Cis- and trans-platinum and palladium complexes: a comparative study review as antitumour agents.

A large body of novel platinum and palladium complexes, in both the cis- and trans-forms, with various donor ligands, e.g. beta-carboline alkaloids, pyrazoles, DMSO, ferrocenylphosphines,...... have been tested for their antitumour activity against number of fluid suspension (P388, L1210, K562, and Raji) and solid tumour (KB, T47D, SW948, HeLa, A549, L929, Hep-2, RD,...) cell lines. Remarkable cytotoxic effects against these cell lines were observed by some of these complexes. The preliminary results indicated that most of the trans-palladium complexes showed a better activity than the cis-platinum isomers and superior activity than that of the cis-palladium isomers. More importantly they showed activities equal to (or superior than) those of cisplatin, carboplatin and oxaliplatin (the anti-cancer drugs) in vitro. Although these results are preliminary, however, encouraging since they are in a disagreement with the previous studies that cis-isomers are more active than trans-ones; the complexes which have not received the required attention from the vast number of researchers in this field.

Cytotoxic activity against a series of tumour cell lines of dimethyltin dichloride complexes with various donor ligands.

Several dimethyltin dichloride complexes of the general formula Me2SnCl2.L, where L = 8-hydroxy quinoline (L1), 8-hydroxy quinoline-N-oxide (L2),2,6-diaminopyridine (L3), 3-amino aniline (L4), cyclohexyl amine (L5), (1R, 2R)-1,2-cyclohexane diamine (L6), 3,5-dimethylpyrazole (L7), harmaline (L8) and harmine (L9), have been prepared and characterized physicochemically and spectroscopically. It was found that tin coordinated with the active site of these ligands to give complexes with penta-coordinated tin or, to some extent, hexa-coordinated tin. The cytotoxic activities of these complexes have been studied against Hep-2, HeLa, L20B and RD lines using the MTT-colorimetric assay. These activities were compared with those of the three reference standards, cisplatin, carboplatin and oxaliplatin. Some of these complexes exhibited a range of significant activities against the cell lines used, whereas no cytotoxic activities were exhibited by the rest of these complexes. The significance of these results is given and discussed.

Dimethyltin(IV) carboxylate compounds; synthesis, characterization and in vitro cytotoxic activity.

Six dimethyltin(IV) carboxylate compounds of the general formula Me2SnX2, where X = 1/2 O2(CO)2 (oxalate), 1/2 O2(CO)2CH2 (malonate), 1/2 O2(CO)2CH = CH (maleate), 1/2 O2(CO)2C-CH2CH2CH2 (cyclobutyl dicarboxylate), O(CO)C6H11 (cyclohexane carboxylate) and O(CO)CMe3 (pivolate) have been prepared and characterized physicochemically and spectroscopically. The cytotoxic activities of these carboxylates have been studied against HeLa, Hep-2, RD, L20B and P388 cell lines using the MTT-colorimetric assay. These activities were compared with the cytotoxic activities of the three reference standards, cisplatin, carboplatin and oxaliplatin. The compounds were X = 1/2 malonate, 1/2 maleate, cyclohexane carboxylate and pivolate exhibited a range of significant activities against the cell lines used, whereas no cytotoxic activities were exhibited by the rest of the six compounds. The significance of these results is given and discussed.

Cytotoxic activity of diorganotin(IV) complexes of some xanthate derivatives.

The cytotoxic activities of diorganotin(IV) complexes of some xanthate derivatives; R2Sn(SSCOR'), where R = Me, Bu(n), Ph and R' = C6H11 - (CyX), CH3NHCHCH2 - (MAEX), (CH3)2NCH2CH2 - (DMAEX), (CH3)2NCH2CH(CH3) - (DMAIX) and (C2H5)2NCH2CH2 - (DEAEX), have been studied against Hep-2, Hela, RD, L20B and BGM cell lines using the MTT-colorimetric assay. The present results indicated that moderate activities were demonstrated by the xanthate complexes of Bu(n)2Sn(IV) against four cell lines, whereas no cytotoxic activities were exhibited by both Me2Sn(IV) and Ph2Sn(IV) complexes of the xanthates. These activities were compared with the cytotoxic activities of two reference standards; the cisplatin and paraplatin complexes. The significance of these results is discussed.

Antibacterial evaluation of some xanthate derivatives and their diorganotin (IV) complexes.

