Evaluation of the ileal digestibility and excreta retention of phosphorus for feed phosphates in broiler chickens and in Pekin ducks.

The study aimed to determine the ileal phosphorus (P) digestibility (iPD) and the excreta P retention (ePR) of 5 monodicalcium phosphate (MCP) samples and 3 dicalcium phosphate (DCP) samples in broiler chickens and in Pekin ducks using the substitution method. A total of 720, 21-d-old Arbor Acres broiler chickens in experiment 1 and 720, 15-d-old Pekin ducks in experiment 2 were randomly allocated to 9 dietary treatments with 8 replicate cages (10 birds/cage) based on the similar mean body weight, respectively. The collection of excreta (for 72 h after a 3-d acclimation) and ileal digesta (after 6 d of feeding experimental diets) was done. The results showed the average iPD/ePR of MCP and DCP for broilers were 83.11%/74.52% and 75.34%/69.46% and for ducks were 79.37%/80.02% and 75.74%/76.44%, respectively. The iPD/ePR of MCP in broilers and the ePR of MCP in ducks were markedly higher (P < 0.05) than those of DCP. Our data suggest that using the substitution method to evaluate the bioavailability of feed phosphates has its own advantages; MCP has higher biological availability than DCP for broilers and ducks.

Clinical efficacy of targeted therapy, immunotherapy combined with hepatic artery infusion chemotherapy (FOLFOX), and lipiodol embolization in the treatment of unresectable hepatocarcinoma.

To evaluate the clinical efficacy of targeted therapy and immunotherapy combined with hepatic arterial infusion chemotherapy (HAIC) of FOLFOX and lipiodol embolization in the treatment of unresectable hepatocellular carcinoma. Patients included in the study were those who received targeted therapy and immunotherapy combined with HAIC of FOLFOX and lipiodol embolization in Zhongshan People's Hospital from December 2020 to June 2021 for unresectable hepatocellular carcinoma. Evaluation indicators included objective response rate (ORR), median progression-free survival (mPFS), median duration of response (mDOR), 1-year overall survival rate (OS), surgical conversion rate, and adverse events. Treatment response was assessed using Response Evaluation Criteria in Solid Tumors (mRECIST and RECIST v1.1). A total of 35 patients were included in this study, 30 of whom completed treatment evaluation. According to mRECIST evaluation criteria, the objective response rate (ORR) was 83.3% (25/30); the complete response (CR) was 60% (18/30); the partial response (PR) was 23.3% (7/30), and stable disease (SD) was 16.7% (5/30). The mDOR was 10.3 months (95% Cl: 8.27-NE), and the mPFS was 13.2 months (95% CI: 10.3-NE); the surgical conversion rate was 30.0% (9/30). The 1-year OS was 96.7%. There were no serious surgical complications and grade 4 or 5 adverse events of targeted therapy, immunotherapy and HAIC. Some patients had grade 3 adverse reactions in gastrointestinal toxicity or hepatotoxicity, and the adverse reactions were improved after corresponding symptomatic treatment. We concluded that HAIC of FOLFOX and lipiodol embolization combined with targeted therapy and immunotherapy had a significant curative effect in the treatment of unresectable hepatocellular carcinoma, with no serious adverse reactions and a high rate of surgical conversion rate.

An acidic pectin lyase from Aspergillus niger with favourable efficiency in fruit juice clarification.

The pectin lyase gene pnl-zj5a from Aspergillus niger ZJ5 was identified and expressed in Pichia pastoris. PNL-ZJ5A was purified by ultrafiltration, anion exchange and gel chromatography. The Km and Vmax values determined using citrus pectin were 0.66 mg ml(-1) and 32.6 µmol min(-1) mg(-1) , respectively. PNL-ZJ5A exhibited optimal activity at 43°C and retained activity over 25-50°C. PNL-ZJ5A was optimally active at pH 5 and effective in apple juice clarification. Compared with controls, PNL-ZJ5A increased the fruit juice yield significantly. Furthermore, PNL-ZJ5A reduced the viscosity of apple juice by 38.8% and increased its transmittance by 86.3%. PNL-ZJ5A combined with a commercial pectin esterase resulted in higher juice volume.

Characterization of an anther- and tapetum-specific gene and its highly specific promoter isolated from tomato.

