Animals ; Cadmium ; toxicity ; Cytochrome P-450 Enzyme System ; blood ; Female ; Ovary ; drug effects ; metabolism ; Phosphoproteins ; blood ; Progesterone ; biosynthesis ; Rats ; Rats, Wistar

OBJECTIVE:To study the preparation technology of Chinese traditional medicine Seborrhea liniment.METHODS:The preparation technology of Seborrhea liniment was optimized by orthogonal experiment design L9(34)using 60% alcohol as solvent with the content of Berberine hydrochloride as index for evaluation and with the extraction method,extraction time,amount of solvent and number of extraction times as factors.RESULTS:The optimum preparation technical conditions were as follows:by impregnating method,the extraction time was 48 h using 1 500 mL alcohol and the extraction frequency was 2 times.CONCLUSION:The preparation technology of Chinese traditional medicine Seborrhea liniment is stable and feasible,and it serves as a theoretical basis for the industrial production.

We designed and synthesized eighteen lycorine derivatives with five different structural types, and evaluated their antiviral activities on a HCoV-OC43-infected H460 cell model. Structure-activity relationships suggested that the introduction of appropriate substituents on the 6N atom of lycorine was beneficial to activity. Compound 6a gave a good activity with the half effective concentration (EC₅₀) and selectivity index (SI) values of 2.36 μmol·L^-1 and 16.52, respectively. Surface plasmon resonance (SPR) result indicated that 6a might target the non-structural protein 12 (NSP12) subunit in RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2 with the dissociation constant (K_D) value of 1.36 μmol·L^-1. Molecular docking indicated that 6a might act on nidovirus RdRp-associated nucleotidyltransferase (NiRAN) catalytic center of NSP12, distinct from the mechanism of nucleoside-like drugs such as remdesivir. This study provides scientific data for the development of lycorine derivatives into a new class of anti-SARS-CoV-2 small molecule inhibitors.

To apply chitooligosaccharide in the preparation of baicalin compound, in order to increase the drug dissolution in vitro, and investigate the basic property of the compound. Baicalin-chitooligosaccharide compound was prepared by using the solvent method. The structure and physicochemical properties of compound were analyzed by using differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray powder diffraction (XRD) and infrared vibrational spectrum (IR), and its dissolution behavior was also investigated. The results showed that the compound prepared at baicalin-chitooligosaccharide molar ratio of 1 : 1 could significantly improve the dissolution of baicalin. The results of DSC and XRD analysis suggested that baicalin may exist in an amorphous state. IR results indicated the interaction between baicalin and chitooligosaccharide. The baicalin-chitooligosaccharide compound could significantly improve dissolution in vitro of drug.
Calorimetry, Differential Scanning ; Chemistry, Pharmaceutical ; Drug Carriers ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Flavonoids ; chemistry ; Oligosaccharides ; chemistry ; Spectroscopy, Fourier Transform Infrared

A new eremophilane derivative, (3aR,4R,5S,7S,7aS)-2-acetyl-7,7a-dihydroxy-3a,4-dimethyl-3a,4,5,6,7,7a-hexahydro-3H-inden-5-yl acetate (1) and three known compounds, 10beta-hydroxy-eremophil-7 (11)-en-12,8alpha-olide(2), beta-sitosterol (3) and beta-daucosterol(4) have been isolated from Ligularia intermedia. The compounds were isolated by column chromatography on silica gel and Sephadex LH-20,and identified on the basis of spectral analyses (MS, 1H-NMR, 13C-NMR).
Asteraceae ; chemistry ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Molecular Structure ; Naphthalenes ; chemistry ; isolation & purification ; Sesquiterpenes

0.01),which were significantly different from group Ⅲ(P

Organic anion transporting polypeptide 1B1 (OATP1B1) is an important liver-specific uptake transporter, which mediates transport of numerous endogenous substances and drugs from blood into hepatocytes. To identify and investigate potential modulators of OATP1B1 from natural products, the effect of 21 frequently used natural compounds and extracts on OATP1B1-mediated fluorescein methotrexate transport was studied by using Chinese hamster ovary cells stably expressing OATP1B1 (CHO-OATP1B1) in 96-well plates. This method could be used for the screening of large compound libraries. Our studies showed that some flavonoids (e.g., quercetin, quercitrin, rutin, chrysanthemum flavonoids and mulberrin) and triterpenoids (e.g., glycyrrhetinic acid and glycyrrhizic acid) were inhibitors of OATP1B1 with IC50 values less than 16 µmol · L(-1). The IC50 value of glycyrrhetinic acid on OATP1B1 was comparable to its blood concentration in clinics, indicating an OATPlB1-mediated drug-drug interaction could occur. Structure-activity relationship analysis showed that flavonoids had much higher inhibitory activity than their glycosides. Furthermore, the type and length of saccharides had a significant effect on their activity. In addition, we used OATP1B1 substrates fluvastatin and rosuvastatin as probe drugs to investigate the substrate-dependent effect of several natural compounds on the function of OATP1B1 in vitro. Our results demonstrated that the effect of these natural products on the function of OATPlB1 was substrate-dependent. In summary, this study would be conducive to predicting and avoiding potential OATP1B1-mediated drug-drug and drug-food interactions and thus provide the experimental basis and guidance for rational drug use.
Animals ; Biological Products ; CHO Cells ; Cricetulus ; Drug Interactions ; Fatty Acids, Monounsaturated ; pharmacology ; Flavonoids ; pharmacology ; Indoles ; pharmacology ; Inhibitory Concentration 50 ; Organic Anion Transporters ; genetics ; metabolism ; Rosuvastatin Calcium ; pharmacology ; Structure-Activity Relationship

Adrenalectomy ; Adult ; Angiomyolipoma ; pathology ; surgery ; Follow-Up Studies ; Humans ; Kidney ; pathology ; Kidney Neoplasms ; pathology ; surgery ; Lymph Node Excision ; Lymph Nodes ; pathology ; Lymphatic Metastasis ; Male ; Nephrectomy ; Ureter ; surgery

The present paper intends to discuss the antioxidant and tyrosinase inhibition effect of solanesol from three aspects of ultraviolet radiation and free radical scavenging. The paper makes a survey on diurnal variation rule of the minimum ultraviolet transmittance and ultraviolet transmittance of solanesol, hydroxyl (OH) free radical scavenging method of Smirnoff reaction system model, superoxide anion O2- free radical scavenging method of pyrogallol autoxidation, and the inhibitory effect of solanesol on tyrosinase activity by enzyme kinetic method. The experiment results showed that solanesol could effectively scavenge lipid radicals to block lipid peroxidation, and inhibit effects on tyrosinase. Solanesol is a natural extract which could be used to prevent senile atrophy of human skin and senile plaque.
Enzyme Inhibitors ; chemistry ; Free Radical Scavengers ; chemistry ; Humans ; Hydroxyl Radical ; chemistry ; Lipid Peroxidation ; Monophenol Monooxygenase ; antagonists & inhibitors ; Terpenes ; chemistry ; Ultraviolet Rays