The antibacterial activity of some xanthate derivatives K(SSCOR), where R = C6H5-(CyX), CH3NHCH2CH2-(MAEX), (CH3)2NCH2CH2-(DMAX), (CH3)2NCH2CH(CH3)-(DMAIX) and (C2H5)2NCH2CH2-(DEAEX) together with their diorganotin (IV) complexes R2Sn(SSCOR)2, where R' = Me, Bu(n), Ph, has been studied against eight species of bacteria in vitro. A significant activity against S. typhimurium was displayed by the xanthate derivative CyX and its complex Ph2Sn(CyX)2 at concentrations ranging from 1-10 micrograms/ml, and a remarkable activity was exhibited by the complexes Ph2Sn(CyX)2, Ph2Sn(MAEX)2 and Ph2Sn(DMAX)2 against P. aeruginosa at concentrations ranging from 0.1-10 micrograms/ml. By contrast, no such activity was demonstrated by the antibiotics used in this study (amoxicillin and chloramphenicol) against the same bacterial species.

Antibacterial and antiproliferative activities of vulpinic acids in vitro.

The antimicrobial and antiproliferative activities of vulpinic acids (1 a, b, c) have been assayed in vitro. Activity was demonstrated by vulpinic acids on Gram-positive bacteria only. The MIC values of these compounds were found to be ranging from 3.8-31.5 micrograms/ml. The significance of these results is discussed.

Synthesis and biological evaluation of N-salicyloyl-N-benzyl thiourea and 2,2-dimethyl-4-oxo-6-methoxy benzo-1,3-dioxin.

The synthesis of N-salicyloyl-N-benzyl-thiourea and 2,2-dimethyl-4-oxo-6-methoxy-benzo-1,3-dioxin are described. They were studied for their antiviral, antiproliferative and antimicrobial activities in vitro. N-salicyloyl-N-benzyl-thiourea exhibited significant activity against Gram-positive bacteria and against influenza viruses types A/Philippine/H3N2, A/Chilli/H1N1 and B/Paraha, as well as against K562 cell proliferation. By contrast, no such activity was demonstrated by 2,2-dimethyl-4-oxo-6-methoxy-benzo-1,3-dioxin.

Synthesis and characterization of novel biologically active platinum(II) and palladium(II) complexes of some beta-carboline alkaloids.

The preparation of novel biologically active platinum(II) and palladium(II) complexes of some beta-carboline alkaloids (harmaline, harmalol, harmine, and harmane) is described. These complexes, characterized on the basis of their CHN elemental analysis, infrared, Raman and 1H and 13C nuclear resonance spectral data, were shown to have the empirical formula [M(alkaloid)Cl2], M = Pt, Pd. The antitumor and antiviral activities of some of these complexes have been demonstrated.

Vulpinic acids inhibit influenza (RNA) viruses but not herpes (DNA) viruses.

Three synthetic vulpinic acids inhibited two influenza RNA viruses, type A (Philippine) and B (Paraha), in tissue culture with ID50 values ranging from 3.9 to 15.5 µg/ml. They had no activity against a third influenza virus or against two herpes viruses.

Synthesis and antiviral evaluation of 6-p-ethylphenyl-5H-pyrrolo [3,4-b]pyridine-5,7-dione.

The synthesis of 6-(p-ethylphenyl)-5H-pyrrolo [3,4-b]pyridine-5,7-dione is described. The compound has been studied for its in vitro activity on RNA-containing influenza viruses types A and B. The preliminary results indicate that the compound has a significant antiviral activity against influenza viruses types A and B at concentrations at which no cytotoxic effects on MRC-5 cells in tissue culture are present.

Histomorphological and histochemical studies on the epidermis of the lumbricid worm, Dendrobaena atheca Cernosvitov.

The epidermis of the fully mature earthworms, Dendrobaena atheca, has been investigated both histomorphologically and histochemically. The epidermis is constructed of two main cell categories: the glandular and nonglandular. The former comprises albumen, and small and large mucous cells whereas the latter includes supporting, basal and sensory cells. All these cell types rest on a prominent basement membrane and touch with their apices, except the basal cells, a thick layer of cuticle covering the epidermis. Epidermal cells are histomorphologically and/or histochemically distinguishable. Secretory granules of the albumen cells are proteinaceous in nature, those of the small mucous cells are neutral mucopolysaccharides and those of the large mucous cells are acid mucopolysaccharides. The histochemical nature of the cuticle indicates that it is mainly composed of neutral mucopolysaccharides and moieties of proteins and bound lipids.

