ArticlePublisher preview available

The composition and anti-inflammatory properties of pumpkin seeds

To read the full-text of this research, you can request a copy directly from the authors.


Pumpkin seeds (PSs) are common in daily diet, which have diverse biological activities. We characterized the metabolome of PSs and revealed their anti-inflammation mechanism that have not been fully elucidated. The air-dried and powdered PSs were extracted and reconstituted in 600 μl phosphate buffer for NMR analyses, and fatty acid profile was analyzed by GC–MS. The fatty acid esters of hydroxy fatty acids (FAHFAs) were analyzed by HPLC–MS, and anti-inflammatory activity of oleic acid ester of hydroxy oleic acid (OAHOA) was explored in vitro and in vivo. Finally, analysis of variance was performed (statistically significant when P < 0.05). PSs were mainly composed of oleic acid (18:1), linoleic acid (18:2△9,12), amino acids, sugars, trigonelline, and betaine. Further we identified OAHOA in PSs and discovered that OAHOA reduced inflammation in adipose tissue by inhibiting the expression of cytokines IL-12, IL-1β, and TNF-α. The metabolic profile of PSs was established, especially the fatty acids composition. This research revealed that the anti-inflammatory effects of PSs might be exerted through FAHFAs.
Journal of Food Measurement and Characterization (2021) 15:1834–1842
1 3
The composition andanti‑inflammatory properties ofpumpkin seeds
Xin‑JieDong1· Jun‑YanChen1· Shu‑FenChen1· YunLi1· Xiu‑JuZhao1
Received: 16 May 2020 / Accepted: 11 December 2020 / Published online: 3 January 2021
© The Author(s), under exclusive licence to Springer Science+Business Media, LLC part of Springer Nature 2021
Pumpkin seeds (PSs) are common in daily diet, which have diverse biological activities. We characterized the metabolome
of PSs and revealed their anti-inflammation mechanism that have not been fully elucidated. The air-dried and powdered
PSs were extracted and reconstituted in 600 μl phosphate buffer for NMR analyses, and fatty acid profile was analyzed by
GC–MS. The fatty acid esters of hydroxy fatty acids (FAHFAs) were analyzed by HPLC–MS, and anti-inflammatory activ-
ity of oleic acid ester of hydroxy oleic acid (OAHOA) was explored invitro and invivo. Finally, analysis of variance was
performed (statistically significant when P < 0.05). PSs were mainly composed of oleic acid (18:1), linoleic acid (18:29,12),
amino acids, sugars, trigonelline, and betaine. Further we identified OAHOA in PSs and discovered that OAHOA reduced
inflammation in adipose tissue by inhibiting the expression of cytokines IL-12, IL-1β, and TNF-α. The metabolic profile
of PSs was established, especially the fatty acids composition. This research revealed that the anti-inflammatory effects of
PSs might be exerted through FAHFAs.
Keywords Anti-inflammation· Fatty acid esters of hydroxy fatty acids (FAHFAs)· Metabolomics/metabonomics·
Pumpkin seeds
Pumpkin (Cucurbita moschata), one of the most common
vegetables consumed in the world, has been produced as
food because of the high nutrient contents. Modern research
shows that pumpkin contains a variety of functional fac-
tors for anti-diabetes, anti-inflammation and anti-cancer and
so on [1, 2]. Furthermore, the pumpkin seeds (PSs) are a
valuable source of protein and fat, have the positive health
effects. Their extracts of secondary metabolites could stimu-
late metabolism of accumulated fats and are functional for
immunomodulation, reproductive health, therapeutics over
a widespread of disease situations [3]. In food industry, PS
paste is a replacement of pork backfat due to their higher
lipid oxidation stability and lower rancidity value [4]. In
short, PS have unique effects not only as edible but as medic-
inal, too.
