This study was designed to explore the traditionally important plants Gaultheria trichophylla and Zanthoxylum armatum for various Pharmacognostic, biological and phytochemical parameters. Keeping in mind the importance of standardization and quality control of herbal drugs, various phamracognostic paratmeters were studied. These parameters include extractive values, ash values, loss on drying, shape, size, color, odor, and surface characteristics were noted for intact drug and powdered drug material. Light and scanning electron microscopic images of cross section of leaf and powdered microscopy revealed useful diagnostic features. Histochemical, phytochemical, physicochemical and fluorescence analysis proved useful tools to differentiate the powdered drug material. HPLC analysis showed the presence of important phytoconstituents; gallic acid, rutin and quercetin with antioxidant properties. In MTT anticancer assay, the methanol extract of G. trichohylla showed a significant dose depended inhibition of growth of MCF-7, MDA MB-468 and Caco-2 cancer cell lines from 10- 500 μg/ml concentrations. The crude saponins of G. trichophylla inhibited the growth of MCF- 7, MDA MB-468 and Caco-2 cancer cell lines by 71.56 (±3.76)% , 42.62(±4.42)%, and 93.59 (±5.00) % respectively, with respect to Actinomycin-D (4µM) which showed the growth inhibition of 62.04 (±1.43)% and 62.87 (±5.28)% respectively. In NRU assay the methanol extract of G. trichophylla showed highly significant dose dependent growth inhibition of the MCF-7, MDA MB-468, and Caco-2 cancer cell lines with dose of 50-100 μg/ml and above concentrations of extracts in each case. The saponins showed maximum effect and inhibited the growth of MCF-7, MDA MB-468, and Caco-2 by 87.29 (±2.88) %, 61.35(±14.88) %, 97.41 (±3.33) % and with respect to Actinomycin-D (4µM) which showed the growth inhibition of 91.84 (±3.73) %, 93.94 (±5.02) % and 65.97(±4.83) % respectively. The DAPI staining of saponins (G.Sa) treated cells clearly showed the numbers of apoptotic cells were higher as compared to untreated cells (Control). This was a clear indication of apoptosis induced in cancer cells. In MTT assay the methanol extract of Zanthoxylum armtum, fruit (Zf), bark (Zb) and leaves (Zl) showed a dose dependent growth inhibition of MCF-7, MDA MB-468, and Caco-2 cancer cell lines from 10-500 μg/ml. The Zf proved more effective and highly significant activity was observed with 200 μg/ml as compared to Zb (400 μg/ml) and Zl (300 μg/ml). The saponins from Z. armatum fruit (Zf.Sa), inhibited the MCF-7, MDA MB-468, and Caco-2 cancer cell lines by 79.89 (±7.45)%, 95 (±2.64)%, and 75.88 (±8.41) % respectively, the saponins from leaves (Zb.Sa) inhibited the growth by 9.43 (± 3.82), 94.59 (± 3.00), and 61.82 (± 4.07) respectively, saponins from leaves (Zl.Sa) inhibited the growth by 49.08 (± 5.21), 85.33 (± 3.41), and 68.62 (± 2.48) respectively. In NRU assay the Z.armatum Zf, Zb and Zl showed the dose dependent growth inhibition of the MCF-7, MDA MB-468, and Caco-2 cancer cell lines from 10-500 μg/ml concentrations. The highly significant response was observed with dose of 100 μg/ml for Zf and Zb and above 300 μg/ml for Zl. The saponins Zf.Sa inhibited the growth of MCF-7 and MDA MB-468 and Caco-2 cells by 81.67 (±4.15)%, 93.81(±2.32)%, and 53.16 (±3.31) % respectively, the saponins Zb.Sa inhibited the growth by 7.77 (± 4.83) and 95.25 (± 4.35) and 66.43 (± 3.24) respectively, and saponins of Zl.Sa inhibited the growth by 48.58 (±7.36), 71.19(± 2.76), and 45.96 (± 10.67) respectively. The DAPI staining and confocal microscopy of Zf-Sa, Zl-Sa, and Zl-Sa treated cells showed marked nuclear fragmentation and chromatin condensation. This is a clear indication of apoptosis induced in cancer cells. In antidiabetic assay, the methanol extract of G. trichophylla caused a significance (p<0.05) decrease in blood glucose level of Alloxan diabetic mice. Z. armatum