[Histochemistry of neurosecretory cells in the cerebral ganglion of the adult or juvenile sweet water crab, Potamon magnum magnum (Pretzman)]. / Sur l'histochimie des cellules neurosécrétrices du ganglion cérébroïde du Crabe d'eau douce, Potamon magnum magnum (Pretzman), adulte ou juvénile.

The histochemistry of the neurosecretory material of the PF-positive neurosecretory cells of the cerebral ganglion of the adult and juvenile crab, Potamon magnum magnum (Pretzman) has been investigated. The PF-positive neurosecretory material is proteinaceous and contains considerable amounts of cystine; it is associated with significant amount of cytoplasmic RNA, lipids and phospholipids and with moderate amounts of carbohydrates, though no glycogen could be detected. The significance of these results is discussed.

Effect of tepa, shikonin and ecdysone on the alkaline phosphatase in the larvae Aedes aegypti (L.).

Effect of shikonin, tapa and ecdysone was studied on the activity of alkaline phosphatase by biochemical and histochemical methods. Tepa and shikonin (sterilants) inhibited the enzyme activity while ecdysone slightly increased the activity. This behaviour has been discussed in the present paper.

Observations on the lateral-line sense organs of the Salamander Neurergus crocatus crocatus Cope (Amphibia: Urodela).

The lateral-line system of the subadult and adult Neurergus crocatus crocatus Cope is retained throughout the life. It is constructed of pear-shaped sense organs or neuromasts which in the subadults are confined entirely to the epidermis with their apices opening distally to the exterior at the general level of the epidermal surface whereas in the adults they are embedded proximally more than halfway in the dermis with their distal apices opening into shallow grooves slightly below the regular epidermal surface. Dimensional differences are also observed between these organs in both stages. The neuromasts are constructed of 4 distinct cell types: sense cells, basal cells, sustentacular cells and mantle cells. These cells differ morphologically, structurally, topographically and functionally. The sense cells are clup-shaped, sensory, central in position and couched among the extremely elongated supporting basal and sustentacular cells, all of which are covered laterally by the extremely slender protective mantle cells. In both the mature and larvae, differences are observed among these cells in their size, number, location and arrangement. The sense organs are richly-supplied and well-nourished with vascular and nervous supplies.

Histochemical observations on the giant neurosecretory cells of the thoracic ganglion of the adult and juvenile crabs, Potamon magnum magnum (Pretzman).

The giant neurosecretory cells in the thoracic ganglion of the adult and juvenile crab, Potamon magnum magnum (Pretzman) were histochemically investigated. The secretion is mainly proteinaceous in nature, containing considerable amounts of acid mucosubstances, sulphate esters, lipids and a little carbohydrate but no glycogen. The detailed nature of proteinaceous neurosecretory material in the adult crab was further tested. It appears that the neurosecretory material of these cells contains moderate amounts of sulfhydryl groups and few of disulphide bonds. No trace of tyrosine could be observed. The neurosecretory granules were associated with considerable amounts of cytoplasmic RNA. In general, stronger reactions were obtained in summer and winter than in other seasons.

Seasonal changes in the histoenzymatic distribution of acid and alkaline phosphatases activity in the B cells of the thoracic ganglion of fresh-water crab, Potamon magnum magnum (Pretzman).

The present study deals with acid and alkaline phosphatases activity determination in B cells of the thoracie ganglion of Potamon magnum magnum. Intense alkaline and acid phosphatases activity is seen in the neurosecretory granules as well as in the neural sheath. Acid phosphatase activity unlike alkaline phosphatase distribution, is seen in form of positive stained spherules showing different pattern of distribution. Alkaline phosphatase activity is linked with the metabolic process. The significance of these results is discussed.

Further observations on the B-type neurosecretory cells in the thoracic ganglion of the crab, Potamon magnum magnum (Pretzman).

Only four types of the secretory neurones were observed in the thoracic ganglion of the fresh water crab, Potamon magnum magnum (Pretzman). These cells are classified as A, A', B and C types. Our results also confirmed that the B and B' types of cells (BAID et al. 1968) are one and the same type, the B cells. The B cells are of two forms, with and without the axons. They clearly showed sequential histological patterns pointing out to their phases. The secretory material is discharged either through the periphery or through the axon and periphery both. The vacuoles were observed in both the forms of the B cells. The remarkable sign of the activity of the nuclear membrane especially at the beginning of the secretory cycle and the appearance of the first secretory granules around the nucleus strongly support the vital role of the nucleus in the initiation of the secretory cycle.