China has a long history of planting pumpkin [5] as
snacks, anti-diabetic foods and beverages. Research has
been reported on compositions of pumpkins but not much
on PS, mainly focused on the PS oil, PS shell fiber and PS
meal [68]. Briefly, the metabolite profile of PS has not been
utterly elucidated.
Metabolomics is quantitative exploration of dynamic
multivariate metabolic responses of complex organisms
subject to physiology or perturbation [9, 10]. The data of
metabolomics comes from nuclear magnetic resonance
(NMR) spectroscopy, chromatography, mass spectrom-
etry (MS), which can be used to characterize and compre-
hensively assay different concentrations and categories of
metabolites. Furthermore, metabolomics employs multivari-
ate pattern recognition methods to provide a suitable tool for
overall modeling, dimensionality reduction, reorganization,
differentiation, prediction, and visualization of biological
metabolites. By combining metabolic network map, metab-
olomics can be constructed with specific biological meta-
bolic fingerprinting (profile) to provide basic information for
Supplementary Information The online version contains
supplementary material available at https ://
4-020-00783 -9.
* Xiu-Ju Zhao
1 Team ofNeonatal & Infant Development, Health
andNutrition, NDHN School ofBiology andPharmaceutical
Engineering, Wuhan Polytechnic University, 68 South
Xuefu Road, Changqing Garden, Wuhan430023,
Content courtesy of Springer Nature, terms of use apply. Rights reserved.
... β-karoten adalah senyawa dengan struktur mengandung beberapa kromofor. Penentuan komposisi bebagai molekul aktif tumbuhan seperti flavonoid, vitamin C, β-karoten, polifenolik, dan beberapa kompenen penting lainnya menggunakan spektrofotometri UV-Vis telah banyak dilaporkan (Bogacz-Radomska & Harasym, 2018;Chao et al., 2022;Dong et al., 2021;Lapedes, 1977). Sehingga metode Spektrofotometri UV-Vis dapat digunakan untuk mengukur kadar β-karoten daging dan biji labu kuning menggunakan pelarut heksan dan etanol pada penelitian ini. ...
Full-text available
Kandungan gizi labu kuning cukup lengkap dengan harga yang relatif terjangkau, serta ketersediaan labu kuning di Indonesia yang berlimpah. Namun pemanfaatanya masih sangat terbatas, karena masyarakat masih belum menyadari akan potensi dan kandungan gizi yang dimiliki buah labu. Penelitian ini bertujuan untuk mengetahui hasil pengukuran β-karoten pada daging labu kuning (cucurbita moschata durch) menggunakan pelarut etanol, metanol dan heksan. Metode penelitian yang digunakan daam penelitian ini adalah metode kuantitatif deskriptif dengan analisis uji laboratorium. Peralatan yang digunakan dalam penelitian ini adalah gelas kimia 250 mL, pipet tetes, spatula, neraca analitik (Ohauss), HPLC, oven, labu ukur 50 mL dan 100 mL, tabung reaksi, rak tabung, erlemeyer, kaca arloji, gelas ukur, kertas saring dan blender. Bahan yang digunakan dalam penelitian ini adalah labu kuning, heksan (p.a), aseton (p.a), etanol 96%, metanol, aquadest, β-karoten standar, dan Spekstrofotometri UV-Vis. Hasil penelitian ini menyatakan bahwa konsentrasi β-karoten pada daging labu kuning dipengaruhi oleh pelarut yang digunakan. Dan β-karoten pada daging labu kuning (DL) memiliki kelarutan yang cukup baik pada pelarut etanol yaitu 380,514 µg/g dengan warna larutan oranye dan jauh lebih pekat dibandingkan warna kelarutan pada pelarut metanol dan heksan.
