This research work includes the exploration of ethnobotanical, pharmacognostic, physicochemical and pharmacological aspects of Monotheca buxifolia (Falc.) A. DC. of the dicotyledonous family, Sapotaceae. It is locally known as ―Gurgura‖ and is used as a source of fuel, fodder, agricultural tools and for Honey bee farming in various areas of Khyber Pakhtunkhwa. Medicinally the fruits are used as a digestive, purgative, laxative, in urinary disorders, diuretic, vermifuge, refrigerant, tonic and in antiseptic pastes. Morphological, anatomical and organoleptic features of different parts of the plant (fruit, seed, leaf, stem bark and root bark) were worked out in detail. M. buxifolia had a palisade ratio of 6.75± 0.5, vein islets number 37.4±2.88 per mm2, vein termination number 35.4±1.8 per mm2, stomatal number of lower epidermis 77.4±3.57 per mm2 and 7.75± 0.97 on upper epidermis while stomatal index of lower epidermis 10.53±0.40 and upper epidermis 5.39±0.33. Stomata on the upper epidermis were of actinocytic type while on the lower epidermis actinostephanocytic type of stomata were present. The powder drug studies of the fruit, seed, leaf, stem bark and root bark showed characteristic fragments.The qualitative preliminary phytochemical screening of different parts of M. buxifolia gave positive indications for presence of aminoacids, proteins, reducing and nonreducing sugars, fixed oils, fats, glycosides, alkaloids, tannins, phenolic compounds, saponins, anthocyanins, Triterpenoids, phytosterols and Flavonoids in both aqueous and methanol extracts. The florescence behaviour, moisture contents and ash values were also worked out. The fruit pulp, seeds and leaves contained 8.33%, 10.62% and 0.56% fixed oil respectively. Linolenic acid, Oleic acid, Palmitic acid, Myristic acid and Stearic acid were the major component fatty acids. Elemental analysis of various parts of M. buxifolia revealed presence of good quantities of Nitrogen, potassium and phosphorus. Trace elements were found to be within the WHO permissible limits except for lead (22.48±0.33) and Cobalt iv (10.7±0.01), which exceeded the permissible limits in barks of stem and root respectively.The methanol extract of M. buxifolia fruit and leaf were tested at 500, 1000 and 2000 mg/kg body weight doses for any toxicological effects. They were found to be safe at all the tested doses.The methanol extracts of different parts of M. buxifolia were evaluated for their cytotoxic potentials against Artemia salina larvae. The fruit pulp had no visible cytotoxic effects. The seed extract produced most significant cytotoxic effects, giving an LD50 value of 4.668 (µg/ml) followed by root bark (31.265 µg/ml), leaf (97.59 µg/ml) and stem bark (199.65 µg/ml). In the in vitro spasmolytic bioassay the crude methanol extract of M. buxifolia fruit produced a significant inhibition of jejunal contractions through cholinergic pathway and voltage gated calcium channel blockade, similar to verapomil.The 250, 500 and 750 mg/kg doses of M. buxifolia fruit and leaf extracts produced significant antidiarrheal effects against Castor oil induced diarrhea in mice, in a dose dependent manner. The fruit extract caused 38.8%, 61% and 61.2% while the leaf extract caused 67.2%, 74.6% and 91.1% inhibition of faecal droppings, respectively, as compared to negative control. The 250 and 500 mg/kg doses of crude methanol extract of M. buxifolia fruit produced remarkable hepatoprotective activity against paracetamol induced hepatic damage in mice. the post-damage treatment was more effective and comparable to the standard hepatoprotective drug, Silymarin. The extract significantly (P ≤ 0.05) lowered the elevated levels of biochemical markers (Total Bilirubin, Direct Bilirubin, SGPT, alkaline phosphatase and Gamma‐GT) towards normal. Histopathological studies further confirmed hepatoprotective potentials of the plant. This study provides useful pharmacognostic standards for M. buxifolia and elaborates its pharmacological significance.