leaves extract showed antidiabetic potential comparable with the standard drug (Glibenclamide). The Z. armatum bark and fruit extracts also showed significant (p<0.001) activity in Alloxan induced diabetic mice. The extract of G. trichophylla increase and Z. armatum extracts showed no prominent effect on the body weights of diabetic mice. Urea, creatinine, HDL, and Hb level were fairly improved in diabetic mice when treated with extracts of G. trichophylla and Z. armatum but both showed no prominent effect on proteins level. Total glycerides, total cholesterol and LDL level was decreased in normal and diabetic mice by extracts of two plants. Values for total phenolic contents of methanol, chloroform and hexane extracts of G. trichophylla were 17.58, 5.01, and 3.214 while for the methanol extracts of Z. armatum fruit, bark and leaves were 25.67, 15.54, and 13.12 GAE mg/g, of extract respectively. Flavonoids contents for methanol extract of G. trichophylla (41.345 QE/g) and for Z. armtum fruit extract 26.34QE/g were higher as compared with other extracts. The DPPH and FRAP antioxidant assays showed that methanol extract of G. trichophylla and Z. armatum fruit extracts have high flavonoids contents, therefore have the highest inhibition values as compared with other extracts. The methanol extract of G. trichophylla showed significant inhibition (83.46%) against BChE, 98.38% against alpha-glucosidase, and 94.70% against lipooxygenase enzyme. Z. armatum bark extract inhibited the BChE and lipooxygenase enzyme to 55.36%, and 54.92% respectively. While against alpha-glucosidase extracts of Z. armatum fruit, bark, and leaves extracts showed maximum inhibition of 83.76, 93.58, and 96.61% respectively. G. trichophylla and Z. armatum extracts reduced the frequency of defecation with 1000 mg/mL in in vivo experiments in mice. The methanol and chloroform extracts of G. trichophylla partially relaxed the spontaneous and K+ (80mM) induced contractions of isolated rabbit jejunum. Z. armatum fruit, bark and leaves extracts showed a concentration dependent inhibitory effect on spontaneous and K+ (80mM) induce contractions in isolated rabbit jejunum preparations with EC50 values of 0.7 and 3 mg/mL, 0.6 and 0.1 mg/mL, and 0.2 and 3 mg/mL respectively, predominantly through Ca++ channel blockade. The methanol, chloroform and hexane extracts of G. trichophylla showed concentration inhibitory effect on K+ (80mM) and carbochol induced isolated rabbit tracheal muscles contractions with EC50 values of 3.12 mg/mL, 0.645 and 2.26 mg/mL, and 6.58 and 0.61 mg/mL respectively. Z. armatum fruit, bark and leaves extracts inhibited the K+ (80mM) and carbochol induced contractions of isolated tracheal muscles with EC50 values of 2.4 and 0.9 mg/mL, 3.0 and 1.2 mg/mL, and 3.1 and 0.7 mg/mL respectively. Chloroform extract of G. trichophylla inhibited the P.E and K+ (80mM) induced contraction of isolated rabbit aorta muscles with EC50 values of 3.52 mg/mL and 5.53 mg/mL respectively. The fruit, bark and leaves extracts of Z. armatum inhibited the P.E and K+ (80mM) induced contraction of isolated rabbit aorta muscles with EC50values of 0.8 and 5 mg/mL, 0.03 and 2.6 mg/mL, and 1 and 5.5 mg/mL. The results showed that extracts of plant explored have potential gut modulatory, bronchodilatory, and cardiovascular activities. In phytochemical analysis, a total of 190 chemical constituents were identified in chromatographic isolated fractions of G. trichophylla extract with GC-MS. The predominant compounds identified belong to alkanes, terpenes, terpenoids, acids, esters, alcohols, aromatic compounds, nitrogen containing compounds (alkaloids), phenolic compounds and coumarins etc. Hydrodistilled essential oils of fruits and whole plant of G. trichophylla showed important volatile constituents like fenchone, linoleic acid, oleic acid, Norbornene, carane, succinic acid, benzoid acid, dodecinal and oxime etc.