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1.
Zhongguo Zhen Jiu ; 44(4): 455-459, 2024 Apr 12.
Article in English, Chinese | MEDLINE | ID: mdl-38621734

ABSTRACT

Focusing on the syndrome/pattern differentiation to determine treatment, the approaches to the diagnosis and treatment of acupuncture and moxibustion for adenomyosis are explored by identifying the etiology, location, nature and development of disease. The syndromes/patterns of adenomyosis are differentiated in view of both zangfu and meridian theories. The treatment is delivered complying with the menstrual cycle and the basic rule of treatment, "treating the symptoms in the acute stage, while the root causes in the recovery stage". During menstrual period, stopping pain and eliminating stasis are dominant; while during the other days of menstrual cycle, regulating zangfu dysfunction (excess or deficiency) is emphasized. In general, the functions of the thoroughfare vessel and the conception vessel should be specially considered and adjusted, and the principles of treatment include strengthening the spleen, regulating the kidney and soothing the liver. Acupoints are selected mainly from the spleen meridian of foot-taiyin, the kidney meridian of foot-shaoyin and the conception vessel. Ciliao (BL 32), Shiqizhui (EX-B 8), Zigong (EX-CA 1), Diji (SP 8) and four-gate points (bilateral Hegu [LI 4] and Taichong [LR 3]) are used in menstrual period; Zusanli (ST 36), Sanyinjiao (SP 6) and Taixi (KI 3) in postmenstrual phase; Guanyuan (CV 4), Luanchao (Ovary, Extra) and Qihai (CV 6) in intermenstrual phase; while, Guanyuan (CV 4), Qihai (CV 6) and Shenque (CV 8), combined with Gongsun (SP 4), Neiguan (PC 6) and Jianshi (PC 5) in premenstrual phase. According to the dynamic development of patient's conditions, the reinforcing or reducing techniques of acupuncture and moxibustion are feasibly applied in treatment of adenomyosis.


Subject(s)
Acupuncture Therapy , Adenomyosis , Meridians , Moxibustion , Female , Humans , Adenomyosis/therapy , Acupuncture Points
2.
Phytother Res ; 38(2): 1104-1158, 2024 Feb.
Article in English | MEDLINE | ID: mdl-38176694

ABSTRACT

Natural products have played a significant role throughout history in the prevention and treatment of numerous diseases, particularly cancers. As a natural product primarily derived from various medicinal plants in the Withania genus, withanolides have been shown in several studies to exhibit potential activities in cancer treatment. Consequently, understanding the molecular mechanism of withanolides could herald the discovery of new anticancer agents. Withanolides have been studied widely, especially in the last 20 years, and attracted the attention of numerous researchers. Currently, over 1200 withanolides have been classified, with approximately a quarter of them having been reported in the literature to be able to modulate the survival and death of cancer cells through multiple avenues. To what extent, though, has the anticancer effects of these compounds been studied? How far are they from being developed into clinical drugs? What are their potential, characteristic features, and challenges? In this review, we elaborate on the current knowledge of natural compounds belonging to this class and provide an overview of their natural sources, anticancer activity, mechanism of action, molecular targets, and implications for anticancer drug research. In addition, direct targets and clinical research to guide the design and implementation of future preclinical and clinical studies to accelerate the application of withanolides have been highlighted.


Subject(s)
Antineoplastic Agents , Neoplasms , Plants, Medicinal , Withania , Withanolides , Humans , Withanolides/pharmacology , Withanolides/therapeutic use , Antineoplastic Agents/pharmacology , Antineoplastic Agents/therapeutic use , Neoplasms/drug therapy
3.
Fitoterapia ; 166: 105460, 2023 Apr.
Article in English | MEDLINE | ID: mdl-36801349

ABSTRACT

Two new verticillane-diterpenoids (1 and 2) were isolated from the gum resin Boswellia sacra. Their structures were elucidated by physiochemical and spectroscopic analysis, as well as ECD calculation. In addition, the in vitro anti-inflammatory activities of the isolated compounds were evaluated by determining the inhibitory effects on lipopolysaccharide (LPS)-induced NO production in RAW 264.7 mouse monocyte-macrophages. The results showed that compound 1 exhibited significant inhibitory effect on NO generation with an IC50 value of 23.3 ± 1.7 µM suggesting that it might be a candidate for an anti-inflammatory agent. Furthermore, 1 potently inhibited the release of inflammatory cytokines IL-6 and TNF-α induced by LPS in a dose-dependent manner. Using Western blot and Immunofluorescence methods, compound 1 was found to inhibit inflammation mainly by restraining the activation of NF-κB pathway. And in the MAPK signaling pathway, it was found to have inhibitory effects on the phosphorylation of JNK and ERK proteins and have no effect on the phosphorylation of p38 protein.


