Screening of Indian Plants for Biological Activity: Part VII - Spermicidal Activity of Indian Plants

Extracts of about 1600 Indian plants were tested in vitro on rat and/or human spermatozoa. Thirty extracts showed spermicidal activity in rat and of these 16 caused instantaneous immobilization of human spermatozoa.

Screening of Indian Plants for Biological Activity : Part VIII

Extracts of 644 plant materials were screened for tannins and 204 extracts gave a positive test. Quantitative evaluation of tannins in positive extracts showed that 16 contained appreciable quantities. Insecticidal activity was tested against Musco domestica and Tribolium casteneum in 162 extracts and was confirmed in 17 and 4 extracts respectively.

Screening of Indian Plants for Biological Activity : Part IX

Two hundred and ninety three botanically identified plant materials have been tested as 50% ethanol extracts, for a wide variety of biological activities including antifertility, anticancer, chemotherapeutic and pharmaceutical activities. Biological activity has been confirmed in fractions of 40 of these extracts.

Screening of Indian Plants for Biological Activity: Part X

Two hundred eightythree botanically identified plant species have been tested as 50% ethanol extracts, for a wide variety of biological activities including antifertility, anticancer, chemotherapeutic and pharmaceutical activities. Biological activity has been observed in 143 of these extracts. The biological Activity has been confirmed in the fraction of 35 extracts and anticancer activity in the extracts of 23 plant species.

Screeningof Indian Plants for Biological Activity :Part XII

Alcoholic extracts of 295 botanically identified plant materials from 267 plant species have been tested for a wide variety of biological activities including chemotherapeutic and pharmacological screenings. Biological activities have been confirmed in fractions of 64 of these extracts. Follow-up studies have been carried out in some plants with confirmed activity. The active principles and results of these studies are reported.

Screening of Indian Plants for Biological Activity : Part XIII

Alcoholic extracts of 300 botanically identified plant materials from 287 plant species have been tested for various biological activities including chemotherapeutic and pharmacological screenings. Biological activities have been confirmed in 51 fractions of the extracts. Follow-up studies have been carried out in some plants with confirmed activity. The active principles and results of these studies are reported.

Screening of Indian plants for biological activity : Part XIV

Alcoholic extracts of 300 botanically identified plant materials from 275 plant species have been tested for various biological activities including chemotherapeutic and pharmacological screenings. Biological activities have been observed in 111 extracts. Follow-up studies have been carried out in some plants with confirmed activity. The active principles and results of these studies are reported.

Screening of Indian plants for biological activity: Part XV

Alcoholics extracts of 266 botanically identified plant materials from 222 plant species have been tested for various biological activities including chemotherapeutic and pharmacological screenings. Biological activities have been observed in 89 extracts. Follow-up studies have been carried out in some plants with confirmed activity. The active principles and results of these studies are reported.

Screening of Indian plants for biological activity: Part XVI

Alcoholic extracts of 288 of plant materials from 199 plant species have been tested for various biological activities including chemotherapeutic and pharmacological screening. Biological activities, ranging from moderate to good degree, have been observed in 61 plants extracts. Follow up studies have been carried out in these extracts and some of them have shown moderate degree of activities at this Institute. However, none of the extracts was found to be good enough for further development. Results of the present studies, alongwith chemical investigations on different species of similar genera which were screened earlier, are also discussed.

Synthesis and Biological Activity of 7,8,9-Trideoxy- and 7 R DesTHP-Peloruside A

The stereoselective syntheses of 7,8,9-trideoxypeloruside A (4) and a monocyclic peloruside A analogue lacking the entire tetrahydropyran moiety (3) are described. The syntheses proceeded through the PMB-ether of an ω-hydroxy β-keto aldehyde as a common intermediate which was elaborated into a pair of diastereomeric 1,3-syn and -anti diols by stereoselective Duthaler–Hafner allylations and subsequent 1,3-syn or anti reduction. One of these isomers was further converted into a tetrahydropyran derivative in a high-yielding Prins reaction, to provide the precursor for bicyclic analogue 4. Downstream steps for both syntheses included the substrate-controlled addition of a vinyl lithium intermediate to an aldehyde, thus connecting the peloruside side chain to C15 (C13) of the macrocyclic core structure in a fully stereoselective fashion. In the case of monocyclic 3 macrocyclization was based on ring-closing olefin metathesis (RCM), while bicyclic 4 was cyclized through Yamaguchi-type macrolactonization. The macrolactonization step was surprisingly difficult and was accompanied by extensive cyclic dimer formation. Peloruside A analogues 3 and 4 inhibited the proliferation of human cancer cell lines in vitro with micromolar and sub-micromolar IC50 values, respectively. The higher potency of 4 highlights the importance of the bicyclic core structure of peloruside A for nM biological activity.

STUDIES ON THE BIOLOGICAL ACTIVITY OF MACROMOLECULES MICROINJECTED INTO MAMMALIAN SOMATIC CELLS

Red Blood cell mediated and glass needle mediated microinjection technology was used to introduce macromolecules into mammalian somatic cells. The biological activities of DNA synthesis inducing factor(s) (Chapter 1), mitotic factor(s) (Chapter 2), and DNA coding for ovalbumin and thymidine kinase (Chapter 3) were studied following injection into mammalian somatic cells.^ Chapter 1. A cell undergoing DNA replication (S phase) contains a factor(s) that induces DNA synthesis prematurely in a G(,1) nucleus when an S phase cell is fused to a G(,1) cell. An assay for the active factor(s) was developed in which a mixture of s phase extract loaded red blood cells (RBC) and synchronous G(,1) HeLa cells was centrifuged onto Concanavalin A (Con A) treated coverslips and fused by PEG. This technique is called "Centrifusion". The synchronous G(,1) HeLa cells injected with S phase extract initiated DNA synthesis earlier than the control G(,1) cells mock injected with RBC loaded with buffer.^ Chapter 2. It has been demonstrated that fusion between a mitotic and an interphase cell usually leads to breakdown of the interphase nucleus, followed by condensation of the interphase chromatin into discrete chromosomes, a process termed premature chromosome condensation. I wanted to develop an assay for the mitotic factor(s) that induces premature chromosome condensation. Experiments were performed utilizing glass needle mediated microinjection of HeLa cell mitotic extract into interphase somatic mammalian cells in an attempt to induce premature chromosome condensation. However, I was not able to induce premature chromosome condensation in the interphase cells, probably because of an inability to introduce sufficient mitotic factor(s) into the cells.^ Chapter 3. A recombinant plasmid containing the chicken ovalbumin gene and three copies of the Herpes thymidine Kinase gene (pOV12-TK) was introduced into mouse LMTK('-) cell nuclei using glass needle mediated gene transfer resulting in LMTK('+) clones that were selected for in HAT medium. Restriction enzyme analysis of the high molecular weight DNA from 6 HAT medium survivor cell clones revealed the presence of one or at best only a few copies of the 12kb ovalbumin gene per mouse genome. Further analysis showed the ovalbumin DNA was not rearranged and was associated with high molecular weight mouse cell DNA. Each of the analyzed cell clones produced ovalbumin demonstrating that the biological activity of the microinjected ovalbumin was retained. ^