... In addition to the use of pumpkin seeds as a snack in several world areas, these seeds possess several health benefits due to their constituents' nutritional and functional properties. For example, pumpkin seeds are a significant source of fat and protein that positively affects human health, and the secondary metabolite extracts stimulate accumulated fat metabolism with functional properties for immunomodulation, reproductive health, therapeutics against several diseases [2][3][4]. Pumpkin fruits are used for many purposes as food and ornaments. Therefore, pumpkin fruit is very healthful, with a balanced combination of beneficial and healthy nutrients for human diets. ...
Full-text available
Background Germplasm identification is an essential connection linking the conservation and exploitation of crop genetic resources in several plant breeding programs. This study highlights the biochemical and molecular variations in a collection of pumpkin genotypes representing four climate zones. The information could help improve germplasm management and sustainable exploitation of the neglected genotypes. Methods and results Chemical characterization and genetic diversity among nine Egyptian landraces of pumpkin (Cucurbita moschata Duchesne) were estimated using Diode Array (DDA) Near Infra-Red (NIR) technology and the Inter simple Sequence Repeat markers (ISSR). Pumpkin seeds were collected from various geographical parts of Egypt. The spectroscopic properties of pumpkin seeds were used to quantify the fat, moisture, protein, ash, fiber, and total carbohydrate contents. The ten ISSR primers generated a total number of 46 genotype-specific bands, and the total polymorphism produced in the tested landraces was 63.58%. Based on the ISSR data, the polymorphism analysis divided the nine pumpkin landraces into two main groups, two subgroups, and four sub subgroups. The most diverse pumpkin landraces were Alexandria and Sohag, with a similarity percentage of 49.6%. However, the highest calculated similarity value was 88.3% between Matruh and Gharbia. The resultant genotype-specific bands can be used as markers for future genotypic characterization of pumpkins. Conclusions The study results could be helpful in the chemical phenotypic characterization and the parental selection and planning for future breeding programs for pumpkin improvement.
... The chemical composition and biological properties of different parts of C. moschata have been examined in many investigations confirming that pumpkins have a wide range of bioactivities, such as anti-diabetes, anti-inflammation, hepatoprotective, anticancer, and anti-obesity properties [15][16][17][18][19][20][21][22]. These properties are generally attributedto the content of phenolic acids [23]. ...
Full-text available
Cucurbita moschata Duchesne (Cucurbitaceae) is a plant food highly appreciated for the content of nutrients and bioactive compounds, including polyphenols and carotenoids, which contribute to its antioxidant and antimicrobial capacities. The purpose of this study was to identify phenolic acids and flavonoids of Cucurbita moschata Duchesne using high-performance liquid chromatography–diode array detection–electrospray ionization tandem mass spectrometry (HPLC–DAD–ESI-MS) at different ripening stages (young, mature, ripened) and determine its antioxidant and antimicrobial activities. According to the results, phenolic acids and flavonoids were dependent on the maturity stage. The mature fruits contain the highest total phenolic and flavonoids contents (97.4 mg GAE. 100 g−1 and 28.6 mg QE. 100 g−1).A total of 33 compounds were identified. Syringic acid was the most abundant compound (37%), followed by cinnamic acid (12%) and protocatechuic acid (11%). Polyphenol extract of the mature fruits showed the highest antioxidant activity when measured by DPPH (0.065 μmol TE/g) and ABTS (0.074 μmol TE/g) assays. In the antimicrobial assay, the second stage of ripening had the highest antibacterial activity. Staphylococcus aureus was the most sensitive strain with an inhibition zone of 12 mm and a MIC of 0.75 mg L−1. The lowest inhibition zone was obtained with Salmonella typhimurium (5 mm), and the MIC value was 10 mg L−1.
