Structure-activity relationship of neuropeptide gamma derived from mammalian and fish.

This study of relationship between structure and biologic activity was performed using five neuropeptide gammas [NPgamma; mammalian-NPgamma (M-NPgamma), trout-NPgamma (T-NPgamma), goldfish-NPgamma (G-NPgamma), bowfin-NPgamma (B-NPgamma), and shark-NPgamma (S-NPgamma)]. Circular dichroism (CD) spectra showed that all peptides took random structure in buffer solution. In neutral and acidic liposomes, M-NPgamma, T-NPgamma, B-NPgamma, and S-NPgamma still adopted random structure, while G-NPgamma had an alpha-helical structure. The biologic activity of NPgammas has been estimated by their effects on the intestinal motility and arterial relaxation. The intestinal motility was investigated with rat duodenum (RD), carp intestine (CI), and guinea-pig ileum (GPI). The arterial relaxing effect was tested with guinea-pig aorta (GPA) and rat mesenteric artery (RMA). In RD, the order of potency compared with the EC50 value was M-NPgamma > S-NPgamma > B-NPgamma > G-NPgamma > T-NPgamma. G-NPgamma was the most contractile agent in CI. S-NPgamma was the most contractile agent in GPI. Using an arterial relaxing test, the order of potency was G-NPgamma > T-NPgamma > B-NPgamma > S-NPgamma > M-NPgamma in GPA, and all NPgammas remarkably reduced relaxing activity in RMA. Despite their structural similarities to NPgammas, G-NPgamma has high affinity to tachykinin receptor-binding sites in GPA and CI, indicating an alpha-helical structure may have a critical role for receptor binding. However, an alpha-helical structure does not play a critical role in recognizing receptor-binding sites in RD and GPI.     

Modulation of catalase in human skin in vivo by acute and chronic UV radiation.

In this study, we demonstrate that catalase is differently regulated either by acute, or chronic UV radiation during the photoaging process. 2MED of UV radiation decreased the activity and expression of catalase gradually in the epidermis and dermis at between 24 and 48 h after the UV exposure. These levels then returned to near normal by 72 h after exposure. The catalase mRNA was also decreased in the skin 24 h after UV irradiation to 50% of the control level, and then started to recover. In contrast, chronic UV irradiation over a lifetime (approximately 50 years) increased the catalase activity in the epidermis and dermis of the human skin in vivo. Our results suggest that catalase might be one of the important enzymes in the skin aging process, and that it plays an important role in the photoprotection of the skin from UV light.     

Plant defense gene promoter enhances the reliability of<Emphasis Type="Italic"> shiva-1</Emphasis> gene-induced resistance to soft rot disease in potato

PAL5, a tomato (Lycopersicon esculentum Mill.) plant defense gene that encodes phenylalanine ammonia-lyase, is known to respond to a variety of environmental stresses including pathogen infection and wounding. A shiva-1 gene recombinant that encodes a small synthetic antibacterial peptide under the PAL5 gene promoter was transformed into potato (Solanum tuberosum L.) and its ability to induce resistance to Erwinia carotovora was compared with a construct under the control of the constitutive and widely used cauliflower mosaic virus (CaMV) 35S promoter. The shiva-1 peptide, an analog of natural cecropin B, was shown previously to have high bactericidal activity in vitro, but when expressed in vivo under the control of the CaMV 35S promoter, the effects were very inconsistent. As observed previously, in the present studies a few transformants with the CaMV 35S promoter were highly resistant when assayed for susceptibility to soft rot disease. In marked contrast the majority of transformants with the PAL5 gene promoter were highly resistant. More-detailed analyses of the incorporated DNA indicated that most of the transformants with the CaMV 35S promoter contained multiple copies of the transforming DNA while all of the PAL5 recombinants contained single copies. The highly resistant CaMV 35S recombinant also was present as a single copy. The results indicate that, at least in this instance, a constitutive promoter may not be ideal for the effective expression of a foreign gene and suggest that multiple insertions may have negative consequences.     

