Photodynamic therapy with Pd-Bacteriopheophorbide (TOOKAD): successful in vivo treatment of human prostatic small cell carcinoma xenografts

Small cell carcinoma of the prostate (SCCP), although relatively rare, is the most aggressive variant of prostate cancer, currently with no successful treatment. It was therefore tempting to evaluate the response of this violent malignancy and its bone lesions to Pd-Bacteriopheophorbide (TOOKAD)-based photodynamic therapy (PDT), already proven by us to efficiently eradicate other aggressive non-epithelial solid tumors. TOOKAD is a novel bacteriochlorophyll-derived, second-generation photosensitizer recently, developed by us for the treatment of bulky tumors. This photosensitizer is endowed with strong light absorbance (epsilon(0) approximately 10(5) mol(-1) cm(-1)) in the near infrared region (lambda=763nm), allowing deep tissue penetration. The TOOKAD-PDT protocol targets the tumor vasculature leading to inflammation, hypoxia, necrosis and tumor eradication. The sensitizer clears rapidly from the circulation within a few hours and does not accumulate in tissues, which is compatible with the treatment of localized tumor and isolated metastases. Briefly, male CD1-nude mice were grafted with the human SCCP (WISH-PC2) in 3 relevant anatomic locations: subcutaneous (representing tumor mass), intraosseous (representing bone metastases) and orthotopically within the murine prostate microenvironment. The PDT protocol consisted of i.v. administration of TOOKAD (4 mg/kg), followed by immediate illumination (650-800 nm) from a xenon light source or a diode laser emitting at 770 nm. Controls included untreated animals or animals treated with light or TOOKAD alone. Tumor volume, human plasma chromogranin A levels, animal well being and survival were used as end points. In addition, histopathology and immunohistochemistry were used to define the tumor response. Subcutaneous tumors exhibited complete healing within 28-40 days, reaching an overall long-term cure rate of 69%, followed for 90 days after PDT. Intratibial WISH-PC2 lesions responded with complete tumor elimination in 50% of the treated mice at 70-90 days after PDT as documented histologically. The response of the orthotopic model was also analyzed histologically with similar results. The study with this model suggests that TOOKAD-based PDT can reach large tumors and is a feasible, efficient and well-tolerated approach for minimally invasive treatment of local and disseminated SCCP.     

Radiobromination of closo‐carboranes using palladium‐catalyzed halogen exchange

closo‐Carborane derivatives are often proposed as boron carriers for use in boron neutron capture therapy (BNCT) of cancer. A positron emitting radiolabel on a boron atom in such carborane compounds might facilitate pharmacokinetic studies in patients. In this paper the four iodo‐closo‐carboranes, namely 3‐iodo‐ortho‐carborane, 9‐iodo‐ortho‐carborane, 9‐iodo‐meta‐carborane and 2‐iodo‐para‐carborane were chosen as model compounds in a study of [⁷⁶Br]bromine labelling of carboranes using palladium‐catalyzed halogen exchange. It was found that within a reaction time of 40 min, the four compounds were all radio‐brominated in good to excellent yield, using Herrmann's catalyst (HC) in toluene. Copyright © 2005 John Wiley & Sons, Ltd.     

石墨炉原子吸收法测定盐酸伐昔洛韦中钯的残留量

目的建立盐酸伐昔洛韦中钯残留量的测定方法。方法采用微波消解系统消解样品,石墨炉原子吸收分光光度法测定盐酸伐昔洛韦中钯的残留量。结果钯在浓度1．0-30．0ug·L-1内呈良好线性关系（r=0．9995）。检出限为0．20ug·L-1,定量限为0．95ug·L-1,特征浓度（灵敏度）为0．57ug·L-1,平均回收率为101．69％。结论采用本法测定盐酸伐昔洛韦中钯的残留量灵敏、准确、可靠,为药品质量控制提供依据。     

New developments in jewellery and dental materials

This communication reviews the latest alloys introduced in the fields of jewellery and dental prostheses. For this we have scanned current patents and others to which we have access, and it is evident that, although not always correctly used, the words "antiallergic", "hypoallergic", "non-allergic", "to avoid allergies", etc., now appear frequently, indicating manufacturers' awareness of the problems that nickel can cause. On the other hand, the problems that may be associated with other sensitizing metals, such as cobalt and palladium, are not yet addressed.     