Full-text available
Background Seeking cures for chronic inflammation-associated diseases and infectious diseases caused by critical human pathogens is challenging and time-consuming. Even as the research community searches for novel bioactive agents, consuming a healthy diet with functional ability might be an effective way to delay and prevent the progression of severe health conditions. Many plant ingredients in Thai food are considered medicinal, and these vegetables, herbs, and spices collectively possess multiple biological and pharmacological activities, such as anti-inflammatory, antimicrobial, antidiabetic, antipyretic, anticancer, hepatoprotective, and cardioprotective effects. Methodology In this review, the selected edible plants are unspecific to Thai food, but our unique blend of recipes and preparation techniques make traditional Thai food healthy and functional. We searched three electronic databases: PUBMED, Science Direct, and Google Scholar, using the specific keywords “Plant name” followed by “Anti-inflammatory” or “Antibacterial” or “Antiviral” and focusing on articles published between 2017 and 2021. Results Our selection of 69 edible and medicinal plant species (33 families) is the most comprehensive compilation of Thai food sources demonstrating biological activities to date. Focusing on articles published between 2017 and 2021, we identified a total of 245 scientific articles that have reported main compounds, traditional uses, and pharmacological and biological activities from plant parts of the selected species. Conclusions Evidence indicates that the selected plants contain bioactive compounds responsible for anti-inflammatory, antibacterial, and antiviral properties, suggesting these plants as potential sources for bioactive agents and suitable for consumption for health benefits.
Full-text available
The number of metabolic syndromes (MetS) is increasing, and a fish phospholipid diet can reduce the risk of MetS. In this study, the changes in lipid metabolism of colon contents were analyzed by extensive lipidomics in mice with metabolic syndrome by fish phospholipid diet, and mice were randomly divided into experimental groups with different diet types by establishing a MetS model. After 14 weeks, the mice were sacrificed and the serum and colon contents were collected. Ultra-high liquid phase tandem mass spectrometry was used for broadly targeted lipidomic analysis, and the qualitative and quantitative detection of lipid metabolism changes in the colonic contents of mice. Under the intervention of fish phospholipids, MetS mice were significantly inhibited, serum total cholesterol (TC) and triglycerides (TG) decreased, serum high-density lipoprotein (HDL-C) and low-density lipoprotein (LDL-C) levels were improved, fasting blood glucose and insulin levels decreased, and inflammatory factors decreased. Through screening, it was found that thirty-three lipid metabolites may be key metabolites and five have significantly changed metabolic pathways. Modularizing lipid metabolites, it is possible to understand the extent to which different types and concentrations of fish phospholipids affect metabolic syndrome. Therefore, our study may provide new therapeutic clues for improving MetS.
Full-text available
Oil seeds are a natural source of phytochemicals with high nutritional value. The present study aims to evaluate for the first time the antioxidant, enzyme inhibitory, and anti-inflammatory activities in vitro and in vivo, as well as the physicochemical properties, fatty acid compositions, total polyphenol, flavonoid, and tocopherol contents of Algerian Prunus amygdalus var. amara cold-pressed oil. Bitter almond produces seeds that yield 35.5% of oil. It was characterized by a high saponification index of 215.94 mg KOH g⁻¹ of oil, a peroxide value of 7.74 meq O2kg of oil, a K232 of 2.612, and a K270 of 0.39. This oil represented a valuable source of healthy fatty acids. GC–MS analysis revealed oleic (68.27%) and linoleic (16.14%) as the main fatty acids. α-Tocopherol (85.77 mg/kg) was found to be the major component. The total phenolic and flavonoid contents were 21.94 ± 0.29 and 21.52 ± 0.14 µg/mL, respectively. The oil showed good antioxidant activity (A0.50 = 34 ± 0.44 μg/mL) using the CUPRAC assay and modest activity with DPPH, ABTS, FRAP, and β-carotene assays, respectively. BAO (bitter almond oil) displayed the most promising α-glucosidase and α-amylase activities compared to acarbose as a reference molecule and moderate acetylcholinesterase (AChE) inhibitory activity. Moreover, BAO demonstrated in vitro and in vivo anti-inflammatory efficacy in a dose-dependent manner, comparable to that of diclofenac sodium. These effects were confirmed by histological examinations. Overall, our results showed that BAO has a strong potential to design new industrial preparations with nutritional, pharmaceutical, and cosmeceutical applications. Graphical abstract
