Application of immobilized lipase in production of camptosar (CPT-11)

Lipase fromPseudomonas cepaica (Amano, PS-30) was immobilized on celite and used in organic solvent for the selective acylation of a key alcohol intermediate. The compound was transformed in the synthesis to the anticancer drug Camptosar (CPT-11). Catalyst activity was influenced by the water content and method used to dry the catalyst. This resolution has been conducted on production scale with equal weight of recyclable catalyst.     

pH/redox/thermo-stimulative nanogels with enhanced thermosensitivity via incorporation of cationic and anionic components for anticancer drug delivery

To explore the potential biomedical applications of nanogels, it is a key factor to improve their thermosensitivity. In this paper, triple-responsive nanogels poly(N-isopropylacrylamide–N,N′-dimethylaminoethyl methacrylate–acrylic acid) (PNDA) were synthesized via in situ incorporating both cationic components and anionic components into a normal thermosensitive polymer matrix. The triple-monomer constructed PNDA nanogels displayed an enhanced thermosensitivity as compared with dual-monomer constructed PND nanogels. The PNDA nanogels presented higher encapsulation efficiency (～89%) and exhibited better pH/redox/thermo-responsivenesses in an anticancer drug delivery. In vitro biological study indicated that the PNDA nanogels have excellent biocompatibility and improved anticancer cytotoxicity to A549 cells after loading drug DOX.     

Anticancer activity of Carica papaya: A review

Carica papaya is widely cultivated in tropical and subtropical countries and is used as food as well as traditional medicine to treat a range of diseases. Increasing anecdotal reports of its effects in cancer treatment and prevention, with many successful cases, have warranted that these pharmacological properties be scientifically validated. A bibliographic search was conducted using the key words “papaya”, “anticancer”, and “antitumor” along with cross‐referencing. No clinical or animal cancer studies were identified and only seven in vitro cell‐culture‐based studies were reported; these indicate that C. papaya extracts may alter the growth of several types of cancer cell lines. However, many studies focused on specific compounds in papaya and reported bioactivity including anticancer effects. This review summarizes the results of extract‐based or specific compound‐based investigations and emphasizes the aspects that warrant future research to explore the bioactives in C. papaya for their anticancer activities.     

In Vitro and In Vivo Preparation Evaluations of Bleomycin Implants and Microspheres Prepared with DL-Poly (Lactide-Co-Glycolide)

ABSTRACT

In this investigation, poly(lactide-co-glycolide) (PLGA) gel implants and microspheric depot systems of bleomycin (BLM) were formulated and evaluated in vivo in mice bearing transplantable solid tumor (fibrosarcoma). The pharmacodynamic studies showed that both the formulations retarded tumor growth significantly (p < 0.05) when compared to the control animals (without any drug treatment). Preliminary pharmacokinetic studies illustrated controlled release of the drug into the systemic circulation to elicit the anti-neoplastic action. The gel implants showed better release characteristics and greater pharmacodynamic action when compared to the microspheres, thus demonstrating the feasibility of employing biodegradable depot polymer gel matrix for chronic cancer therapy.     

Anticancer therapeutic self-aggregates of sphingolipid metabolite-grafted poly(amino acid)-derivative and their enhanced intracellular delivery

Novel sphingolipid metabolite conjugated poly(amino acid)-derivative, poly-α,β-(2-hydroxylethyl l-aspartamide)-g-phytosphingosine copolymer, was designed as an anticancer prodrug-type carrier for enhanced intracellular uptake and physicochemical properties of polymeric micelle-like aggregates were evaluated. The resultant micelle-like aggregates showed a spherical shape and uniform size with a diameter less than 20 nm in an aqueous solution upon the increased number of phytosphingosine grafts. By the steady-state fluorescence of pyrene in aqueous polymer solutions, critical aggregation concentration (CAC) was obtained in the range of 0.166–0.0036 mg/ml and K_v, equilibrium partition constants of the pyrene in the self-aggregate solutions were estimated to be from 2.39 × 10³ to 1.96 × 10⁶. Phytosphingosine-grafted polymeric micelle-like aggregates as small as 20 nm were efficiently delivered into various cancer cell lines including oral, breast and colon carcinoma with the extent which is comparable to the level of targeting carrier system. The enhanced cellular uptake and anticancer therapeutic effect was evaluated by flow cytometry, confocal laser scanning microscopy (CLSM), and MTT assay.     