Subject(s)
Boswellia , Diterpenes , Animals , Mice , NF-kappa B/metabolism , Boswellia/chemistry , Lipopolysaccharides/pharmacology , Molecular Structure , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/therapeutic use , Inflammation/drug therapy , RAW 264.7 Cells
4.
Biomed Pharmacother ; 153: 113542, 2022 Sep.
Article in English | MEDLINE | ID: mdl-36076619

ABSTRACT

Coptidis Rhizoma exhibits potent effects on ameliorating metabolic disease through modulation of gut bacteria. Gut fungi play a significant role on the homeostasis of the intestinal microecosystem and several types of metabolic disorders. Previous studies have mainly concentrated on the function of bacteria on the beneficial effects of Coptidis Rhizoma and its main component berberine, but whether gut fungi are linked to the improvement of glycolipid metabolism disorder of Coptidis Rhizoma is not clear. Here, the anti-hyperlipidemic effects of Coptidis Rhizoma was firstly confirmed in the high fat diet (HFD)-induced mice. The changes of gut fungi and bacteria of the mice treated with Coptidis Rhizoma and the interaction of intestinal fungi and bacteria were investigated. Coptidis Rhizoma significantly decreased serum lipids and inhibited the hepatic lipid accumulation in the HFD-fed mice. Mechanistically, Coptidis Rhizoma reduced the diversity of gut bacteria and fungi, meanwhile changed their composition. Fungus Aspergillus species (A. chevalieri, A. luteovirescens, A. oryzae, A. sp. F51) and Penicillium (P. expansum, P. janthinellum, P. sp. BAB-5649 and P. sp. GZU-BCECYN66-5) were decreased in Coptidis Rhizoma-treated group, while Tilletia bornmuelleri, Tilletia bromi were increased. Furthermore, there are complex association between intestinal fungi and bacteria. For example, fungus Aspergillus (Aspergillus chevalieri, Aspergillus luteovirescens, Aspergillus oryzae) was negative associated with bacterium Blautia coccoides, but positive associated with Lactobacillus (L. johnsonii, L. sparagasseri, L. taiwanensis, L. amylovorus). These results demonstrated that Coptidis Rhizoma might exhibit anti-hyperlipidemic effects through modulation of the intestinal bacteria and fungi composition, and regulation their interaction.


Subject(s)
Berberine , Drugs, Chinese Herbal , Animals , Bacteria , Berberine/pharmacology , Drugs, Chinese Herbal/pharmacology , Drugs, Chinese Herbal/therapeutic use , Fungi , Mice , Rhizome
5.
Nat Prod Res ; 36(7): 1820-1826, 2022 Apr.
Article in English | MEDLINE | ID: mdl-32954869

ABSTRACT

The chemical investigation of the fruits of Xanthium strumarium (Asteraceae) led to the isolation of two new ent-kauranoid glucosides named 2-O-(6-O-isocaleryl-ß-D-glucopyranosyl) atractyligenin (1) and 2-O-(2-O-isovaleryl-ß-D-glucopyranosyl) atractyligenin (2), together with one known compound. Their structures were established by comprehensive spectroscopic analysis coupled with single-crystal X-ray diffraction and electronic circular dichroism data. All compounds and their aglycone were evaluated for their anti-proliferative activities in vitro against three human cancer cell lines.