Full-text available
Dietary oils have critical influences on human health, and thermally cooking or frying modify the components and nutritional functions of oils. Palm oil was the most widely used oil in food processing industry, but its health effects remain debatable. In the current study, we aimed to compare the effects of thermally oxidized palm oil and canola oil on gut microbiota. Palm oil or canola oil were heated at 180 °C for 10 hours to prepare high-fat diets. Rats were fed high-fat diets for 3 months, and hematological properties, gut microflora composition and intestinal gene expression were examined. The results indicated that heated canola oil consumption elevated plasma total cholesterol and LDL-c levels compared with unheated canola oil, but heated palm oil do not had these effects; and consumption of heated palm oil significantly elevated the relative abundance of Lactobacillucs and Roseburia in gut, compared with non-heated palm oil or two canola oil groups. Moreover, intestinal expression of IL-22 was increased in heated palm oil fed animal, though ZO-1 and GPR41 were reduced. In conclusion, heating process may enhance the effects of palm oil on proliferation of probiotics Lactobacillucs, and weaken the effects of canola oil on cholesterol transport and metabolism.
Full-text available
Microbial lipids have been considered as promising resources for the production of renewable biofuels and oleochemicals. Various feedstocks, including sugars, crude glycerol, and volatile fatty acids, have been used as substrates for microbial lipid production, yet amino acid (AA) wastes remain to be evaluated. Here, we describe the potential to use AA wastes for lipid production with a two-stage culture mode by an oleaginous yeast strain Rhodosporidium toruloides CGMCC 2.1389. Each of the 20 proteinogenic AAs was evaluated individually as sole carbon source, with 8 showing capability to facilitate cellular lipid contents of more than 20%. It was found that L-proline was the most favored AA, with which cells accumulated lipids to a cellular lipid content of 37.3%. When blends with AA profiles corresponding to those of meat industry by-products and sheep viscera were used, the cellular lipid contents reached 27.0% and 28.7%, respectively. The fatty acid compositional analysis of these lipid products revealed similar profiles to those of vegetable oils. These results, thus, demonstrate a potential route to convert AA wastes into lipids, which is of great importance for waste management and biofuel production.
Full-text available
Hyperlipidemia dynamics need to be elucidated. 90 Kunming male mice were randomly divided into 18 groups, control groups, and high fat diet groups at 9 time points. On days 7, 10, 15, 18, 21, 24, 28, 31, and 35, the mice were anesthetized and blood was collected into tubes from the eyes. Sections of livers were taken. The plasma glycerol, glucose, leucine, arginine, betaine, lysine, glutamine, glutamate, valine, alanine, and choline were significantly different between the high fat diet groups and the corresponding controls (P < 0.05; VIP > 1). Therefore, the eleven metabolites may be used as potential biomarkers of hyperlipidemia. Based on the Spearman correlation analysis, it was found that valine was significantly associated with C22:6 from the 28th day to the end of the experiment, implying that these two metabolites may be a key point in subsequent research. These significantly affected metabolic pathways, namely arginine biosynthesis, D-glutamine and D-glutamate metabolism, alanine, aspartate and glutamate metabolism, were involved in the pathophysiological process of hyperlipidemia.
Full-text available
Oleogel from soybean oil and pumpkin seed paste were proposed as full replacements for pork backfat to decrease the saturated fat contents and improve the PUFA/SFA ratio in meat batters. Textural compression, along with shear and penetration tests provided similar information related to meat batter structure according to the type of fat, showing that a tougher but brittle texture was produced. Meat batters with fat replacers were darker and less red, but more yellow due to the incorporation of vegetable oil. Both hue angle (H) and saturation index (S) values increased due to changes in color components, in addition to a higher total color difference compared to the control sample. Soybean oil oleogel increased the PUFA content considerably, maintaining a total fat content close to the control sample. Pumpkin seed paste increased PUFA but also reduced to caloric content due lower fat content. Consumers preferred pumpkin seed paste samples regardless of the color difference and lower fat content. Fat replacers employed to replace pork backfat substantially modified the fatty acid profile and decreased lipid oxidation with no detrimental effects on texture or acceptance.
