol (6).</p><p><b>CONCLUSION</b>Compound 1 was isolated from this genus, while compounds 4 and 5 were isolated from this plant for the first time.</p>

Studies on constituents from root and stem of Ervatamia hainanensis / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the constituents of Ervatamia hainanensis systematically.</p><p><b>METHOD</b>Various chromatographic techniques were applied to isolate and purify the constituents of this plant. The structures were elucidated by spectroscopic analysis.</p><p><b>RESULT</b>Eight compounds were obtained, which were identified as alpha-amyrin acetate (1), 11-oxo-alpha-amyrin acetate (2), beta-sitosterol (3), cycloart-23-ene-3beta, 25-diol(4), cycloart-25-ene-3beta, 24-diol (5), 5alpha, 8alpha-epidioxyergosta-6, 22-dien-3beta-ol (6), ibogamin-3-one (7), beta-daucosterol (8).</p><p><b>CONCLUSION</b>Compounds 1, 2, 4- 7 were isolated from this plant for the first time.</p>

The chemical constituents of Rhododendron ovatum Planch / 药学学报

<p><b>AIM</b>To study the chemical constituents of Rhododendron ovatum Planch.</p><p><b>METHODS</b>The chemical constituents were isolated and purified by silica gel column chromatography and identified on the basis of their physiochemical and spectral data.</p><p><b>RESULTS</b>Seven compounds were isolated and identified. Their structures were established as 3,5,7-trihydroxylchromone 3-O-beta-D-xylopyranoside (I), taraxerol (II), beta-sitosterol (III), betulinic acid (IV), quercetin (V), quercetin-3-O-alpha-L-rhamnopyranoside (VI), and D-glucose (VII).</p><p><b>CONCLUSION</b>Compound I is a new compound. Compounds II-VII were isolated from this plant for the first time.</p>

Chemical constituents from root of Prismatomeris tetrandra / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents from root of Prismatomeris tetrandra.</p><p><b>METHOD</b>Compounds were isolated by chromatographic techniques on silica gel column. Their structures were elucidated by chemical and spectral methods.</p><p><b>RESULT</b>Six compounds were identified as 1-hydroxy-2-methylanthraquinone (I), 2-hydoxy-3-methoxyanthraquinone (II), 1, 3-dihydroxy-2-methoxyanthraquione (II), rubiadin (IV), rubiadin-1-methyl ether (V) and beta-sitosterol (V).</p><p><b>CONCLUSION</b>I, II and III were isolated from the plant for the first time.</p>

Chemical constituents from the leaves of Dalbergia hainanensis / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents from the leaves of Dalbergia hainanensis.</p><p><b>METHOD</b>Compounds were isolated by chromatographic techniques on silica gel and polyamide column. Their structures were elucidated by chemical and spectroscopic methods.</p><p><b>RESULTS</b>Thirteen compounds were identified as 8-C-glucosylprunetin (1), 8-C-glucosylgenistein (2), 2-hydroxy-5-methoxy biochanin A (3), formononetin (4), 3,5-dimethoxy-4-hydroxybenzaldehyde (5), 1-O-beta-D-glucopyranosyl-(2S, 3S, 4R, 8Z)-2-[(2R)-2-hydroxyl docosylamino]-8-octadecene-1, 3, 4-triol (6), friedelin (7), taxaxerol (8), 3(-hydroxy-glutin-5-ene (9), ursolic acid (10), beta-sitosterol (11), daucosterol (12), lupeol (13).</p><p><b>CONCLUSION</b>All the compounds were isolated from the plant for the first time.</p>