A surgical approach for earlobe keloid: keloid fillet flap

Earlobe keloid can form after cosmetic ear piercing, trauma, or burns, and it poses several difficulties in treatment and distinctive cosmetic implications. Treatment methods for earlobe keloids include both surgical and nonsurgical methods. After excision of the earlobe keloid, healing by secondary intention, primary suture, skin graft, or local flap has revealed some disadvantages. The authors approached this problem with a new excision and covering method. The surgery was performed under local anesthesia. Skin over the keloid was dissected from the keloid mass as a flap, which they termed a "keloid fillet flap," and the keloid mass was completely removed. Subcutaneous sutures were not used, and the keloid fillet flaps were closed with 6-0 nylon sutures after trimming. Other intraoperative or postoperative preventive procedures, such as steroid injection, pressure device, or irradiation, were not applied primarily. In the period from May of 1999 to October of 2000, nine earlobe keloids in eight patients were treated with this protocol. One patient had bilateral keloids. Of the eight patients, there were six women and two men, ranging in age from 21 to 61 years (mean age, 28.5 years). The causes of keloids were ear piercing in six cases and trauma in three cases. The largest lesion was 3 cm in its greatest dimension, and the smallest was 1.5 cm (mean, 2.3 cm). All flaps survived completely. There were four cases of recurrence. Seven cases, including two recurrences, showed good results. The authors believe the recurrence of earlobe keloid was closely related to the method for coverage of the defect after its surgical excision, and the "5 As and one B" (Asepsis, Atraumatic technique, Absence of raw surface, Avoidance of tension, Accurate approximation of wound margin, and complete Bleeding control) are important factors in reducing the recurrence rate of earlobe keloids in surgical excision. The authors' protocol is very effective in closing the defect after surgical excision of earlobe keloids and offers many advantages over other surgical approaches. The recurrence rate of earlobe keloid may be lower than in their results if other intraoperative and postoperative treatment procedures are combined with their protocol.     

Structural basis for the selective inhibition of JNK1 by the scaffolding protein JIP1 and SP600125

The c-jun N-terminal kinase (JNK) signaling pathway is regulated by JNK-interacting protein-1 (JIP1), which is a scaffolding protein assembling the components of the JNK cascade. Overexpression of JIP1 deactivates the JNK pathway selectively by cytoplasmic retention of JNK and thereby inhibits gene expression mediated by JNK, which occurs in the nucleus. Here, we report the crystal structure of human JNK1 complexed with pepJIP1, the peptide fragment of JIP1, revealing its selectivity for JNK1 over other MAPKs and the allosteric inhibition mechanism. The van der Waals contacts by the three residues (Pro157, Leu160, and Leu162) of pepJIP1 and the hydrogen bonding between Glu329 of JNK1 and Arg156 of pepJIP1 are critical for the selective binding. Binding of the peptide also induces a hinge motion between the N- and C-terminal domains of JNK1 and distorts the ATP-binding cleft, reducing the affinity of the kinase for ATP. In addition, we also determined the ternary complex structure of pepJIP1-bound JNK1 complexed with SP600125, an ATP-competitive inhibitor of JNK, providing the basis for the JNK specificity of the compound.     

Production of high molecular weight pullulan by Aureobasidium pullulans HP-2001 with soybean pomace as a nitrogen source

The production of pullulan by Aureobasidium pullulans HP-2001 was enhanced by yeast extract as a nitrogen source as well as soybean pomace. The highest production of pullulan by A. pullulans HP-2001 with yeast extract was 5.5 g/l whereas that of pullulan with soybean pomace was 7.5 g/l. The gas chromatogram of pullulan produced by A. pullulans HP-2001 with soybean pomace as a nitrogen source showed that the major and minor components were glucose and mannose. The FTIR spectra of pullulans produced with yeast extract, a mixture of yeast extract and soybean pomace, and soybean pomace alone exhibited similar features. The increase in content of reducing sugars after pullulanase treatment of pullulans produced with different nitrogen sources indicated that all the pullulans had alpha-(1,6) glucosidic linkages of alpha-(1,4) linked maltotriose units. The average molecular weights of pullulans produced with various concentrations of yeast extract and soybean pomace ranged from 0.17 to 1.32x10(6) and from 1.32 to 5.66x10(6), respectively. All pullulans produced by A. pullulans HP-2001 in this study had the same basic structures, but their ratios of monomeric components were a little different, which might result in the production of pullulans with different molecular weights.     

Syntheses and anti-MRSA activities of the C3 analogs of mansonone F, a potent anti-bacterial sesquiterpenoid: insights into its structural requirements for anti-MRSA activity

Syntheses and excellent anti-MRSA activities of the mansonone F analogs are reported. In addition, the minimal structural requirements for its anti-MRSA activities as well as its structure-activity relationship including the C3 substituents effects on anti-MRSA activity are also described. In particular, this study revealed that both ortho-quinone and tricyclic systems of mansonone F are essential for anti-MRSA activities.     

Syntheses and radical scavenging activities of resveratrol derivatives

Nine new resveratrol derivatives, having bromo, iodo, and fluoroethyl groups, were designed and synthesized. All compounds having free phenol groups showed good free radical scavenging activity. Among them, 2-bromoresveratrol 19 has a similar free radical scavenging activity to (+)-catechin.