Full-text available
Scope : The aim of this study was to examine whether perilla oil supplementation would improve glucolipid metabolism and modulate gut microbiota in diabetic KKAy mice. Methods and results : The successfully established diabetic KKAy mice were randomized into 4 groups: diabetic model (DM), low‐dose perilla oil (LPO), middle‐dose perilla oil (MPO), and high‐dose perilla oil (HPO). C57BL/6J mice were fed chow diet as normal control (NC). At the end of 12 weeks, mice were euthanized and glucolipid indications were analyzed. Gut microbiota analysis were investigated based on the sequencing results on V4 region of 16S rRNA. Although serum glucose, insulin, total cholesterol, low density lipoprotein cholesterol, high density lipoprotein cholesterol, abundance‐based coverage estimator and shannon were unchanged, serum triglyceride significantly decreased in LPO compared with DM. The histopathological changes of hepatocellular macrovesicular steatosis and adipocyte hypertrophy were ameliorated by perilla oil supplementation. Blautia was significantly decreased in LPO, MPO and HPO, compared with DM. Nonmetric multidimensional scaling analysis showed NC and LPO were relatively coherent. Conclusion : These findings indicate that dietary supplementation with perilla oil can improve hypertriglyceridemia and gut dysbiosis in diabetic KKAy mice, which could be associated with potential benefits to human health. This article is protected by copyright. All rights reserved
Full-text available
Few studies have investigated the influence of increased amounts of dietary linoleic acid on the epidermal lipid biochemistry and TEWL in healthy subject. The influence of dietary linoleic acid on canine stratum corneum (SC) lipids was studied by feeding two groups of five dogs differential amounts of linoleic acid (LA) for three months. SC was harvested by tape stripping and lipids were analyzed by thin-layer chromatography and mass spectrometry. The dogs that were fed the higher concentration of LA showed high increases in the contents of both linoleic acid and free ceramides in the SC, whereas the protein-bound ceramide content was unchanged. Acylacids that represent the esterified form of linoleic acid in omega hydroxy very long chain fatty acids (ω-OH VLCFA) accounted for most of the elevation of LA, whereas the concentration of the free form was not significantly changed. Corroborating the absence of change in the protein-bound ceramides content of healthy dogs SC, TEWL was nearly unaffected by the linoleic acid-enriched diet.
Full-text available
Objective Non-alcoholic fatty liver disease (NAFLD) is a major public health burden in China, and its prevalence is increasing. This study aimed to determine the risk factors and biomarkers of NAFLD. Design An observational cross-sectional primary survey. Setting Central China. Participants The study included 1479 participants aged over 18 and below 80 years, not currently being treated for cancer or infectious disease or no surgery in the previous year, and no history of cancer or an infectious disease. Participants underwent clinical examination, metabolomic assay and anthropometric assessment. Univariate and logistic regression analyses were used to evaluate associations between covariates and NAFLD. Main outcome measures Risk factors and metabolic biomarkers including sex, body mass index, hypertension, body fat ratio, blood triglycerides, blood fasting glucose, liver enzyme elevation, uric acid and oleic acid-hydroxy oleic acid (OAHOA). Results Data from the 447 participants (mean age 44.3±11.9 years) were analysed, and the prevalence of NAFLD was 24.7%. Male sex (OR 3.484, 95% CI 2.028 to 5.988), body mass index ≥24 kg/m² (OR 8.494, 95% CI 5.581 to 12.928), body fat ratio (≥25 for women, ≥20 for men) (OR 1.833, 95% CI 1.286 to 2.756), triglycerides ≥1.7 mmol/L (OR 1.340, 95% CI 1.006 to 1.785), fasting glucose ≥6.1 mmol/L (OR 3.324, 95% CI 1.888 to 5.850), blood pressure ≥140/90 mm Hg or antihypertensive drug treatment (OR 1.451, 95% CI 1.069 to 1.970), uric acid (≥357 μmol/L for women, ≥416 μmol/L for men) (OR 2.755, 95% CI 2.009 to 3.778) and OAHOA (<5 nmol/L) (OR 1.340, 95% CI 1.006 to 1.785) were independent predictors of NAFLD (all P<0.05). These results were verified by all 1479 participants. Conclusions NAFLD was common among the study participants. In particular, NAFLD was correlated with uric acid. We identified OAHOA as a novel marker of NAFLD prevalence. It provides a reference on the prevention of NAFLD and related metabolic diseases with the rapid urbanisation, technological advancement and population ageing in China over the recent decades.