A full-length genomic clone of 2,233 bp long containing an anther- and tapetum-specific gene TomA108 was isolated and characterized from tomato. The gene was present in one copy per haploid genome. The isolated clone contained 5' and 3' untranslated regions of 810 and 170 nucleotides, respectively and a single intron with highly repetitive sequences. The cDNA encoded the protein with an apparent mass of 10.6 kDa and a pI (isoelectric point) of 5.3. It was cysteine-rich and had an N-terminal hydrophobic domain with characteristics of a secretory signal. Amino acid sequence comparisons demonstrated that the protein was closely related to a family of cereal seed storage proteins and protease inhibitors. The fusion of beta-glucuronidase to the TomA108 promoter demonstrated that the promoter was highly active from early-meiosis to free microspores production in tapetum of tobacco. This strong and highly specific promoter can be potentially used to generate male sterility for efficient production of plant hybrids.

Two new saponins from the bud of Aralia elata (Miq.) Seem.

Two new saponins, named congmuyanoside A and congmuyanoside B, have been isolated from the buds of Aralia elata (Miq.) Seem. Their structures have been determined on the basis of chemical and spectroscopic evidence.

Ocular hypotensive FP prostaglandin (PG) analogs: PG receptor subtype binding affinities and selectivities, and agonist potencies at FP and other PG receptors in cultured cells.

Natural prostaglandins (PGs) such as PGD2, PGE2, PGF2(2alpha), and PGI2 exhibited the highest affinity for their respective cognate receptors, but were the least selective agents when tested in receptor binding assays. Travoprost acid ([+]-fluprostenol) was the most FP-receptor-selective compound, exhibiting a high affinity (Ki = 35 +/- 5 nM) for the FP receptor, and minimal affinity for DP (Ki = 52,000 nM), EP1 (Ki = 9540 nM), EP3 (Ki = 3501 nM), EP4 (Ki = 41,000 nM), IP (Ki > 90,000 nM), and TP (Ki = 121,000 nM) receptors. Travoprost acid was the most potent PG analog tested in FP receptor functional phosphoinositide turnover assays in the following cell types: human ciliary muscle (EC50 = 1.4 nM), human trabecular meshwork (EC50 = 3.6 nM), and mouse fibroblasts and rat aortic smooth muscle cells (EC50 = 2.6 nM). Although latanoprost acid exhibited a relatively high affinity for the FP receptor (Ki = 98 nM), it had significant functional activity at FP (EC50 = 32-124 nM) and EP1 (EC50 = 119 nM) receptors. Bimatoprost acid was less selective, exhibiting a relatively high affinity for the FP (Ki = 83 nM), EP1 (Ki = 95 nM), and EP3 (Ki = 387 nM) receptors. Bimatoprost acid exhibited functional activity at the EP1 (EC50 = 2.7 nM) and FP (EC50 = 2.8-3.8 nM in most cells) receptors. Bimatoprost (nonhydrolyzed amide) also behaved as an FP agonist at the cloned human FP receptor (EC50 = 681 nM), in h-TM (EC50 = 3245 nM) and other cell types. Unoprostone and S-1033 bound with low affinity (Ki = 5.9 microM to > 22 microM) to the FP receptor, were not selective, but activated the FP receptor. In conclusion, travoprost acid has the highest affinity, the highest FP-receptor-selectivity, and the highest potency at the FP receptor as compared to the other ocular hypotensive PG analogs known so far, including free acids of latanoprost, bimatoprost, and unoprostone isopropyl ester.

Levobetaxolol (Betaxon) and other beta-adrenergic antagonists: preclinical pharmacology, IOP-lowering activity and sites of action in human eyes.

The pharmacological characteristics of levobetaxolol, a single active isomer of betaxolol, were determined and compared with activities of other beta-adrenoceptor antagonists. Levobetaxolol (43-fold beta1-selective) exhibited a higher affinity at cloned human beta1 (Ki = 0.76 nM) than at beta2 (Ki = 32.6 nM) receptors, while dextrobetaxolol was much weaker at both receptors. Levobetaxolol potently antagonized functional activities at cloned human beta1 and beta2 receptors, and also at guinea pig atrial beta1, tracheal beta2 and rat colonic beta3 receptors (IC50s = 33.2 nM, 2970 nM and 709 nM, respectively). Thus, levobetaxolol was 89-times beta1-selective (vs beta2). Levobetaxolol (Ki = 16.4 nM) was more potent than dextrobetaxolol (Ki = 2.97 microM) at inhibiting isoproterenol-induced cAMP production in human non-pigmented ciliary epithelial cells. Levobunolol and (l)-timolol had high affinities at beta1 and beta2 receptors but were considerably less beta1-selective than levobetaxolol. Levo-, dextro- and racemic-betaxolol exhibited little or no affinity, except at sigma sites and Ca2+-channels (IC50s > 1 microM), at 89 other receptor/ligand binding sites. Levobetaxolol exhibited a micromolar affinity for L-type Ca2+-channels. In conscious ocular hypertensive cynomolgus monkeys, levobetaxolol was more potent than dextrobetaxolol, reducing intraocular pressure by 25.9+/-3.2% at a dose of 150 microg/eye (n = 15-30). Quantitative [3H]-levobetaxolol autoradiography revealed high levels of binding to human ciliary processes, iris, choroid/retina, and ciliary muscles. In conclusion, levobetaxolol is a potent, high affinity and beta1-selective IOP-lowering beta-adrenoceptor antagonist.