Subject(s)
Diterpenes, Kaurane , Xanthium , Diterpenes, Kaurane/chemistry , Fruit , Glucosides/chemistry , Glucosides/pharmacology , Humans , Xanthium/chemistry
6.
Planta Med ; 88(11): 921-932, 2022 Sep.
Article in English | MEDLINE | ID: mdl-34111890

ABSTRACT

Rhizoma coptidis has been clinically used for a long time for the treatment of various diseases in China, such as hypertension, diabetes, and inflammation. Previous studies have shown that alkaloid components of Rhizoma coptidis extract could be extensively metabolized and the metabolites were also considered to be the therapeutic material basis. However, until now, pharmacokinetic studies of the in vivo metabolites have not been revealed yet. The aim of the present study was to characterize the pharmacokinetics and excretions of five main alkaloids (berberine, jatrorrhizine, palmatine, epiberberine, and coptisine) and their seven metabolites (berberrubine, demethyleneberberine, jatrorrhizine-3-O-ß-D-glucuronide, thalifendine-10-O-ß-D-glucuronide, berberrubine-9-O-ß-D-glucuronide, demethyleneberberine-2-O-sulfate, and demethyleneberberine-2-O-ß-D-glucuronide) in rats after oral administration of Rhizoma coptidis extract. Meanwhile, comparative pharmacokinetics and excretions of these analytes in diabetic model rats were also investigated, since Rhizoma coptidis is widely used for the treatment of diabetes. Our results showed that the in vivo existing forms of alkaloid components were phase II metabolites, highlighting the glucuronidation metabolic pathway. In diabetic model rats, the utilization of Rhizoma coptidis alkaloids was significantly increased and the biotransformation of berberine into berberrubine was significantly inhibited.


Subject(s)
Alkaloids , Berberine Alkaloids , Berberine , Coptis , Diabetes Mellitus, Experimental , Drugs, Chinese Herbal , Administration, Oral , Animals , Berberine Alkaloids/metabolism , Coptis/metabolism , Diabetes Mellitus, Experimental/drug therapy , Drugs, Chinese Herbal/pharmacology , Glucuronides , Rats
7.
Fitoterapia ; 146: 104728, 2020 Oct.
Article in English | MEDLINE | ID: mdl-32949648

ABSTRACT

Phytochemical investigation of Physalis minima led to the isolation of six new withanolides, including physaminilides HK (1-4), two artificial withanolides (5-6), and 19 known ones (7-25). Their structures were elucidated on the basis of spectroscopic analysis, including NMR and electronic circular dichroism (ECD) data. The isolates were evaluated for their cytotoxic activities against A375 human melanoma cells. Compounds 1, 8-9, 12-13, 15-17 and 19 exhibited significant cytotoxic activities with IC50 values in the range of 1.2-7.5 µM.


Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Physalis/chemistry , Withanolides/pharmacology , Antineoplastic Agents, Phytogenic/isolation & purification , Cell Line, Tumor , China , Humans , Molecular Structure , Phytochemicals/isolation & purification , Phytochemicals/pharmacology , Withanolides/isolation & purification
8.
Pharmacol Ther ; 216: 107650, 2020 12.
Article in English | MEDLINE | ID: mdl-32758647

ABSTRACT

As a Traditional Chinese Medicine, Artemisia annua L. (A. annua) has been used for the treatment of various diseases since ancient times, including intermittent fevers due to malaria, bone steaming and heat/fever arising from exhaustion, tuberculosis, lice, wounds, scabies, dysentery et al. With the discovery of artemisinin and its excellent anti-malarial activity, A. annua has received great attention. Recently, A. annua has been revealed to show inhibitory effects against parasites (e.g. Plasmodium, Toxoplasma gondii, Leishmania, Acanthamoeba, Schistosoma), viruses (e.g. hepatitis A virus, herpes simplex viruses 1 and 2, human immunodeficiency virus), fungi (Candida, Malassezia, Saccharomyces spp.) and bacteria (Enterococcus, Streptococcus, Staphylococcus, Bacillus, Listeria, Haemophilus, Escherichia, Pseudomonas, Klebsiella, Acinetobacter, Salmonella, Yersinia spp.). A. annua has also been reported to possess anti-inflammatory and anti-cancer actions and been employed for the treatment of osteoarthritis, leukemia, colon cancer, renal cell carcinoma, breast cancer, non-small cell lung cancer, prostate cancre and hepatoma. Besides, the immunoregulation, anti-adipogenic, anti-ulcerogenic, anti-asthmatic, anti-nociceptive and anti-osteoporotic activities of A. annua were also evaluated. Along these lines, this review summarizes the traditional application and modern pharmacological research of A. annua, providing novel insights of A. annua in the treatment of various diseases.