钯催化Suzuki偶联高效合成2-烷基取代碳青霉烯类衍生物

目的高效合成多个2-烷基取代碳青霉烯类化合物。方法通过钯催化下三氟甲磺酰碳青霉烯与烷基硼经由Suzuki偶联高效合成2-烷基取代碳青霉烯化合物。结果反应合成得到多个目标产物,反应条件温和,收率理想。结论在合成2-烷基取代碳青霉烯化合物的简便方法中,由于在C-2位引入了烷基链,由此可制备一系列具有临床应用价值的2-烷基取代碳青霉烯类化合物。     

改进制备钯／陶瓷复合膜化学镀新工艺

对利用渗透作用的化学镀新工艺进行了全面的改进，对陶瓷管所处环境，镀液浓度，沉积温度和镀膜时间以及对钯层沉积量和表面形貌的影响进行了系统的研究。结果表明，镀液浓度，沉积温度和镀膜时间对钯层沉积量和表面形貌具有较为明显的影响，而陶瓷管所处环境只影响钯层沉积量。改进后的工艺比其他类型的化学镀具有较高的钯沉积速率，较短的制膜时间和较高的镀液利用率，使制膜成本降低，且钯层与陶瓷管结合牢固。     

Homogeneous deuteriodeiodination of iodinated tyrosine in angiotensin‐I using synthesized triethyl[2H]silane and Pd(0)

In our efforts to develop new reactions for the efficient labelling of peptides and proteins with tritium, we now report the use of silane hydrides together with homogenous Pd(0) catalysis for the protio‐ and deuteriodeiodination of an o‐iodo‐tyrosine containing peptide (angiotensin‐I) performed at room temperature. Copyright © 2010 John Wiley & Sons, Ltd.     

Improved Hydrogenation Kinetics of TiMn1.52 Alloy Coated with Palladium through Electroless Deposition

The deterioration of hydrogen charging performances resulting from the surface chemical action of electrophilic gases such as CO₂ is one of the prevailing drawbacks of TiMn_1.52 materials. In this study, we report the effect of autocatalytic Pd deposition on the morphology, structure, and hydrogenation kinetics of TiMn_1.52 alloy. Both the uncoated and Pd-coated materials were characterized using scanning electron microscopy/energy dispersive spectroscopy (SEM/EDS) and X-ray diffraction (XRD). XRD analyses indicated that TiMn_1.52 alloy contains C14-type Laves phase without any second phase, while the SEM images, together with a particle size distribution histogram, showed a smooth non-porous surface with irregular-shaped particles ranging in size from 1 to 8 µm. The XRD pattern of Pd-coated alloy revealed that C14-type Laves phase was still maintained upon Pd deposition. This was further supported by calculated crystallite size of 29 nm for both materials. Furthermore, a Sieverts-type apparatus was used to study the kinetics of the alloys after pre-exposure to air and upon vacuum heating at 300 °C. The Pd-coated AB₂ alloy exhibited good coating quality as confirmed by EDS with enhanced hydrogen absorption kinetics, even without activation. This is attributed to improved surface tolerance and a hydrogen spillover mechanism, facilitated by Pd nanoparticles. Vacuum heating at 300 °C resulted in removal of surface barriers and showed improved hydrogen absorption performances for both coated and uncoated alloys.     

In Situ Photogeneration of Palladium Nanoparticles in Thermoplastic Polyurethane: Photopatterning and Enhanced Oxygen Barrier Property

A solid phase synthesis of sub 5 nm palladium nanoparticles (Pd NP) by in situ photogeneration in thermoplastic polyurethane (TPU) composite films containing metal precursor and organic photoreducing agent is reported. The technique is highly facile, controllable, and potentially scalable to production quantities. Selective reduction and photopatterning can also be afforded using a shadow mask. The TPU films with Pd NP significantly enhance the barrier property by 64%. This photochemical approach shows promise for the fabrication of oxygen scavenging packaging systems for food, pharmaceutical, and electronics applications as well as for other products that require low oxygen storage atmosphere.