Enabling technologies have led to the design of new extraction protocols for naturally occurring compounds that are fast, sustainable and have low energy demands. Ultrasound-assisted extraction (UAE) and microwave-assisted extraction (MAE) have been used, in this study, for the recovery of valuable nutraceuticals and primary metabolites from pumpkin seeds (Curcubita sp.) and have been compared with conventional methods. In order to optimise extraction parameters and conditions, we have compared yields, total phenolic content, antioxidant activity, as well as fatty-acid and lipid profiles. The best yield, in both lipophilic and hydrophilic compounds, was achieved under UAE with a ternary solvent mixture (hexane/ethanol/water - 30:49:21). However, the highest phenolic content and antioxidant capacity were obtained using MAE under subcritical conditions with good extraction yields. The oil composition, as obtained using GC-FID analyses, showed a prevalence for unsaturated fatty acids; mainly linoleic and oleic acids. The use of UAE with ternary mixtures presented the highest lipid content and a slightly higher percentage of unsaturated compounds. Preliminary tests to verify the scalability of UAE with a ternary mixture showed that the extraction performance was maintained when using larger volumes (factor 10). This study will pave the road for the potential exploitation of UAE as a fast and efficient procedure for the simultaneous recovery of lipophilic and hydrophilic compounds from pumpkin seeds.
Metabolomics is an analytical approach to metabolism and involves quantitative and comparative analysis of low-molecular-weight metabolites in body fluids or cellular/tissues extracts. Owing to its ability to reveal disease-specific metabolic patterns or metabolic changes produced in response to a therapeutic intervention; it is gaining widespread applications virtually in all aspects of biomedical and pharmaceutical research pertaining to human healthcare management. It has also started playing a strategic role in pharmacological and toxicological research for evaluating therapeutic efficacy/safety of promising drug candidates either alone or in conjunction with other omics tools such as genomics, transcriptomics and proteomics. The metabolic profiling capabilities of nuclear magnetic resonance (NMR) spectroscopy along with pattern recognition methods have successfully been applied for identifying diagnostic panel of biomarkers, evaluating drug efficacy/safety, screening toxicity and disease mechanism. Particularly, the interest in applying NMR-based metabolomics for the assessment of therapeutic efficacy and safety is increasing among drug researchers and drug regulators owing to its non-destructive, non-selective and minimal sample preparation requirement. On top of this, it offers the potential for high-throughput (i.e. >100 samples a day is attainable) and provides highly reproducible results. In this review, we will discuss some of the recent developments related to NMR based metabolomics followed by some recent literature examples to highlight its potential in (a) the evaluation of therapeutic efficacy and safety of lead discovery compounds, (b) monitoring disease status and recovery after treatment and (c) identification and evaluation of biomarkers of systemic/organ-specific toxicity. Additionally, the review will also highlight its role to facilitate clinical trial testing and improve post-approval drug monitoring.