Subject(s)
Anti-Infective Agents/pharmacology , Anti-Inflammatory Agents/pharmacology , Antineoplastic Agents, Phytogenic/pharmacology , Artemisia annua/chemistry , Plant Extracts/pharmacology , Animals , Anti-Infective Agents/isolation & purification , Anti-Inflammatory Agents/isolation & purification , Antineoplastic Agents, Phytogenic/isolation & purification , Humans , Plant Extracts/isolation & purification
9.
Biomed Chromatogr ; 34(10): e4919, 2020 Oct.
Article in English | MEDLINE | ID: mdl-32533560

ABSTRACT

Rhizoma coptidis has been used for a long time in China owing to its anti-bacterial, anti-diabetes, anti-hyperlipidemia and anti-obesity activities. However, the in vivo biotransformation of Rhizoma coptidis is still unclear to date. In this study, a three-step strategy using UPLC-Q-TOF/MS was applied to clarify the in vivo absorbed constituents and metabolites in rats after oral administration of Rhizoma coptidis. First, alkaloids in Rhizoma coptidis extract were identified. Second, six abundant alkaloids (berberine, palmatine, coptisine, epiberberine, jatrorrhizine, and columbamine) were selected as representative prototypes and the metabolic fates of them in rats were investigated to obtain a database of Rhizoma coptidis-derived metabolites. Finally, the metabolic profiles of Rhizoma coptidis were fully elucidated based on the above-mentioned results. In summary, 29 alkaloids were identified in Rhizoma coptidis, and a database of Rhizoma coptidis-derived metabolites was obtained with 144 characterized metabolites. A total of 89 xenobiotics including 12 absorbed constituents and 77 metabolites were identified in dosed rat biosamples. Major metabolic pathways of Rhizoma coptidis were hydroxylation, reduction, methylation, demethylation, demethylenation, desaturation, glucuronidation and sulfation. This is the first systematic study on the in vivo absorbed constituents and metabolic profiling of Rhizoma coptidis and will be beneficial for its further studies.


Subject(s)
Alkaloids , Chromatography, High Pressure Liquid/methods , Drugs, Chinese Herbal , Mass Spectrometry/methods , Administration, Oral , Alkaloids/analysis , Alkaloids/metabolism , Animals , Biotransformation , Coptis chinensis , Drugs, Chinese Herbal/administration & dosage , Drugs, Chinese Herbal/pharmacokinetics , Male , Rats , Rats, Sprague-Dawley
10.
J Ethnopharmacol ; 259: 113015, 2020 Sep 15.
Article in English | MEDLINE | ID: mdl-32464315

ABSTRACT

ETHNOPHARMACOLOGICAL EVIDENCE: Curcumin (CUR) is the active ingredient of Traditional Chinese Medicine turmeric (Curcuma longa L.), which has been used for treatment of diabetes in Ayurveda and China. CUR exerts potent anti-insulin-resistant effects in various cell lines. However, previous studies indicated CUR was metabolized extensively in vivo and massively degraded in a medium alkaline buffer solution. The real active component of the anti-insulin-resistant activity of CUR in vitro is not clear. AIM OF THE STUDY: Our study identified the functional contribution of the metabolites of CUR and the related molecular mechanism in improving insulin sensitivity. MATERIALS AND METHODS: HPLC and UPLC-QQQ-MS analyses were used to investigate the stability and metabolism of CUR in HepG2 cells. The effect of the metabolic products of CUR on insulin sensitivity was evaluated in high glucose (HG)-induced insulin-resistant HepG2 cells. A network pharmacology approach was used to examine the potential targets of the metabolites, and Western blotting was performed to verify changes in the targets. RESULTS: CUR was unstable in the cell culture medium, but the prototypes, metabolites and degradation products of CUR coexisted in the HepG2 cell culture experiment. The insulin sensitivity assay demonstrated that CUR and its metabolites enhanced insulin sensitivity in HG-induced insulin-resistant HepG2 cells, but the total degradation products of CUR may not play the major role. Similar to CUR, hexahydrocurcumin (HHC) and octahydrocurcumin (OHC) improved insulin sensitivity by strengthening the PI3K-AKT-GSK3B signal and suppressing the phosphorylation of ERK/JNK in HG-induced insulin-resistant HepG2 cells. CONCLUSIONS: Metabolites of CUR played a critical role in counteracting insulin resistance in HG-induced HepG2 cells. CUR exerted anti-insulin resistance effect in HepG2 cells in a multi-component, multi-target, and multi-pathway manner.