A new triterpenoidal saponin from Ixeris sonchifolia and its cytotoxic activity.

A new triterpenoidal saponin, echinocystic acid 3-O-beta-D-glucopyranosyl-(1-->3)-alpha-L-arabinopyranoside (1), was isolated from Ixeris sonchifolia. Its structure was elucidated on the basis of full spectral data analysis and chemical methods. The cytotoxic activity of compound 1 was evaluated using the tumor cell lines of A375, Hela, and L929 in vitro.

A pair of 24-hydroperoxyl epimeric dammarane saponins from flower-buds of Panax ginseng.

Further investigation on the saponins of the flower-buds of Panax ginseng C. A. Meyer has resulted in the isolation and structural elucidation of a pair of new 24-epimers of dammarane type saponins named ginsenoside I and II. The structures of the epimers were characterized on the basis of chemical and spectral evidence as 3-O-[beta-D-glucopyranosyl-(1-->2)-beta-D-glucopyranosyl]-20-S-O-beta-D-glucopyranosyl-3beta, 12beta,20(S)-trihydroxy-24xi-hydroperoxydammar-25-ene, except for their C-24 configurations. Ginsenoside I is a new triterpene glycoside, and ginsenoside II is a known compound first isolated from a natural plant.

Flavonoid ketohexosefuranosides from the leaves of Crataegus pinnatifida Bge. var. major N.E.Br.

Four flavonoid ketohexosefuranosides, pinnatifinoside A, pinnatifinoside B, pinnatifinoside C, and pinnatifinoside D were isolated from the leaves of Crataegus pinnatifida Bge. var. major N.E.Br. Their structures were elucidated by spectroscopic analysis (UV, IR, MS and 1D, 2D NMR) and chemical evidence.

Two novel flavonoid glycosides from Crataegus pinnatifida Bge.var.major N.E.Br.

Two novel natural products, namely pinnatifida C, pinnatifida D, were isolated from the leaves of Crataegus pinnatifida Bge.var.major N.E.Br. Their structures were elucidated by the spectroscopic analysis and chemical evidence.

A new sesquiterpene lactone glucoside from Ixeris sonchifolia.

A new sesquiterpene lactone glucoside, Ixerin Z1 (1), was isolated from the whole plants of Ixeris sonchifolia (Bge.) Hance, along with 15 known compounds. The structure of 1 was elucidated as 1(10),3,11(13)-guaiatriene-12,6-olide-2-one-3-O-[6'-(p-hydroxyphenylacetyl)]-glucopyranoside by spectroscopic methods including 2D-NMR techniques.

[Chemical constituents from the leaves of crataegus pinnatifida Bge. var. major N.E.Br].

AIM: To study the chemical constituents in the leaves of Crataegus pinnatifida Bge. var. major N.E.Br.. METHODS: Compounds were isolated by using porous resin, silica gel, polyamide chromatographic techniques etc. Their structures were elucidated by chemical and spectroscopic methods. RESULTS: Eight compounds were identified as pinnatifin I (1), quercetin (2), 3-O-beta-D-glucopyranosyl quercetin (3), 3-O-beta-D-galacopyranosyl quercetin (4), 3-O-beta-D-glucopyranosyl (6-->1)-alpha-L-rhamnosyl quercetin (5), 3-O-beta-D-galacopyranosyl (6-->1)-alpha-L-rhamnosyl quercetin (6), kaempferol (7), 7-O-alpha-L-rhamnosyl-3-O-beta-D- glucopyranosyl kaempferol (8). CONCLUSION: Compound 1 is a new compound. Compound 8 was isolated from this plant for the first time.

[Quantitative determination of icariin in "tangzhi shuangjiang cha" by high performance liquid chromatography].

Icariin in "Tangzhi Shuangjiang Cha" was quantitatively determined by HPLC with ODS column, a mixture of MeOH-H2O(60:40, V/V) as mobile phase and UV detection at 270 nm. There was a good linear relationship within the range of 0.1 g/L-0.5 g/L(r = 0.9993). The average recovery was 101.4%, RSD was below 2.7%(n = 3). The method is rapid, simple, accurate and reproducible. And the method is proposed to be used for quality control of "Tangzhi Shuangjiang Cha".

Anti-proliferative effect of ginseng saponins on human prostate cancer cell line.