Comparative study on the potentialities of two halophytic species in the green synthesis of gold nanoparticles and their anticancer,antioxidant and catalytic efficiencies

In the current investigation, a comparative study between stems of two halophytic species; Atriplex halimus and Chenopodium amperosidies in a single step, efficient and environmentally safe phytosynthesis of gold nanoparticles (AuNPs) is reported. The green synthesized AuNPs were characterized using various techniques. Results showed the formation of violet-colored, mostly spherical-shaped AuNPs with a particle size of 2–10 nm for A. halimus-AuNPs and up to 40 nm for C. amperosidies-AuNPs. The plasmon peak of UV–Visible spectroscopy appeared at 535 nm for both AuNPs samples, confirming the successful phytosynthesis of AuNPs. The cytotoxicity investigation using MTT assay denoted a comparatively higher efficiency of A. halimus-AuNPs than C. amperosidies-AuNPs in inhibiting the proliferation of human breast cancer cells (MCF7 cell line). The recorded cell viability was 35.64 μg/mL for A. halimus-AuNPs and 38.46 μg/mL for C. amperosidies-AuNPs. The antioxidant efficiency of A. halimus-AuNPs was one-fold higher than that of C. amperosidies-AuNPs. Likewise, the catalytic degradation efficiency of methylene blue by A. halimus-AuNPs was noticeably higher than that of the other sample. Thus, reflects the relatively higher efficacy of A. halimus’ stem aqueous extract in the phytosynthesis of AuNPs compared to those of C. amperosidies.     

Green synthesis of gold nanoparticles using Parsley leaves extract and their applications as an alternative catalytic,antioxidant, anticancer,and antibacterial agents

For the first time in this study, gold nanoparticles (AuNPs) were biosynthesized by the eco-friendly and cost-effective procedure using Presley leaf (Petroselinum crispum) extract then used as antioxidant, anticancer, antibacterial and photocatalytic agents. Different four-volume of the extract 2.5 mL, 5 mL, 10 mL, and 20 ML named AuNPs(A), AuNPs(B), AuNPs(C) and AuNPs(D) were used to module the size and shape of AuNPs. The prepared NPs were characterized by various techniques including UV–Vis absorption spectroscopy, Transmission Electron Microscopy (TEM), dynamic light scattering (EDX), and X-ray diffractometric (XRD). TEM imaging confirmed the formation of spherical, semi-rod aggregates, and flower-shaped NPs. The reduction and stabilization effect of the plant extract to fabricate AuNPs were explained by FTIR analysis. The four AuNPs provided high antioxidant ability, while AuNPs(D) was the best one. The NPs showed an emerging antimicrobial activity against two gram-negative microbes and not effective against the gram-positive microbes. The photocatalytic capacity for degradation of methylene blue dye was achieved after only one minute (the four samples have an equal effect). The AuNPs(D) provide the best anticancer activity on the human cancerous colorectal cell line using MTT assay rather than the other three AuNPs. The results spotlight for using Presley as a common cheap plant for bio-fabricating AuNPs who possess huge multifunctional applications.     

2—哌嗪羧酸的合成

设计了一套从基本化工原料,合成一种可能具有抗肿瘤作用的基因栽体物质的路线,通过实验得到了标题化合物,证明了本方案合理,可行。     

Study on the electrochemical behaviour of the anticancer herbal drug emodin

The electrochemical behaviour of the anticancer herbal drug emodin was investigated by cyclic voltammetry (CV) at glassy carbon electrode. In 0.05 M NH₃-NH₄Cl (50% ethanol, pH 7.2) buffer solution, a pair of quasi-reversible redox peaks at potentials of Ep1 = −0.688 V and Ep2 = −0.628 V and one irreversible anodic peak, which was a typical anodic peak of emodin, at Ep3 = −0.235 V appeared at a scan rate of 100 mV/s. The irreversible anodic peak currents are linearly related to the emodin concentrations in a range from 8.9 × 10⁻⁸ M to 7.8 × 10⁻⁶ M with a pre-concentration time of 80 s under −0.620 V. Using the established method without pretreatment and pre-separation, emodin in herbal drug was determined with satisfactory results. Moreover, the electrode process dynamics parameters were also investigated by electrochemical techniques.