Subject(s)
Curcumin/pharmacology , Glucose/metabolism , Hepatocytes/drug effects , Insulin Resistance , Insulin/pharmacology , Biotransformation , Curcumin/metabolism , Drug Stability , Extracellular Signal-Regulated MAP Kinases/metabolism , Glycogen Synthase Kinase 3 beta/metabolism , Hep G2 Cells , Hepatocytes/metabolism , Humans , JNK Mitogen-Activated Protein Kinases/metabolism , Phosphatidylinositol 3-Kinase/metabolism , Phosphorylation , Proto-Oncogene Proteins c-akt/metabolism , Signal Transduction
11.
RSC Adv ; 10(67): 41154-41163, 2020 Nov 09.
Article in English | MEDLINE | ID: mdl-35519219

ABSTRACT

Xanthium strumarium L. (XS) is a traditional Chinese medicine (TCM) that has been widely used in Chinese medicine prescription for allergic rhinitis (AR). However, the action mechanisms of XS on the therapeutic effects on AR remain elusive. Herein, an integrated approach of phytochemistry, network pharmacology and metabolomics was first applied to uncover the action mechanisms of XS for AR. The therapeutic effect of XS extract on AR was evaluated in rat models of ovalbumin (OVA)-induced AR. The cytokine levels in rat serum and histopathological changes of nasal mucosa were assessed after oral treatment with XS. Chemical compositions of XS were elucidated by phytochemical methods, and active ingredients were identified via ADME-TOX screening in silico. Network pharmacology was performed to establish and analyze the compound-target-disease network so as to find the possible mechanism of XS in treating AR. In addition, metabolomics analysis was applied to investigate the changes in the endogenous metabolite levels that result from XS treatments. As result, the XS extract significantly increased the serum concentrations of IL-2 and reduced the levels of serum IL-4, while XS could ameliorate inflammation in the nasal sub-mucosal area, indicating that XS has significant therapeutic effects on AR model rats. Furthermore, a total of 119 compounds were isolated from XS, and 59 of these compounds were identified as active ingredients through ADME-TOX screening in silico. An in-depth analysis of the network pharmacology implied that the active ingredients of XS could regulate the inflammatory response via "multi-component, multi-target" patterns. In combination with the results of metabolomics, we found that the active ingredients of XS have a beneficial effect on AR through regulating the metabolism of arachidonic acid, which was reflected by medicating the Fc epsilon RI signaling pathway, and the neuroactive ligand-receptor interaction pathway, as well as the key proteins in arachidonic acid metabolism, such as PTGS2, PTGS1, PTGES and ALOX5. Additionally, molecular docking showed that multiple compounds have better binding with PTGS2 and ALOX5, which might be two crucial targets. Overall, these results suggest that the treatment of XS for AR is realized by regulating the metabolism of arachidonic acid via a combination form. This study provides the basis for clinical applications of XS.

12.
Molecules ; 24(22)2019 Nov 09.
Article in English | MEDLINE | ID: mdl-31717579

ABSTRACT

The dried seeds of Aesculus chinensis Bge. var. chekiangensis (Hu et Fang) Fang, called "Suo Luo Zi", have been used in traditional Chinese medicine. Nevertheless, most studies have been focused on components of less polarity fractions. In this research, twelve indoles, including six new indole glycosides (1-6) as well as six known analogs were isolated from the polar portion which has been seldom studied. This is the first description of N-glucosylated indoles obtained from the genus of Aesculus. Structures of the new compounds (1-6) were elucidated based on comprehensive interpretation of HRESIMS, 1D and 2D NMR. Additionally, the neuroprotective activities of the N-glucosylated indoles were evaluated for the first time indicating that compounds 1-5 and 9-10 exhibited moderate neuroprotective activities. Further cytotoxicity tests of isolates 1-10 on three human tumor cell lines suggested that none of these compounds were cytotoxic (IC50 > 50 µM).