Ginseng is a medicinal herb widely used in Asian countries, and many of its pharmacological actions are attributed to the ginsenosides. In a study of the anti-proliferative activity of ginsenosides using human prostate carcinoma LNCaP cell line, ginsenoside Rg3 displayed growth inhibitory activity. The cells lost its adherent property after incubation in the presence of 250 microM of ginsenoside for 48h. The expression of biomarker genes, including prostate specific antigen (PSA), androgen receptor (AR) and 5alpha-reductase (5alphaR), and that of the proliferating cell nuclear antigen (PCNA), were suppressed. Ginsenoside Rg3 induced classic apoptotic morphology and interfered with the expression of apoptosis-related genes, bcl-2 and caspase-3, in LNCaP cells, as demonstrated by fluorescence microscopy, flow cytometry and reverse transcriptase-polymerase chain reaction. Taken our results together, we suggested that ginsenoside Rg3 activated the expression of cyclin-kinase inhibitors, p21 and p27, arrested LNCaP cells at G1 phase, and subsequently inhibited cell growth through a caspase3-mediated apoptosis mechanism.

Four new saponins from the root bark of Aralia elata.

Four new saponins, 3-O-[beta-D-glucopyranosyl(1-->3)-alpha-L-arabinopyranosyl]-16a lpha-hydroxyoleanolic acid 28-O-beta-D-glucopyranosyl ester (called aralia-saponin I), 3-O-[beta-D-glucopyranosyl(1-->3)-alpha-L-arabinopyranosyl]-16a lpha-hydroxyhederagenin 28-O-beta-D-glucopyranosyl ester (aralia-saponin II), 3-O-[beta-D-glucopyranosyl(1-->3)-beta-D-glucopyranosyl(1-->3)-alpha-L-+ ++arabinopyranosyl]-16alpha-hydroxyoleanolic acid 28-O-beta-D-glucopyranosyl ester (aralia-saponin III), 3-O-[beta-D-glucopyranosyl(1-->3)-beta-D-gucopyranosyl(1-->3)-beta -D-glucucopyranosyl]-16alpha-hydroxyoleanolic acid 28-O-beta-D-glucopyranosyl ester (aralia-saponin IV), were isolated from the root bark of Aralia elata (Miq.) Seem., together with nineteen known compounds including glycosides of (20S)-protopanaxadiol and (20S)-protopanaxatriol. Their structures were determined on the basis of chemical and spectroscopy methods.

Steroidal saponins from Anemarrhena asphodeloides and their effects on superoxide generation.

A new steroidal saponin, timosaponin F, along with six known compounds was isolated from the rhizomes of Anemarrhena asphodeloides Bge. On the basis of chemical and spectroscopic evidence, the structure of timosaponin F was elucidated as (5beta, 25 S):-spirostan-3beta,15alpha,23alpha-triol-3-O-beta- glucopyranosyl-(1--->2)-beta-galactopyranoside. The six known compounds were anemarrhenasaponin I, anemarrhenasaponin Ia, timosaponin BI, timosaponin BII, timosaponin B, timosaponin AIII; their effects on superoxide generation are also reported.

Two new 6-alkylcoumarins from Angelica pubescens f. biserrata.

Two new 6-alkylcoumarins, angelitriol (1) and angelol J (2), were isolated from the EtOAc-soluble fraction of the roots of Angelica pubescens Maxim f. biserrata Shan et Yuan. Their structures were elucidated as 6-[(1R,2S)-1,2,3-trihydroxy-3-methylbutyl]-7-methoxycoumarin (1) and 6-[(1R,2R)-1-ethoxy-2,3-dihydroxy-3-methylbutyl]-7-methoxycoumarin (2), respectively, on the basis of spectral evidence. Both of them showed strong inhibitory effects on human platelet aggregation.

Angelol-type coumarins from Angelica pubescence F. biserrata and their inhibitory effect on platelet aggregation.

An ethyl acetate-soluble root extract of Angelica pubescence f. biserrata afforded two new angelol-type coumarins, angelols K and L, in addition to angelols B, C, D and G. Some of the compounds were tested on human platelet aggregation and showed significant activity.

Dauricoside, a new glycosidal alkaloid having an inhibitory activity against blood-platelet aggregation.

Dauricoside (1), a new glycosidal alkaloid, was isolated from the rhizomes of Menispermum dauricum DC. along with dauricine (2), daurisoline (3), dauriporphine (4), menisporphine (5), and 6-O-demethylmenisporphine (6), and its structure was determined by means of spectroscopic methods. Compounds 1, 2, and 3 inhibited blood-platelet aggregation induced by adenosine 5'-diphosphate (ADP).