Subject(s)
Aesculus/chemistry , Glycosides/pharmacology , Indoles/pharmacology , Neuroprotective Agents/pharmacology , Plant Extracts/pharmacology , Cell Line, Tumor , HCT116 Cells , Hep G2 Cells , Humans , Medicine, Chinese Traditional/methods
13.
J Sep Sci ; 42(16): 2592-2601, 2019 Aug.
Article in English | MEDLINE | ID: mdl-31161707

ABSTRACT

A rapid and sensitive liquid chromatography with tandem mass spectrometry method was developed and validated for simultaneous determination of puerarin, daidzin, daidzein, 3'-hydroxy puerarin, and genistein in rat plasma after oral administration of Puerariae lobatae radix extract. The method of protein precipitation with acetonitrile was used for sample preparation. Chromatographic separation was achieved on a C18 column with the mobile phases of acetonitrile/water containing 0.1% formic acid. The analytes were detected by mass spectrometer with an electrospray ionization source operating in the negative ion mode. The linearity, precision, accuracy, dilution reliability, recovery, matrix effects, and stability of the method were within acceptable ranges. The developed method was successfully used to compare the pharmacokinetic characteristics of five analytes in normal and type 2 diabetics rats after oral administration of Puerariae lobatae radix extract. Several pharmacokinetic alterations were observed and this might be caused by the pathological state of type 2 diabetes.


Subject(s)
Diabetes Mellitus, Type 2/blood , Diabetes Mellitus, Type 2/metabolism , Drugs, Chinese Herbal/analysis , Drugs, Chinese Herbal/pharmacokinetics , Isoflavones/blood , Isoflavones/pharmacokinetics , Pueraria/chemistry , Administration, Oral , Animals , Chromatography, Liquid , Diabetes Mellitus, Type 2/pathology , Drugs, Chinese Herbal/administration & dosage , Isoflavones/administration & dosage , Male , Molecular Conformation , Rats , Rats, Sprague-Dawley , Tandem Mass Spectrometry
14.
J Nat Med ; 73(4): 847-854, 2019 Sep.
Article in English | MEDLINE | ID: mdl-31218551

ABSTRACT

Two new flavonoid glycosides, 2',4'-dihydroxydihydrochalcone-4-O-ß-D-glucopyranoside (1) and medicarpin-3-O-ß-D-apiofuranosyl (1 → 2)-ß-D-glucopyranoside (2), together with 34 known flavonoids were isolated from the 75% EtOH extract of the dried roots of Glycyrrhiza uralensis Fisch. Their structures were elucidated on the basis of spectroscopic analyses. The flavonoids were classified into ten sub-types, namely, dihydrochalcone (1), pterocarpans (2-4), flavones (5-6), flavanones (7-11), chalcones (12-15), retro-chalcones (16-18), isoflavans (19-21), isoflavones (22-28), 3-arylcoumarins (29-30), and coumestans (31-36). The isolated flavonoids were evaluated for in vitro hepatoprotective activity against D-galactosamine-induced toxicity in human hepatoma HepG2 cells.


Subject(s)
Flavonoids/isolation & purification , Flavonoids/pharmacology , Glycosides/isolation & purification , Glycosides/pharmacology , Glycyrrhiza uralensis/chemistry , Cell Line, Tumor , Chalcones/chemistry , Chalcones/isolation & purification , Coumarins/chemistry , Coumarins/isolation & purification , Flavanones/chemistry , Flavanones/isolation & purification , Flavones/chemistry , Flavones/isolation & purification , Flavonoids/chemistry , Glycosides/chemistry , Glycyrrhiza/chemistry , Hep G2 Cells , Humans , Isoflavones/chemistry , Isoflavones/isolation & purification , Plant Roots/chemistry , Pterocarpans/chemistry , Pterocarpans/isolation & purification
15.
Molecules ; 24(10)2019 May 14.
Article in English | MEDLINE | ID: mdl-31091775

ABSTRACT

A chemical investigation on 70% EtOH extract from the bark of Phellodendron chinense Schneid (Rutaceae) led to six new methyl apiofuranosides (1-6), and ten known compounds (7-16). All these compounds were characterized by the basic analysis of the spectroscopic data including extensive 1D-, 2D-NMR (HSQC, HMBC), and high-resolution mass spectrometry, and the absolute configurations were determined by both empirical approaches and NOESY. Inhibitory effects of compounds 1-9 and 11-16 on nitric oxide production were investigated in lipopolysaccharide (LPS)-mediated RAW 264.7 cells, as a result, most of these isolates inhibited nitric oxide (NO) release, and among them 9, 11, and 12 displayed the strongest inhibition on NO release at the concentration of 12.5 µM.


Subject(s)
Lipopolysaccharides/adverse effects , Nitric Oxide/metabolism , Pentoses/pharmacology , Phellodendron/chemistry , Animals , Mice , Molecular Structure , Pentoses/chemistry , Plant Bark/chemistry , Plant Extracts/chemistry , Plant Extracts/pharmacology , RAW 264.7 Cells
16.
Nat Prod Res ; 33(24): 3485-3492, 2019 Dec.
Article in English | MEDLINE | ID: mdl-29968479

ABSTRACT

Two new isoflavone glucosides, 3'-methoxyneopuerarin A (1) and 3'-methoxyneopuerarin B (2), together with nine known isoflavones including puerarin (3), neopuerarin A (4), neopuerarin B (5), daidzin (6), daidzein (7), 3'-methoxypuerarin (PG-3) (8), puerarin xyloside (9), mirificin (10), 3'-hydroxypuerarin (11) were isolated from the water extraction of the dried roots of Pueraria lobata (Willd.) Ohwi. Their structures were elucidated by the means of spectroscopic and chromatographic analysis methods. All compounds were evaluated for their hepatoprotective activity on HepG2 cells. All of them showed statistically significant hepatoprotective effect.


Subject(s)
Isoflavones/chemistry , Isoflavones/pharmacology , Liver/drug effects , Protective Agents/chemistry , Protective Agents/pharmacology , Pueraria/chemistry , Drug Evaluation, Preclinical , Glucosides/chemistry , Glucosides/isolation & purification , Glucosides/pharmacology , Hep G2 Cells , Humans , Isoflavones/isolation & purification , Liver/cytology , Magnetic Resonance Spectroscopy , Molecular Structure , Plant Extracts/chemistry , Plant Roots/chemistry , Spectrometry, Mass, Electrospray Ionization
17.
Zhongguo Zhong Yao Za Zhi ; 43(19): 3834-3840, 2018 Oct.
Article in Chinese | MEDLINE | ID: mdl-30453706

ABSTRACT

The bitter taste is one of the important properties among five flavors of Chinese materia medica (CMM), characterized by downbearing and discharging, drying dampness, and consolidating Yin. In common CMM, bitter-taste CMM accounts for a large proportion, indicating the importance of it. Through the efficacy of clearing away heat and dampness, reducing fire and removing toxin, bitter-taste CMM has achieved good results in treating diabetes in clinical application, proving their definite therapeutic effect on regulating glucose and lipid metabolism (main features of diabetes). At present, there are many reports about the chemical constituents and pharmacological effects of CMM on diabetes, but there are few reviews on the chemistry and biology of bitter-taste CMM. This study summarized the properties and compatibility characteristics of bitter-taste CMM for treating diabetes, and mainly analyzed the chemistry and biology basis of bitter-taste CMM with function of regulating glycolipid metabolism, laying foundation for further researches on properties theory of CMM.


Subject(s)
Materia Medica/chemistry , Medicine, Chinese Traditional , Taste , Glycolipids/metabolism , Research
18.
Fitoterapia ; 124: 23-33, 2018 Jan.
Article in English | MEDLINE | ID: mdl-28993283

ABSTRACT

Berberrubine, an isoquinoline alkaloid isolated from many medicinal plants, possesses diverse pharmacological activities, including glucose-lowering, lipid-lowering, anti-inflammatory, and anti-tumor effects. This study aimed to investigate the metabolic profile of berberrubine in vivo. Therefore, a rapid and reliable method using the ultra-high performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) and metabolynx™ software with mass defect filter (MDF) technique was developed. Plasma, bile, urine and feces samples were collected from rats after oral administration of berberrubine with a dose of 30.0mg/kg and analyzed to characterize the metabolites of berberrubine in vivo for the first time. A total of 57 metabolites were identified, including 54 metabolites in urine, 39 metabolites in plasma, 28 metabolites in bile and 18 metabolites in feces. The results indicated that demethylenation, reduction, hydroxylation, demethylation, glucuronidation, and sulfation were the major metabolic pathways of berberrubine in vivo.


Subject(s)
Berberine/analogs & derivatives , Metabolome , Administration, Oral , Animals , Berberine/metabolism , Berberine/pharmacokinetics , Bile/chemistry , Chromatography, High Pressure Liquid , Feces/chemistry , Male , Mass Spectrometry , Plasma/chemistry , Rats , Rats, Sprague-Dawley
19.
Eur J Med Chem ; 141: 92-100, 2017 Dec 01.
Article in English | MEDLINE | ID: mdl-29028535

ABSTRACT

Scutellaria baicalensis Georgi (S. baicalensis), as a traditional Chinese herbal medicine, is an important component of several famous Chinese medicinal formulas for treating patients with diabetes mellitus. Baicalin (BG), a main bioactive component of S. baicalensis, has been reported to have antidiabetic effects. However, pharmacokinetic studies have indicated that BG has poor oral bioavailability. Therefore, it is hard to explain the pharmacological effects of BG in vivo. Interestingly, several reports show that BG is extensively metabolized in rats and humans. Therefore, we speculate that the BG metabolites might be responsible for the pharmacological effects. In this study, BG and its three metabolites (M1-M3) were examined their effects on glucose consumption in insulin resistant HepG-2 cells with a commercial glucose assay kit. Real-time PCR and western blot assay were used to confirm genes and proteins of interest, respectively. The results demonstrate that BG and its metabolites (except for M3) enhanced the glucose consumption which might be associated with inhibiting the expression of the key gluconeogenic genes, including glucose-6-phosphatase (G6Pase), phosphoenolypyruvate carboxykinase (PEPCK) and glucose transporter 2 (GLUT2). Further study found that BG and M1 could suppress hepatic gluconeogenesis via activation of the AMPK pathway, while M2 could suppress hepatic gluconeogenesis via activation of the PI3K/AKT signaling pathway. Taken together, our findings suggest that both BG and its metabolites have antihyperglycemic activities, and might be the active forms of oral doses of BG in vivo.


Subject(s)
AMP-Activated Protein Kinases/metabolism , Flavonoids/pharmacology , Gluconeogenesis/drug effects , Hypoglycemic Agents/pharmacology , Insulin-Secreting Cells/drug effects , Proto-Oncogene Proteins c-akt/metabolism , Cell Survival/drug effects , Dose-Response Relationship, Drug , Flavonoids/chemistry , Flavonoids/metabolism , Hep G2 Cells , Humans , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/metabolism , Insulin Resistance , Molecular Structure , Structure-Activity Relationship , Tumor Cells, Cultured
20.
Mol Cell Biochem ; 415(1-2): 145-55, 2016 Apr.
Article in English | MEDLINE | ID: mdl-27000859

ABSTRACT

Physalin A (PA) is an active withanolide isolated from Physalis alkekengi var. franchetii, a traditional Chinese herbal medicine named Jindenglong, which has long been used for the treatment of sore throat, hepatitis, and tumors in China. In the present study, we firstly investigated the effects of PA on proliferation and cell cycle distribution of the human non-small cell lung cancer (NSCLC) A549 cell line, and the potential mechanisms involved. Here, PA inhibited cell growth in dose- and time-dependent manners. Treatment of A549 cells with 28.4 µM PA for 24 h resulted in approximately 50 % cell death. PA increased the amount of intracellular ROS and the proportion of cells in G2/M. G2/M arrest was attenuated by the addition of ROS scavenger NAC. ERK and P38 were triggered by PA through phosphorylation in a time-dependent manner. The phosphorylation of ERK and P38 were not attenuated by the addition of NAC, but the use of the p38 inhibitor could reduce, at least in part, PA-induced ROS and the proportion of cells in G2/M. PA induces G2/M cell cycle arrest in A549 cells involving in the p38 MAPK/ROS pathway. This study suggests that PA might be a promising therapeutic agent against NSCLC.


Subject(s)
Carcinoma, Non-Small-Cell Lung/pathology , Cell Division/drug effects , G2 Phase/drug effects , Lung Neoplasms/pathology , Reactive Oxygen Species/metabolism , Withanolides/pharmacology , p38 Mitogen-Activated Protein Kinases/metabolism , Acetylcysteine/administration & dosage , Carcinoma, Non-Small-Cell Lung/enzymology , Carcinoma, Non-Small-Cell Lung/metabolism , Cell Line, Tumor , Humans , Lung Neoplasms/enzymology , Lung Neoplasms/metabolism , Phosphorylation
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